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Patent code US10676465

Compile Data Set for Download or QSAR
Found 188 hits of Enzyme Inhibition Constant Data   
Target/Host
(Institution)
LigandTarget/Host
Links
Ligand
Links
Trg + Lig
Links
Ki
nM
ΔG°
kJ/mole
IC50
nM
Kd
nM
EC50
nM
koff
s-1
kon
M-1s-1
pHTemp
°C
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450629
PNG
(Ammonium 2-({4-[(2R)-2-(4-chloro-2-fluorophenyl)-2...)
Show SMILES C[C@@]1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4C[C@@H]4CCO4)C([O-])=O)CC3)c2O1)c1ccc(Cl)cc1F
Show InChI InChI=1S/C32H31ClFN3O5/c1-32(24-7-6-21(33)16-25(24)34)41-28-4-2-3-23(30(28)42-32)19-9-12-36(13-10-19)18-29-35-26-8-5-20(31(38)39)15-27(26)37(29)17-22-11-14-40-22/h2-8,15-16,19,22H,9-14,17-18H2,1H3,(H,38,39)/p-1/t22-,32-/m0/s1
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n/an/an/an/a 140n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450632
PNG
(US10676465, Example 9)
Show SMILES C[C@@]1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4C[C@@H]4CCO4)C(O)=O)CC3)c2O1)c1ccc(cc1F)C#N
Show InChI InChI=1S/C33H31FN4O5/c1-33(25-7-5-20(17-35)15-26(25)34)42-29-4-2-3-24(31(29)43-33)21-9-12-37(13-10-21)19-30-36-27-8-6-22(32(39)40)16-28(27)38(30)18-23-11-14-41-23/h2-8,15-16,21,23H,9-14,18-19H2,1H3,(H,39,40)/t23-,33-/m0/s1
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n/an/an/an/a 73n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450638
PNG
(2-{6-[2-(4-Chloro-2-fluorophenyl)-2-methyl-1,3-ben...)
Show SMILES COCCn1c(nc2ccc(cc12)C(=O)OC)[C@@H]1CC11CCN(CC1)c1cccc2OC(C)(Oc12)c1ccc(Cl)cc1F
Show InChI InChI=1S/C33H33ClFN3O5/c1-32(22-9-8-21(34)18-24(22)35)42-28-6-4-5-26(29(28)43-32)37-13-11-33(12-14-37)19-23(33)30-36-25-10-7-20(31(39)41-3)17-27(25)38(30)15-16-40-2/h4-10,17-18,23H,11-16,19H2,1-3H3/t23-,32?/m0/s1
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n/an/an/an/a>1.80E+4n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450643
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-1,3- benzodioxo...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(Oc23)c2ccc(Cl)cc2F)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C30H29ClFN3O5/c1-38-14-13-35-25-15-19(29(36)37)5-8-24(25)33-27(35)17-34-11-9-18(10-12-34)21-3-2-4-26-28(21)40-30(39-26)22-7-6-20(31)16-23(22)32/h2-8,15-16,18,30H,9-14,17H2,1H3,(H,36,37)
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n/an/an/an/a 17n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450660
PNG
(1-(2-methoxyethyl)-2-({4-[2-(2- methoxyphenyl)-2-m...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccccc2OC)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C32H35N3O6/c1-32(24-8-4-5-9-27(24)39-3)40-28-10-6-7-23(30(28)41-32)21-13-15-34(16-14-21)20-29-33-25-12-11-22(31(36)37)19-26(25)35(29)17-18-38-2/h4-12,19,21H,13-18,20H2,1-3H3,(H,36,37)
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n/an/an/an/a 81n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450661
PNG
(2-({4-[2-(4-fluorophenyl)-2-methyl-1,3- benzodioxo...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(F)cc2)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C31H32FN3O5/c1-31(22-7-9-23(32)10-8-22)39-27-5-3-4-24(29(27)40-31)20-12-14-34(15-13-20)19-28-33-25-11-6-21(30(36)37)18-26(25)35(28)16-17-38-2/h3-11,18,20H,12-17,19H2,1-2H3,(H,36,37)
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n/an/an/an/a 10n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450666
PNG
(1-{2-[acetyl(methyl)amino]ethyl}-2-({4-[2- (4-chlo...)
Show SMILES CN(CCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(Cl)cc2F)nc2ccc(cc12)C(O)=O)C(C)=O
Show InChI InChI=1S/C33H34ClFN4O5/c1-20(40)37(3)15-16-39-28-17-22(32(41)42)7-10-27(28)36-30(39)19-38-13-11-21(12-14-38)24-5-4-6-29-31(24)44-33(2,43-29)25-9-8-23(34)18-26(25)35/h4-10,17-18,21H,11-16,19H2,1-3H3,(H,41,42)
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n/an/an/an/a 65n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450669
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES CC1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4CCN4CCOC4=O)C(O)=O)CC3)c2O1)c1ccc(Cl)cc1F
Show InChI InChI=1S/C33H32ClFN4O6/c1-33(24-7-6-22(34)18-25(24)35)44-28-4-2-3-23(30(28)45-33)20-9-11-37(12-10-20)19-29-36-26-8-5-21(31(40)41)17-27(26)39(29)14-13-38-15-16-43-32(38)42/h2-8,17-18,20H,9-16,19H2,1H3,(H,40,41)
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n/an/an/an/a 5.20n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450670
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES CN(C)S(=O)(=O)CCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(Cl)cc2F)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C32H34ClFN4O6S/c1-32(24-9-8-22(33)18-25(24)34)43-28-6-4-5-23(30(28)44-32)20-11-13-37(14-12-20)19-29-35-26-10-7-21(31(39)40)17-27(26)38(29)15-16-45(41,42)36(2)3/h4-10,17-18,20H,11-16,19H2,1-3H3,(H,39,40)
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n/an/an/an/a 1.40E+3n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450673
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES CC1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4CCn4ccnc4)C(O)=O)CC3)c2O1)c1ccc(Cl)cc1F
Show InChI InChI=1S/C33H31ClFN5O4/c1-33(25-7-6-23(34)18-26(25)35)43-29-4-2-3-24(31(29)44-33)21-9-12-38(13-10-21)19-30-37-27-8-5-22(32(41)42)17-28(27)40(30)16-15-39-14-11-36-20-39/h2-8,11,14,17-18,20-21H,9-10,12-13,15-16,19H2,1H3,(H,41,42)
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n/an/an/an/a 140n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450679
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES CC1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4CC4CCOC4)C(O)=O)CC3)c2O1)c1ccc(Cl)cc1F
Show InChI InChI=1S/C33H33ClFN3O5/c1-33(25-7-6-23(34)16-26(25)35)42-29-4-2-3-24(31(29)43-33)21-9-12-37(13-10-21)18-30-36-27-8-5-22(32(39)40)15-28(27)38(30)17-20-11-14-41-19-20/h2-8,15-16,20-21H,9-14,17-19H2,1H3,(H,39,40)
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n/an/an/an/a 11n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450684
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES CC1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4C4CCOC4)C(O)=O)CC3)c2O1)c1ccc(Cl)cc1F
Show InChI InChI=1S/C32H31ClFN3O5/c1-32(24-7-6-21(33)16-25(24)34)41-28-4-2-3-23(30(28)42-32)19-9-12-36(13-10-19)17-29-35-26-8-5-20(31(38)39)15-27(26)37(29)22-11-14-40-18-22/h2-8,15-16,19,22H,9-14,17-18H2,1H3,(H,38,39)
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n/an/an/an/a 240n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450686
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES Cn1cc(Cn2c(CN3CCC(CC3)c3cccc4OC(C)(Oc34)c3ccc(Cl)cc3F)nc3ccc(cc23)C(O)=O)nn1
Show InChI InChI=1S/C32H30ClFN6O4/c1-32(24-8-7-21(33)15-25(24)34)43-28-5-3-4-23(30(28)44-32)19-10-12-39(13-11-19)18-29-35-26-9-6-20(31(41)42)14-27(26)40(29)17-22-16-38(2)37-36-22/h3-9,14-16,19H,10-13,17-18H2,1-2H3,(H,41,42)
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n/an/an/an/a 66n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450687
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES CC1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4C[C@H]4CCCO4)C(O)=O)CC3)c2O1)c1ccc(Cl)cc1F
Show InChI InChI=1S/C33H33ClFN3O5/c1-33(25-9-8-22(34)17-26(25)35)42-29-6-2-5-24(31(29)43-33)20-11-13-37(14-12-20)19-30-36-27-10-7-21(32(39)40)16-28(27)38(30)18-23-4-3-15-41-23/h2,5-10,16-17,20,23H,3-4,11-15,18-19H2,1H3,(H,39,40)/t23-,33?/m1/s1
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n/an/an/an/a 91n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450691
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES COCc1cc(Cn2c(CN3CCC(CC3)c3cccc4OC(C)(Oc34)c3ccc(Cl)cc3F)nc3ccc(cc23)C(O)=O)[nH]n1
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n/an/an/an/a 1.20E+3n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450694
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES CN(CCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(Cl)cc2F)nc2ccc(cc12)C(O)=O)S(C)(=O)=O
Show InChI InChI=1S/C32H34ClFN4O6S/c1-32(24-9-8-22(33)18-25(24)34)43-28-6-4-5-23(30(28)44-32)20-11-13-37(14-12-20)19-29-35-26-10-7-21(31(39)40)17-27(26)38(29)16-15-36(2)45(3,41)42/h4-10,17-18,20H,11-16,19H2,1-3H3,(H,39,40)
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n/an/an/an/a 6.80n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450694
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES CN(CCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(Cl)cc2F)nc2ccc(cc12)C(O)=O)S(C)(=O)=O
Show InChI InChI=1S/C32H34ClFN4O6S/c1-32(24-9-8-22(33)18-25(24)34)43-28-6-4-5-23(30(28)44-32)20-11-13-37(14-12-20)19-29-35-26-10-7-21(31(39)40)17-27(26)38(29)16-15-36(2)45(3,41)42/h4-10,17-18,20H,11-16,19H2,1-3H3,(H,39,40)
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n/an/an/an/a 74n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450697
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES CC1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4CCc4ncc[nH]4)C(O)=O)CC3)c2O1)c1ccc(Cl)cc1F
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n/an/an/an/a 460n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450698
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES CC1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4CCO)C(O)=O)CC3)c2O1)c1ccc(Cl)cc1F
Show InChI InChI=1S/C30H29ClFN3O5/c1-30(22-7-6-20(31)16-23(22)32)39-26-4-2-3-21(28(26)40-30)18-9-11-34(12-10-18)17-27-33-24-8-5-19(29(37)38)15-25(24)35(27)13-14-36/h2-8,15-16,18,36H,9-14,17H2,1H3,(H,37,38)
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n/an/an/an/a 1.00E+3n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450700
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES CCn1nncc1Cn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(Cl)cc2F)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C33H32ClFN6O4/c1-3-41-23(17-36-38-41)18-40-28-15-21(32(42)43)7-10-27(28)37-30(40)19-39-13-11-20(12-14-39)24-5-4-6-29-31(24)45-33(2,44-29)25-9-8-22(34)16-26(25)35/h4-10,15-17,20H,3,11-14,18-19H2,1-2H3,(H,42,43)
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n/an/an/an/a 7.60n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450702
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES Cn1cnnc1Cn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(Cl)cc2F)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C32H30ClFN6O4/c1-32(23-8-7-21(33)15-24(23)34)43-27-5-3-4-22(30(27)44-32)19-10-12-39(13-11-19)16-28-36-25-9-6-20(31(41)42)14-26(25)40(28)17-29-37-35-18-38(29)2/h3-9,14-15,18-19H,10-13,16-17H2,1-2H3,(H,41,42)
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n/an/an/an/a 4.5n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450708
PNG
(1-(2-methoxyethyl)-2-({4-[2-methyl-2-(4- methylphe...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(C)cc2)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C32H35N3O5/c1-21-7-10-24(11-8-21)32(2)39-28-6-4-5-25(30(28)40-32)22-13-15-34(16-14-22)20-29-33-26-12-9-23(31(36)37)19-27(26)35(29)17-18-38-3/h4-12,19,22H,13-18,20H2,1-3H3,(H,36,37)
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n/an/an/an/a 9.10n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450720
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-7- fluoro-2-met...)
Show SMILES CC1(Oc2c(O1)c(ccc2F)C1CCN(Cc2nc3ccc(cc3n2C[C@@H]2CCO2)C(O)=O)CC1)c1ccc(Cl)cc1F
Show InChI InChI=1S/C32H30ClF2N3O5/c1-32(23-5-3-20(33)15-25(23)35)42-29-22(4-6-24(34)30(29)43-32)18-8-11-37(12-9-18)17-28-36-26-7-2-19(31(39)40)14-27(26)38(28)16-21-10-13-41-21/h2-7,14-15,18,21H,8-13,16-17H2,1H3,(H,39,40)/t21-,32?/m0/s1
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n/an/an/an/a 11n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450720
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-7- fluoro-2-met...)
Show SMILES CC1(Oc2c(O1)c(ccc2F)C1CCN(Cc2nc3ccc(cc3n2C[C@@H]2CCO2)C(O)=O)CC1)c1ccc(Cl)cc1F
Show InChI InChI=1S/C32H30ClF2N3O5/c1-32(23-5-3-20(33)15-25(23)35)42-29-22(4-6-24(34)30(29)43-32)18-8-11-37(12-9-18)17-28-36-26-7-2-19(31(39)40)14-27(26)38(28)16-21-10-13-41-21/h2-7,14-15,18,21H,8-13,16-17H2,1H3,(H,39,40)/t21-,32?/m0/s1
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n/an/an/an/a 14n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450625
PNG
(US10676465, Example 2*)
Show SMILES COCCn1c(CN2CCN(CC2)c2cccc3O[C@@H](Oc23)c2ccc(Cl)cc2F)nc2ccc(cc12)C(=O)OC
Show InChI InChI=1S/C30H30ClFN4O5/c1-38-15-14-36-25-16-19(29(37)39-2)6-9-23(25)33-27(36)18-34-10-12-35(13-11-34)24-4-3-5-26-28(24)41-30(40-26)21-8-7-20(31)17-22(21)32/h3-9,16-17,30H,10-15,18H2,1-2H3/t30-/m0/s1
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n/an/an/an/a 260n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450629
PNG
(Ammonium 2-({4-[(2R)-2-(4-chloro-2-fluorophenyl)-2...)
Show SMILES C[C@@]1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4C[C@@H]4CCO4)C([O-])=O)CC3)c2O1)c1ccc(Cl)cc1F
Show InChI InChI=1S/C32H31ClFN3O5/c1-32(24-7-6-21(33)16-25(24)34)41-28-4-2-3-23(30(28)42-32)19-9-12-36(13-10-19)18-29-35-26-8-5-20(31(38)39)15-27(26)37(29)17-22-11-14-40-22/h2-8,15-16,19,22H,9-14,17-18H2,1H3,(H,38,39)/p-1/t22-,32-/m0/s1
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n/an/an/an/a 2.40E+3n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450633
PNG
(US10676465, Example 10)
Show SMILES C[C@@]1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4C[C@@H]4CCO4)C(O)=O)CC3)c2O1)c1ccc(Cl)cn1
Show InChI InChI=1S/C31H31ClN4O5/c1-31(27-8-6-21(32)16-33-27)40-26-4-2-3-23(29(26)41-31)19-9-12-35(13-10-19)18-28-34-24-7-5-20(30(37)38)15-25(24)36(28)17-22-11-14-39-22/h2-8,15-16,19,22H,9-14,17-18H2,1H3,(H,37,38)/t22-,31-/m0/s1
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n/an/an/an/a 0.960n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450639
PNG
(2-{6-[2-(4-Chloro-2-fluorophenyl)-2-methyl-1,3-ben...)
Show SMILES COCCn1c(nc2ccc(cc12)C(=O)OC)[C@H]1CC11CCN(CC1)c1cccc2OC(C)(Oc12)c1ccc(Cl)cc1F
Show InChI InChI=1S/C33H33ClFN3O5/c1-32(22-9-8-21(34)18-24(22)35)42-28-6-4-5-26(29(28)43-32)37-13-11-33(12-14-37)19-23(33)30-36-25-10-7-20(31(39)41-3)17-27(25)38(30)15-16-40-2/h4-10,17-18,23H,11-16,19H2,1-3H3/t23-,32?/m1/s1
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n/an/an/an/a 120n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450641
PNG
(Ammonium 2-({4-[2-(4-chloro-2-fluorophenyl)-2-meth...)
Show SMILES CCn1cncc1Cn1c(CN2CCC(CC2)c2cccc3O[C@](C)(Oc23)c2ccc(Cl)cc2F)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C34H33ClFN5O4/c1-3-40-20-37-17-24(40)18-41-29-15-22(33(42)43)7-10-28(29)38-31(41)19-39-13-11-21(12-14-39)25-5-4-6-30-32(25)45-34(2,44-30)26-9-8-23(35)16-27(26)36/h4-10,15-17,20-21H,3,11-14,18-19H2,1-2H3,(H,42,43)/t34-/m1/s1
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n/an/an/an/a 1.00E+3n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450642
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES COCCn1c(CN2CCN(CC2)c2cccc3OC(C)(Oc23)c2ccc(Cl)cc2F)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C30H30ClFN4O5/c1-30(21-8-7-20(31)17-22(21)32)40-26-5-3-4-24(28(26)41-30)35-12-10-34(11-13-35)18-27-33-23-9-6-19(29(37)38)16-25(23)36(27)14-15-39-2/h3-9,16-17H,10-15,18H2,1-2H3,(H,37,38)
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n/an/an/an/a 1.20n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450643
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-1,3- benzodioxo...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(Oc23)c2ccc(Cl)cc2F)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C30H29ClFN3O5/c1-38-14-13-35-25-15-19(29(36)37)5-8-24(25)33-27(35)17-34-11-9-18(10-12-34)21-3-2-4-26-28(21)40-30(39-26)22-7-6-20(31)16-23(22)32/h2-8,15-16,18,30H,9-14,17H2,1H3,(H,36,37)
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n/an/an/an/a 270n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450652
PNG
(2-({4-[2-(4-ethylphenyl)-2-methyl-1,3- benzodioxol...)
Show SMILES CCc1ccc(cc1)C1(C)Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4CCOC)C(O)=O)CC3)c2O1
Show InChI InChI=1S/C33H37N3O5/c1-4-22-8-11-25(12-9-22)33(2)40-29-7-5-6-26(31(29)41-33)23-14-16-35(17-15-23)21-30-34-27-13-10-24(32(37)38)20-28(27)36(30)18-19-39-3/h5-13,20,23H,4,14-19,21H2,1-3H3,(H,37,38)
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n/an/an/an/a 150n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450660
PNG
(1-(2-methoxyethyl)-2-({4-[2-(2- methoxyphenyl)-2-m...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccccc2OC)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C32H35N3O6/c1-32(24-8-4-5-9-27(24)39-3)40-28-10-6-7-23(30(28)41-32)21-13-15-34(16-14-21)20-29-33-25-12-11-22(31(36)37)19-26(25)35(29)17-18-38-2/h4-12,19,21H,13-18,20H2,1-3H3,(H,36,37)
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n/an/an/an/a 1.00E+3n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450661
PNG
(2-({4-[2-(4-fluorophenyl)-2-methyl-1,3- benzodioxo...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(F)cc2)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C31H32FN3O5/c1-31(22-7-9-23(32)10-8-22)39-27-5-3-4-24(29(27)40-31)20-12-14-34(15-13-20)19-28-33-25-11-6-21(30(36)37)18-26(25)35(28)16-17-38-2/h3-11,18,20H,12-17,19H2,1-2H3,(H,36,37)
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n/an/an/an/a 240n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450663
PNG
(1-(2-methoxyethyl)-2-[(4-{2-methyl-2-[4- (trifluor...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(cc2)C(F)(F)F)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C32H32F3N3O5/c1-31(22-7-9-23(10-8-22)32(33,34)35)42-27-5-3-4-24(29(27)43-31)20-12-14-37(15-13-20)19-28-36-25-11-6-21(30(39)40)18-26(25)38(28)16-17-41-2/h3-11,18,20H,12-17,19H2,1-2H3,(H,39,40)
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n/an/an/an/a 14n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450673
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES CC1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4CCn4ccnc4)C(O)=O)CC3)c2O1)c1ccc(Cl)cc1F
Show InChI InChI=1S/C33H31ClFN5O4/c1-33(25-7-6-23(34)18-26(25)35)43-29-4-2-3-24(31(29)44-33)21-9-12-38(13-10-21)19-30-37-27-8-5-22(32(41)42)17-28(27)40(30)16-15-39-14-11-36-20-39/h2-8,11,14,17-18,20-21H,9-10,12-13,15-16,19H2,1H3,(H,41,42)
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n/an/an/an/a 12n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450677
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES CC1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4CCCn4cncn4)C(O)=O)CC3)c2O1)c1ccc(Cl)cc1F
Show InChI InChI=1S/C33H32ClFN6O4/c1-33(25-8-7-23(34)17-26(25)35)44-29-5-2-4-24(31(29)45-33)21-10-14-39(15-11-21)18-30-38-27-9-6-22(32(42)43)16-28(27)41(30)13-3-12-40-20-36-19-37-40/h2,4-9,16-17,19-21H,3,10-15,18H2,1H3,(H,42,43)
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n/an/an/an/a 18n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450677
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES CC1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4CCCn4cncn4)C(O)=O)CC3)c2O1)c1ccc(Cl)cc1F
Show InChI InChI=1S/C33H32ClFN6O4/c1-33(25-8-7-23(34)17-26(25)35)44-29-5-2-4-24(31(29)45-33)21-10-14-39(15-11-21)18-30-38-27-9-6-22(32(42)43)16-28(27)41(30)13-3-12-40-20-36-19-37-40/h2,4-9,16-17,19-21H,3,10-15,18H2,1H3,(H,42,43)
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n/an/an/an/a 160n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450678
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES Cn1cnc(CCn2c(CN3CCC(CC3)c3cccc4OC(C)(Oc34)c3ccc(Cl)cc3F)nc3ccc(cc23)C(O)=O)c1
Show InChI InChI=1S/C34H33ClFN5O4/c1-34(26-8-7-23(35)17-27(26)36)44-30-5-3-4-25(32(30)45-34)21-10-13-40(14-11-21)19-31-38-28-9-6-22(33(42)43)16-29(28)41(31)15-12-24-18-39(2)20-37-24/h3-9,16-18,20-21H,10-15,19H2,1-2H3,(H,42,43)
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n/an/an/an/a 1.10E+3n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450695
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES CC1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4CC4(O)CCC4)C(O)=O)CC3)c2O1)c1ccc(Cl)cc1F
Show InChI InChI=1S/C33H33ClFN3O5/c1-32(24-8-7-22(34)17-25(24)35)42-28-5-2-4-23(30(28)43-32)20-10-14-37(15-11-20)18-29-36-26-9-6-21(31(39)40)16-27(26)38(29)19-33(41)12-3-13-33/h2,4-9,16-17,20,41H,3,10-15,18-19H2,1H3,(H,39,40)
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n/an/an/an/a 310n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450696
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES CC1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4Cc4cn[nH]c4)C(O)=O)CC3)c2O1)c1ccc(Cl)cc1F
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n/an/an/an/a 1.70n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450701
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES Cn1cnc(Cn2c(CN3CCC(CC3)c3cccc4OC(C)(Oc34)c3ccc(Cl)cc3F)nc3ccc(cc23)C(O)=O)c1
Show InChI InChI=1S/C33H31ClFN5O4/c1-33(25-8-7-22(34)15-26(25)35)43-29-5-3-4-24(31(29)44-33)20-10-12-39(13-11-20)18-30-37-27-9-6-21(32(41)42)14-28(27)40(30)17-23-16-38(2)19-36-23/h3-9,14-16,19-20H,10-13,17-18H2,1-2H3,(H,41,42)
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n/an/an/an/a 53n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450703
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES CC1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4C[C@@H]4CCCO4)C(O)=O)CC3)c2O1)c1ccc(Cl)cc1F
Show InChI InChI=1S/C33H33ClFN3O5/c1-33(25-9-8-22(34)17-26(25)35)42-29-6-2-5-24(31(29)43-33)20-11-13-37(14-12-20)19-30-36-27-10-7-21(32(39)40)16-28(27)38(30)18-23-4-3-15-41-23/h2,5-10,16-17,20,23H,3-4,11-15,18-19H2,1H3,(H,39,40)/t23-,33?/m0/s1
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n/an/an/an/a 1.40n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450705
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES CC1(Oc2cccc(C3CCN(Cc4nc5ccc(nc5n4Cc4cnco4)C(O)=O)CC3)c2O1)c1ccc(Cl)cc1F
Show InChI InChI=1S/C31H27ClFN5O5/c1-31(22-6-5-19(32)13-23(22)33)42-26-4-2-3-21(28(26)43-31)18-9-11-37(12-10-18)16-27-35-24-7-8-25(30(39)40)36-29(24)38(27)15-20-14-34-17-41-20/h2-8,13-14,17-18H,9-12,15-16H2,1H3,(H,39,40)
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n/an/an/an/a 29n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450706
PNG
(1-(2-methoxyethyl)-2-{[4-(2-methyl-2- phenyl-1,3-b...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccccc2)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C31H33N3O5/c1-31(23-7-4-3-5-8-23)38-27-10-6-9-24(29(27)39-31)21-13-15-33(16-14-21)20-28-32-25-12-11-22(30(35)36)19-26(25)34(28)17-18-37-2/h3-12,19,21H,13-18,20H2,1-2H3,(H,35,36)
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n/an/an/an/a 1.00E+3n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450709
PNG
(1-(2-methoxyethyl)-2-({4-[2-methyl-2-(3- methylphe...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2cccc(C)c2)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C32H35N3O5/c1-21-6-4-7-24(18-21)32(2)39-28-9-5-8-25(30(28)40-32)22-12-14-34(15-13-22)20-29-33-26-11-10-23(31(36)37)19-27(26)35(29)16-17-38-3/h4-11,18-19,22H,12-17,20H2,1-3H3,(H,36,37)
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n/an/an/an/a 230n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450710
PNG
(2-({4-[2-(2-chlorophenyl)-2-methyl-1,3- benzodioxo...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccccc2Cl)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C31H32ClN3O5/c1-31(23-7-3-4-8-24(23)32)39-27-9-5-6-22(29(27)40-31)20-12-14-34(15-13-20)19-28-33-25-11-10-21(30(36)37)18-26(25)35(28)16-17-38-2/h3-11,18,20H,12-17,19H2,1-2H3,(H,36,37)
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n/an/an/an/a 410n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450712
PNG
(1-(2-methoxyethyl)-2-({4-[2-methyl-2-(2- methylphe...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccccc2C)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C32H35N3O5/c1-21-7-4-5-9-25(21)32(2)39-28-10-6-8-24(30(28)40-32)22-13-15-34(16-14-22)20-29-33-26-12-11-23(31(36)37)19-27(26)35(29)17-18-38-3/h4-12,19,22H,13-18,20H2,1-3H3,(H,36,37)
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n/an/an/an/a 17n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450715
PNG
(US10676465, Example 91 | US10676465, Example 92 | ...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(Cl)cn2)nc2ccc(cc12)C([O-])=O
Show InChI InChI=1S/C30H31ClN4O5/c1-30(26-9-7-21(31)17-32-26)39-25-5-3-4-22(28(25)40-30)19-10-12-34(13-11-19)18-27-33-23-8-6-20(29(36)37)16-24(23)35(27)14-15-38-2/h3-9,16-17,19H,10-15,18H2,1-2H3,(H,36,37)/p-1
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n/an/an/an/a>2.00E+4n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450626
PNG
(2-({4-[2-(4-Chloro-2-fluorophenyl)-2-methyl-1,3-be...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(Cl)cc2F)nc2ncc(cc12)C(O)=O
Show InChI InChI=1S/C30H30ClFN4O5/c1-30(22-7-6-20(31)15-23(22)32)40-25-5-3-4-21(27(25)41-30)18-8-10-35(11-9-18)17-26-34-28-24(36(26)12-13-39-2)14-19(16-33-28)29(37)38/h3-7,14-16,18H,8-13,17H2,1-2H3,(H,37,38)
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n/an/an/an/a 1.30n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450634
PNG
(1-(2-Methoxyethyl)-2-({4-[2-methyl-2-(pyridin-3-yl...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3O[C@@](C)(Oc23)c2cccnc2)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C30H32N4O5/c1-30(22-5-4-12-31-18-22)38-26-7-3-6-23(28(26)39-30)20-10-13-33(14-11-20)19-27-32-24-9-8-21(29(35)36)17-25(24)34(27)15-16-37-2/h3-9,12,17-18,20H,10-11,13-16,19H2,1-2H3,(H,35,36)/t30-/m0/s1
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n/an/an/an/a 290n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450640
PNG
(Ammonium 2-({4-[2-(4-chloro-2-fluorophenyl)-2-meth...)
Show SMILES CCn1cncc1Cn1c(CN2CCC(CC2)c2cccc3O[C@@](C)(Oc23)c2ccc(Cl)cc2F)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C34H33ClFN5O4/c1-3-40-20-37-17-24(40)18-41-29-15-22(33(42)43)7-10-28(29)38-31(41)19-39-13-11-21(12-14-39)25-5-4-6-30-32(25)45-34(2,44-30)26-9-8-23(35)16-27(26)36/h4-10,15-17,20-21H,3,11-14,18-19H2,1-2H3,(H,42,43)/t34-/m0/s1
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n/an/an/an/a 0.0790n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450648
PNG
(2-{6-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-be...)
Show SMILES COCCn1c(nc2ccc(cc12)C(O)=O)C1CC11CCN(CC1)c1cccc2OC(C)(Oc12)c1ccc(Cl)cc1F
Show InChI InChI=1S/C32H31ClFN3O5/c1-31(21-8-7-20(33)17-23(21)34)41-27-5-3-4-25(28(27)42-31)36-12-10-32(11-13-36)18-22(32)29-35-24-9-6-19(30(38)39)16-26(24)37(29)14-15-40-2/h3-9,16-17,22H,10-15,18H2,1-2H3,(H,38,39)
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n/an/an/an/a>2.00E+4n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450648
PNG
(2-{6-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-be...)
Show SMILES COCCn1c(nc2ccc(cc12)C(O)=O)C1CC11CCN(CC1)c1cccc2OC(C)(Oc12)c1ccc(Cl)cc1F
Show InChI InChI=1S/C32H31ClFN3O5/c1-31(21-8-7-20(33)17-23(21)34)41-27-5-3-4-25(28(27)42-31)36-12-10-32(11-13-36)18-22(32)29-35-24-9-6-19(30(38)39)16-26(24)37(29)14-15-40-2/h3-9,16-17,22H,10-15,18H2,1-2H3,(H,38,39)
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n/an/an/an/a>2.00E+4n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450648
PNG
(2-{6-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-be...)
Show SMILES COCCn1c(nc2ccc(cc12)C(O)=O)C1CC11CCN(CC1)c1cccc2OC(C)(Oc12)c1ccc(Cl)cc1F
Show InChI InChI=1S/C32H31ClFN3O5/c1-31(21-8-7-20(33)17-23(21)34)41-27-5-3-4-25(28(27)42-31)36-12-10-32(11-13-36)18-22(32)29-35-24-9-6-19(30(38)39)16-26(24)37(29)14-15-40-2/h3-9,16-17,22H,10-15,18H2,1-2H3,(H,38,39)
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n/an/an/an/a>2.00E+4n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450653
PNG
(2-({4-[2-(3-fluoro-4-methoxyphenyl)-2- methyl-1,3-...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(OC)c(F)c2)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C32H34FN3O6/c1-32(22-8-10-27(40-3)24(33)18-22)41-28-6-4-5-23(30(28)42-32)20-11-13-35(14-12-20)19-29-34-25-9-7-21(31(37)38)17-26(25)36(29)15-16-39-2/h4-10,17-18,20H,11-16,19H2,1-3H3,(H,37,38)
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n/an/an/an/a 45n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450654
PNG
(2-({4-[2-(3-fluorophenyl)-2-methyl-1,3- benzodioxo...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2cccc(F)c2)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C31H32FN3O5/c1-31(22-5-3-6-23(32)18-22)39-27-8-4-7-24(29(27)40-31)20-11-13-34(14-12-20)19-28-33-25-10-9-21(30(36)37)17-26(25)35(28)15-16-38-2/h3-10,17-18,20H,11-16,19H2,1-2H3,(H,36,37)
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n/an/an/an/a 190n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450654
PNG
(2-({4-[2-(3-fluorophenyl)-2-methyl-1,3- benzodioxo...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2cccc(F)c2)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C31H32FN3O5/c1-31(22-5-3-6-23(32)18-22)39-27-8-4-7-24(29(27)40-31)20-11-13-34(14-12-20)19-28-33-25-10-9-21(30(36)37)17-26(25)35(28)15-16-38-2/h3-10,17-18,20H,11-16,19H2,1-2H3,(H,36,37)
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n/an/an/an/a 1.90E+3n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450655
PNG
(1-(2-methoxyethyl)-2-({4-[2-(4- methoxyphenyl)-2-m...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(OC)cc2)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C32H35N3O6/c1-32(23-8-10-24(39-3)11-9-23)40-28-6-4-5-25(30(28)41-32)21-13-15-34(16-14-21)20-29-33-26-12-7-22(31(36)37)19-27(26)35(29)17-18-38-2/h4-12,19,21H,13-18,20H2,1-3H3,(H,36,37)
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n/an/an/an/a 18n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450655
PNG
(1-(2-methoxyethyl)-2-({4-[2-(4- methoxyphenyl)-2-m...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(OC)cc2)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C32H35N3O6/c1-32(23-8-10-24(39-3)11-9-23)40-28-6-4-5-25(30(28)41-32)21-13-15-34(16-14-21)20-29-33-26-12-7-22(31(36)37)19-27(26)35(29)17-18-38-2/h4-12,19,21H,13-18,20H2,1-3H3,(H,36,37)
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n/an/an/an/a 450n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450667
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES CC1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4CCN4CCOCC4)C(O)=O)CC3)c2O1)c1ccc(Cl)cc1F
Show InChI InChI=1S/C34H36ClFN4O5/c1-34(26-7-6-24(35)20-27(26)36)44-30-4-2-3-25(32(30)45-34)22-9-11-39(12-10-22)21-31-37-28-8-5-23(33(41)42)19-29(28)40(31)14-13-38-15-17-43-18-16-38/h2-8,19-20,22H,9-18,21H2,1H3,(H,41,42)
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n/an/an/an/a 160n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450668
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES CC1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4Cc4ccccn4)C(O)=O)CC3)c2O1)c1ccc(Cl)cc1F
Show InChI InChI=1S/C34H30ClFN4O4/c1-34(26-10-9-23(35)18-27(26)36)43-30-7-4-6-25(32(30)44-34)21-12-15-39(16-13-21)20-31-38-28-11-8-22(33(41)42)17-29(28)40(31)19-24-5-2-3-14-37-24/h2-11,14,17-18,21H,12-13,15-16,19-20H2,1H3,(H,41,42)
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n/an/an/an/a 220n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450674
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES CCn1ccnc1Cn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(Cl)cc2F)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C34H33ClFN5O4/c1-3-40-16-13-37-30(40)20-41-28-17-22(33(42)43)7-10-27(28)38-31(41)19-39-14-11-21(12-15-39)24-5-4-6-29-32(24)45-34(2,44-29)25-9-8-23(35)18-26(25)36/h4-10,13,16-18,21H,3,11-12,14-15,19-20H2,1-2H3,(H,42,43)
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n/an/an/an/a 280n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450685
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES Cc1nccn1CCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(Cl)cc2F)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C34H33ClFN5O4/c1-21-37-12-15-40(21)16-17-41-29-18-23(33(42)43)6-9-28(29)38-31(41)20-39-13-10-22(11-14-39)25-4-3-5-30-32(25)45-34(2,44-30)26-8-7-24(35)19-27(26)36/h3-9,12,15,18-19,22H,10-11,13-14,16-17,20H2,1-2H3,(H,42,43)
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n/an/an/an/a 2.20n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450687
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES CC1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4C[C@H]4CCCO4)C(O)=O)CC3)c2O1)c1ccc(Cl)cc1F
Show InChI InChI=1S/C33H33ClFN3O5/c1-33(25-9-8-22(34)17-26(25)35)42-29-6-2-5-24(31(29)43-33)20-11-13-37(14-12-20)19-30-36-27-10-7-21(32(39)40)16-28(27)38(30)18-23-4-3-15-41-23/h2,5-10,16-17,20,23H,3-4,11-15,18-19H2,1H3,(H,39,40)/t23-,33?/m1/s1
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n/an/an/an/a 9.20n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450692
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES CC1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4Cc4cnco4)C(O)=O)CC3)c2O1)c1ccc(Cl)cc1F
Show InChI InChI=1S/C32H28ClFN4O5/c1-32(24-7-6-21(33)14-25(24)34)42-28-4-2-3-23(30(28)43-32)19-9-11-37(12-10-19)17-29-36-26-8-5-20(31(39)40)13-27(26)38(29)16-22-15-35-18-41-22/h2-8,13-15,18-19H,9-12,16-17H2,1H3,(H,39,40)
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n/an/an/an/a 10n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450705
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES CC1(Oc2cccc(C3CCN(Cc4nc5ccc(nc5n4Cc4cnco4)C(O)=O)CC3)c2O1)c1ccc(Cl)cc1F
Show InChI InChI=1S/C31H27ClFN5O5/c1-31(22-6-5-19(32)13-23(22)33)42-26-4-2-3-21(28(26)43-31)18-9-11-37(12-10-18)16-27-35-24-7-8-25(30(39)40)36-29(24)38(27)15-20-14-34-17-41-20/h2-8,13-14,17-18H,9-12,15-16H2,1H3,(H,39,40)
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n/an/an/an/a 54n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450707
PNG
(2-({4-[2-(2-chloro-4-methoxyphenyl)-2- methyl-1,3-...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(OC)cc2Cl)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C32H34ClN3O6/c1-32(24-9-8-22(40-3)18-25(24)33)41-28-6-4-5-23(30(28)42-32)20-11-13-35(14-12-20)19-29-34-26-10-7-21(31(37)38)17-27(26)36(29)15-16-39-2/h4-10,17-18,20H,11-16,19H2,1-3H3,(H,37,38)
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n/an/an/an/a 44n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450722
PNG
(US10676465, Example 98 | US10676465, Example 99 | ...)
Show SMILES CC1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4Cc4ncco4)C([O-])=O)CC3)c2O1)c1ccc(cc1F)C#N
Show InChI InChI=1S/C33H28FN5O5/c1-33(24-7-5-20(17-35)15-25(24)34)43-28-4-2-3-23(31(28)44-33)21-9-12-38(13-10-21)18-29-37-26-8-6-22(32(40)41)16-27(26)39(29)19-30-36-11-14-42-30/h2-8,11,14-16,21H,9-10,12-13,18-19H2,1H3,(H,40,41)/p-1
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n/an/an/an/a 440n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450724
PNG
(2-({4-[(2S)-2-(4-chloro-2-fluorophenyl)-2- methyl-...)
Show SMILES C[C@@]1(Oc2cccc(C3CCN(Cc4nc5ccc(C(O)=O)c(F)c5n4C[C@@H]4CCO4)CC3)c2O1)c1ccc(Cl)cc1F
Show InChI InChI=1S/C32H30ClF2N3O5/c1-32(23-7-5-19(33)15-24(23)34)42-26-4-2-3-21(30(26)43-32)18-9-12-37(13-10-18)17-27-36-25-8-6-22(31(39)40)28(35)29(25)38(27)16-20-11-14-41-20/h2-8,15,18,20H,9-14,16-17H2,1H3,(H,39,40)/t20-,32-/m0/s1
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n/an/an/an/a 7.60n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450726
PNG
(US10676465, Example 102)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(CO)(Oc23)c2ccccc2)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C31H33N3O6/c1-38-17-16-34-26-18-22(30(36)37)10-11-25(26)32-28(34)19-33-14-12-21(13-15-33)24-8-5-9-27-29(24)40-31(20-35,39-27)23-6-3-2-4-7-23/h2-11,18,21,35H,12-17,19-20H2,1H3,(H,36,37)
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n/an/an/an/a 600n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450628
PNG
(US10676465, Example 5**)
Show SMILES [O-]C(=O)c1ccc2nc(CN3CCC(CC3)c3cccc4O[C@@H](Oc34)c3ccc(Cl)cc3F)n(C[C@@H]3CCO3)c2c1
Show InChI InChI=1S/C31H29ClFN3O5/c32-20-5-6-23(24(33)15-20)31-40-27-3-1-2-22(29(27)41-31)18-8-11-35(12-9-18)17-28-34-25-7-4-19(30(37)38)14-26(25)36(28)16-21-10-13-39-21/h1-7,14-15,18,21,31H,8-13,16-17H2,(H,37,38)/p-1/t21-,31-/m0/s1
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n/an/an/an/a 1.30n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450628
PNG
(US10676465, Example 5**)
Show SMILES [O-]C(=O)c1ccc2nc(CN3CCC(CC3)c3cccc4O[C@@H](Oc34)c3ccc(Cl)cc3F)n(C[C@@H]3CCO3)c2c1
Show InChI InChI=1S/C31H29ClFN3O5/c32-20-5-6-23(24(33)15-20)31-40-27-3-1-2-22(29(27)41-31)18-8-11-35(12-9-18)17-28-34-25-7-4-19(30(37)38)14-26(25)36(28)16-21-10-13-39-21/h1-7,14-15,18,21,31H,8-13,16-17H2,(H,37,38)/p-1/t21-,31-/m0/s1
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n/an/an/an/a 23n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450630
PNG
(US10676465, Example 7**)
Show SMILES C[C@]1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4C[C@@H]4CCO4)C([O-])=O)CC3)c2O1)c1ccc(Cl)cc1F
Show InChI InChI=1S/C32H31ClFN3O5/c1-32(24-7-6-21(33)16-25(24)34)41-28-4-2-3-23(30(28)42-32)19-9-12-36(13-10-19)18-29-35-26-8-5-20(31(38)39)15-27(26)37(29)17-22-11-14-40-22/h2-8,15-16,19,22H,9-14,17-18H2,1H3,(H,38,39)/p-1/t22-,32+/m0/s1
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n/an/an/an/a 3.10n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450632
PNG
(US10676465, Example 9)
Show SMILES C[C@@]1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4C[C@@H]4CCO4)C(O)=O)CC3)c2O1)c1ccc(cc1F)C#N
Show InChI InChI=1S/C33H31FN4O5/c1-33(25-7-5-20(17-35)15-26(25)34)42-29-4-2-3-24(31(29)43-33)21-9-12-37(13-10-21)19-30-36-27-8-6-22(32(39)40)16-28(27)38(30)18-23-11-14-41-23/h2-8,15-16,21,23H,9-14,18-19H2,1H3,(H,39,40)/t23-,33-/m0/s1
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n/an/an/an/a 1.60E+3n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450637
PNG
(2-({4-[(2S)-2-(4-Chloro-2-fluorophenyl)-2-methyl-1...)
Show SMILES Cn1c(CN2CCC(CC2)c2cccc3O[C@@](C)(Oc23)c2ccc(Cl)cc2F)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C29H27ClFN3O4/c1-29(21-8-7-19(30)15-22(21)31)37-25-5-3-4-20(27(25)38-29)17-10-12-34(13-11-17)16-26-32-23-9-6-18(28(35)36)14-24(23)33(26)2/h3-9,14-15,17H,10-13,16H2,1-2H3,(H,35,36)/t29-/m0/s1
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n/an/an/an/a 7n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450643
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-1,3- benzodioxo...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(Oc23)c2ccc(Cl)cc2F)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C30H29ClFN3O5/c1-38-14-13-35-25-15-19(29(36)37)5-8-24(25)33-27(35)17-34-11-9-18(10-12-34)21-3-2-4-26-28(21)40-30(39-26)22-7-6-20(31)16-23(22)32/h2-8,15-16,18,30H,9-14,17H2,1H3,(H,36,37)
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n/an/an/an/a>2.00E+4n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450650
PNG
(2-({4-[2-(4-cyano-2-fluorophenyl)-1,3- benzodioxol...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(Oc23)c2ccc(cc2F)C#N)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C31H29FN4O5/c1-39-14-13-36-26-16-21(30(37)38)6-8-25(26)34-28(36)18-35-11-9-20(10-12-35)22-3-2-4-27-29(22)41-31(40-27)23-7-5-19(17-33)15-24(23)32/h2-8,15-16,20,31H,9-14,18H2,1H3,(H,37,38)
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n/an/an/an/a 61n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450664
PNG
(2-({4-[2-(3,4-difluorophenyl)-2-methyl- 1,3-benzod...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(F)c(C)c2)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C32H34FN3O5/c1-20-17-23(8-9-25(20)33)32(2)40-28-6-4-5-24(30(28)41-32)21-11-13-35(14-12-21)19-29-34-26-10-7-22(31(37)38)18-27(26)36(29)15-16-39-3/h4-10,17-18,21H,11-16,19H2,1-3H3,(H,37,38)
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n/an/an/an/a 2.00E+3n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450679
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES CC1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4CC4CCOC4)C(O)=O)CC3)c2O1)c1ccc(Cl)cc1F
Show InChI InChI=1S/C33H33ClFN3O5/c1-33(25-7-6-23(34)16-26(25)35)42-29-4-2-3-24(31(29)43-33)21-9-12-37(13-10-21)18-30-36-27-8-5-22(32(39)40)15-28(27)38(30)17-20-11-14-41-19-20/h2-8,15-16,20-21H,9-14,17-19H2,1H3,(H,39,40)
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n/an/an/an/a 1.20n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450680
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES Cn1ncnc1Cn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(Cl)cc2F)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C32H30ClFN6O4/c1-32(23-8-7-21(33)15-24(23)34)43-27-5-3-4-22(30(27)44-32)19-10-12-39(13-11-19)16-29-37-25-9-6-20(31(41)42)14-26(25)40(29)17-28-35-18-36-38(28)2/h3-9,14-15,18-19H,10-13,16-17H2,1-2H3,(H,41,42)
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n/an/an/an/a 500n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450685
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES Cc1nccn1CCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(Cl)cc2F)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C34H33ClFN5O4/c1-21-37-12-15-40(21)16-17-41-29-18-23(33(42)43)6-9-28(29)38-31(41)20-39-13-10-22(11-14-39)25-4-3-5-30-32(25)45-34(2,44-30)26-8-7-24(35)19-27(26)36/h3-9,12,15,18-19,22H,10-11,13-14,16-17,20H2,1-2H3,(H,42,43)
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n/an/an/an/a 82n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450692
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES CC1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4Cc4cnco4)C(O)=O)CC3)c2O1)c1ccc(Cl)cc1F
Show InChI InChI=1S/C32H28ClFN4O5/c1-32(24-7-6-21(33)14-25(24)34)42-28-4-2-3-23(30(28)43-32)19-9-11-37(12-10-19)17-29-36-26-8-5-20(31(39)40)13-27(26)38(29)16-22-15-35-18-41-22/h2-8,13-15,18-19H,9-12,16-17H2,1H3,(H,39,40)
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n/an/an/an/a 8.30n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450693
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES COCCn1cnnc1Cn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(Cl)cc2F)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C34H34ClFN6O5/c1-34(25-8-7-23(35)17-26(25)36)46-29-5-3-4-24(32(29)47-34)21-10-12-40(13-11-21)18-30-38-27-9-6-22(33(43)44)16-28(27)42(30)19-31-39-37-20-41(31)14-15-45-2/h3-9,16-17,20-21H,10-15,18-19H2,1-2H3,(H,43,44)
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n/an/an/an/a 2.80n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450695
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES CC1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4CC4(O)CCC4)C(O)=O)CC3)c2O1)c1ccc(Cl)cc1F
Show InChI InChI=1S/C33H33ClFN3O5/c1-32(24-8-7-22(34)17-25(24)35)42-28-5-2-4-23(30(28)43-32)20-10-14-37(15-11-20)18-29-36-26-9-6-21(31(39)40)16-27(26)38(29)19-33(41)12-3-13-33/h2,4-9,16-17,20,41H,3,10-15,18-19H2,1H3,(H,39,40)
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n/an/an/an/a 14n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450696
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES CC1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4Cc4cn[nH]c4)C(O)=O)CC3)c2O1)c1ccc(Cl)cc1F
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n/an/an/an/a 10n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450704
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES CC1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4Cc4ncco4)C(O)=O)CC3)c2O1)c1ccc(Cl)cc1F
Show InChI InChI=1S/C32H28ClFN4O5/c1-32(23-7-6-21(33)16-24(23)34)42-27-4-2-3-22(30(27)43-32)19-9-12-37(13-10-19)17-28-36-25-8-5-20(31(39)40)15-26(25)38(28)18-29-35-11-14-41-29/h2-8,11,14-16,19H,9-10,12-13,17-18H2,1H3,(H,39,40)
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n/an/an/an/a 6.90n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450715
PNG
(US10676465, Example 91 | US10676465, Example 92 | ...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(Cl)cn2)nc2ccc(cc12)C([O-])=O
Show InChI InChI=1S/C30H31ClN4O5/c1-30(26-9-7-21(31)17-32-26)39-25-5-3-4-22(28(25)40-30)19-10-12-34(13-11-19)18-27-33-23-8-6-20(29(36)37)16-24(23)35(27)14-15-38-2/h3-9,16-17,19H,10-15,18H2,1-2H3,(H,36,37)/p-1
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n/an/an/an/a 4.20n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450717
PNG
(US10676465, Example 93 | US10676465, Example 94 | ...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(cn2)C#N)nc2ccc(cc12)C([O-])=O
Show InChI InChI=1S/C31H31N5O5/c1-31(27-9-6-20(17-32)18-33-27)40-26-5-3-4-23(29(26)41-31)21-10-12-35(13-11-21)19-28-34-24-8-7-22(30(37)38)16-25(24)36(28)14-15-39-2/h3-9,16,18,21H,10-15,19H2,1-2H3,(H,37,38)/p-1
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n/an/an/an/a>6.50E+3n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450717
PNG
(US10676465, Example 93 | US10676465, Example 94 | ...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(cn2)C#N)nc2ccc(cc12)C([O-])=O
Show InChI InChI=1S/C31H31N5O5/c1-31(27-9-6-20(17-32)18-33-27)40-26-5-3-4-23(29(26)41-31)21-10-12-35(13-11-21)19-28-34-24-8-7-22(30(37)38)16-25(24)36(28)14-15-39-2/h3-9,16,18,21H,10-15,19H2,1-2H3,(H,37,38)/p-1
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n/an/an/an/a>2.00E+4n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450717
PNG
(US10676465, Example 93 | US10676465, Example 94 | ...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(cn2)C#N)nc2ccc(cc12)C([O-])=O
Show InChI InChI=1S/C31H31N5O5/c1-31(27-9-6-20(17-32)18-33-27)40-26-5-3-4-23(29(26)41-31)21-10-12-35(13-11-21)19-28-34-24-8-7-22(30(37)38)16-25(24)36(28)14-15-39-2/h3-9,16,18,21H,10-15,19H2,1-2H3,(H,37,38)/p-1
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n/an/an/an/a 360n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450720
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-7- fluoro-2-met...)
Show SMILES CC1(Oc2c(O1)c(ccc2F)C1CCN(Cc2nc3ccc(cc3n2C[C@@H]2CCO2)C(O)=O)CC1)c1ccc(Cl)cc1F
Show InChI InChI=1S/C32H30ClF2N3O5/c1-32(23-5-3-20(33)15-25(23)35)42-29-22(4-6-24(34)30(29)43-32)18-8-11-37(12-9-18)17-28-36-26-7-2-19(31(39)40)14-27(26)38(28)16-21-10-13-41-21/h2-7,14-15,18,21H,8-13,16-17H2,1H3,(H,39,40)/t21-,32?/m0/s1
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n/an/an/an/a 1.10n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450722
PNG
(US10676465, Example 98 | US10676465, Example 99 | ...)
Show SMILES CC1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4Cc4ncco4)C([O-])=O)CC3)c2O1)c1ccc(cc1F)C#N
Show InChI InChI=1S/C33H28FN5O5/c1-33(24-7-5-20(17-35)15-25(24)34)43-28-4-2-3-23(31(28)44-33)21-9-12-38(13-10-21)18-29-37-26-8-6-22(32(40)41)16-27(26)39(29)19-30-36-11-14-42-30/h2-8,11,14-16,21H,9-10,12-13,18-19H2,1H3,(H,40,41)/p-1
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n/an/an/an/a 5.40n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450631
PNG
(US10676465, Example 8***)
Show SMILES C[C@]1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4C[C@@H]4CCO4)C(O)=O)CC3)c2O1)c1ccc(cc1F)C#N
Show InChI InChI=1S/C33H31FN4O5/c1-33(25-7-5-20(17-35)15-26(25)34)42-29-4-2-3-24(31(29)43-33)21-9-12-37(13-10-21)19-30-36-27-8-6-22(32(39)40)16-28(27)38(30)18-23-11-14-41-23/h2-8,15-16,21,23H,9-14,18-19H2,1H3,(H,39,40)/t23-,33+/m0/s1
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n/an/an/an/a 3.60n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450635
PNG
(2-({4-[2-(4-Chloro-2-fluorophenyl)-2-methyl-1,3-be...)
Show SMILES CN(C)CCn1c(CN2CCC(CC2)c2cccc3O[C@@](C)(Oc23)c2ccc(Cl)cc2F)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C32H34ClFN4O4/c1-32(24-9-8-22(33)18-25(24)34)41-28-6-4-5-23(30(28)42-32)20-11-13-37(14-12-20)19-29-35-26-10-7-21(31(39)40)17-27(26)38(29)16-15-36(2)3/h4-10,17-18,20H,11-16,19H2,1-3H3,(H,39,40)/t32-/m0/s1
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n/an/an/an/a 690n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450636
PNG
(2-({4-[2-(4-Chloro-2-fluorophenyl)-2-methyl-1,3-be...)
Show SMILES C[C@@]1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4Cc4ncco4)C(O)=O)CC3)c2O1)c1ccc(Cl)cc1F
Show InChI InChI=1S/C32H28ClFN4O5/c1-32(23-7-6-21(33)16-24(23)34)42-27-4-2-3-22(30(27)43-32)19-9-12-37(13-10-19)17-28-36-25-8-5-20(31(39)40)15-26(25)38(28)18-29-35-11-14-41-29/h2-8,11,14-16,19H,9-10,12-13,17-18H2,1H3,(H,39,40)/t32-/m0/s1
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n/an/an/an/a 4.5n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450636
PNG
(2-({4-[2-(4-Chloro-2-fluorophenyl)-2-methyl-1,3-be...)
Show SMILES C[C@@]1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4Cc4ncco4)C(O)=O)CC3)c2O1)c1ccc(Cl)cc1F
Show InChI InChI=1S/C32H28ClFN4O5/c1-32(23-7-6-21(33)16-24(23)34)42-27-4-2-3-22(30(27)43-32)19-9-12-37(13-10-19)17-28-36-25-8-5-20(31(39)40)15-26(25)38(28)18-29-35-11-14-41-29/h2-8,11,14-16,19H,9-10,12-13,17-18H2,1H3,(H,39,40)/t32-/m0/s1
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n/an/an/an/a 38n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450638
PNG
(2-{6-[2-(4-Chloro-2-fluorophenyl)-2-methyl-1,3-ben...)
Show SMILES COCCn1c(nc2ccc(cc12)C(=O)OC)[C@@H]1CC11CCN(CC1)c1cccc2OC(C)(Oc12)c1ccc(Cl)cc1F
Show InChI InChI=1S/C33H33ClFN3O5/c1-32(22-9-8-21(34)18-24(22)35)42-28-6-4-5-26(29(28)43-32)37-13-11-33(12-14-37)19-23(33)30-36-25-10-7-20(31(39)41-3)17-27(25)38(30)15-16-40-2/h4-10,17-18,23H,11-16,19H2,1-3H3/t23-,32?/m0/s1
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n/an/an/an/a>2.00E+4n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450639
PNG
(2-{6-[2-(4-Chloro-2-fluorophenyl)-2-methyl-1,3-ben...)
Show SMILES COCCn1c(nc2ccc(cc12)C(=O)OC)[C@H]1CC11CCN(CC1)c1cccc2OC(C)(Oc12)c1ccc(Cl)cc1F
Show InChI InChI=1S/C33H33ClFN3O5/c1-32(22-9-8-21(34)18-24(22)35)42-28-6-4-5-26(29(28)43-32)37-13-11-33(12-14-37)19-23(33)30-36-25-10-7-20(31(39)41-3)17-27(25)38(30)15-16-40-2/h4-10,17-18,23H,11-16,19H2,1-3H3/t23-,32?/m1/s1
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n/an/an/an/a 7.70n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450642
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES COCCn1c(CN2CCN(CC2)c2cccc3OC(C)(Oc23)c2ccc(Cl)cc2F)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C30H30ClFN4O5/c1-30(21-8-7-20(31)17-22(21)32)40-26-5-3-4-24(28(26)41-30)35-12-10-34(11-13-35)18-27-33-23-9-6-19(29(37)38)16-25(23)36(27)14-15-39-2/h3-9,16-17H,10-15,18H2,1-2H3,(H,37,38)
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n/an/an/an/a 25n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450652
PNG
(2-({4-[2-(4-ethylphenyl)-2-methyl-1,3- benzodioxol...)
Show SMILES CCc1ccc(cc1)C1(C)Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4CCOC)C(O)=O)CC3)c2O1
Show InChI InChI=1S/C33H37N3O5/c1-4-22-8-11-25(12-9-22)33(2)40-29-7-5-6-26(31(29)41-33)23-14-16-35(17-15-23)21-30-34-27-13-10-24(32(37)38)20-28(27)36(30)18-19-39-3/h5-13,20,23H,4,14-19,21H2,1-3H3,(H,37,38)
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n/an/an/an/a 5.30n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450656
PNG
(2-({4-[2-(4-chlorophenyl)-2-methyl-1,3- benzodioxo...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(Cl)cc2)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C31H32ClN3O5/c1-31(22-7-9-23(32)10-8-22)39-27-5-3-4-24(29(27)40-31)20-12-14-34(15-13-20)19-28-33-25-11-6-21(30(36)37)18-26(25)35(28)16-17-38-2/h3-11,18,20H,12-17,19H2,1-2H3,(H,36,37)
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n/an/an/an/a 2.60n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450671
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES CC1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4CCN4CCCC4=O)C(O)=O)CC3)c2O1)c1ccc(Cl)cc1F
Show InChI InChI=1S/C34H34ClFN4O5/c1-34(25-9-8-23(35)19-26(25)36)44-29-5-2-4-24(32(29)45-34)21-11-14-38(15-12-21)20-30-37-27-10-7-22(33(42)43)18-28(27)40(30)17-16-39-13-3-6-31(39)41/h2,4-5,7-10,18-19,21H,3,6,11-17,20H2,1H3,(H,42,43)
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n/an/an/an/a 280n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450672
PNG
(1-[2-(acetylamino)ethyl]-2-({4-[2-(4- chloro-2-flu...)
Show SMILES CC(=O)NCCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(Cl)cc2F)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C32H32ClFN4O5/c1-19(39)35-12-15-38-27-16-21(31(40)41)6-9-26(27)36-29(38)18-37-13-10-20(11-14-37)23-4-3-5-28-30(23)43-32(2,42-28)24-8-7-22(33)17-25(24)34/h3-9,16-17,20H,10-15,18H2,1-2H3,(H,35,39)(H,40,41)
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n/an/an/an/a 230n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450676
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES CC1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4CCn4cccn4)C(O)=O)CC3)c2O1)c1ccc(Cl)cc1F
Show InChI InChI=1S/C33H31ClFN5O4/c1-33(25-8-7-23(34)19-26(25)35)43-29-5-2-4-24(31(29)44-33)21-10-14-38(15-11-21)20-30-37-27-9-6-22(32(41)42)18-28(27)40(30)17-16-39-13-3-12-36-39/h2-9,12-13,18-19,21H,10-11,14-17,20H2,1H3,(H,41,42)
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n/an/an/an/a 52n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450678
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES Cn1cnc(CCn2c(CN3CCC(CC3)c3cccc4OC(C)(Oc34)c3ccc(Cl)cc3F)nc3ccc(cc23)C(O)=O)c1
Show InChI InChI=1S/C34H33ClFN5O4/c1-34(26-8-7-23(35)17-27(26)36)44-30-5-3-4-25(32(30)45-34)21-10-13-40(14-11-21)19-31-38-28-9-6-22(33(42)43)16-29(28)41(31)15-12-24-18-39(2)20-37-24/h3-9,16-18,20-21H,10-15,19H2,1-2H3,(H,42,43)
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n/an/an/an/a 74n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450683
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES Cn1cc(CCn2c(CN3CCC(CC3)c3cccc4OC(C)(Oc34)c3ccc(Cl)cc3F)nc3ccc(cc23)C(O)=O)nn1
Show InChI InChI=1S/C33H32ClFN6O4/c1-33(25-8-7-22(34)17-26(25)35)44-29-5-3-4-24(31(29)45-33)20-10-13-40(14-11-20)19-30-36-27-9-6-21(32(42)43)16-28(27)41(30)15-12-23-18-39(2)38-37-23/h3-9,16-18,20H,10-15,19H2,1-2H3,(H,42,43)
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n/an/an/an/a 15n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450688
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES CC1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4Cc4cccnc4)C(O)=O)CC3)c2O1)c1ccc(Cl)cc1F
Show InChI InChI=1S/C34H30ClFN4O4/c1-34(26-9-8-24(35)17-27(26)36)43-30-6-2-5-25(32(30)44-34)22-11-14-39(15-12-22)20-31-38-28-10-7-23(33(41)42)16-29(28)40(31)19-21-4-3-13-37-18-21/h2-10,13,16-18,22H,11-12,14-15,19-20H2,1H3,(H,41,42)
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n/an/an/an/a 11n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450689
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES CN(C)C(=O)Cn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(Cl)cc2F)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C32H32ClFN4O5/c1-32(23-9-8-21(33)16-24(23)34)42-27-6-4-5-22(30(27)43-32)19-11-13-37(14-12-19)17-28-35-25-10-7-20(31(40)41)15-26(25)38(28)18-29(39)36(2)3/h4-10,15-16,19H,11-14,17-18H2,1-3H3,(H,40,41)
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n/an/an/an/a 850n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450693
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES COCCn1cnnc1Cn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(Cl)cc2F)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C34H34ClFN6O5/c1-34(25-8-7-23(35)17-26(25)36)46-29-5-3-4-24(32(29)47-34)21-10-12-40(13-11-21)18-30-38-27-9-6-22(33(43)44)16-28(27)42(30)19-31-39-37-20-41(31)14-15-45-2/h3-9,16-17,20-21H,10-15,18-19H2,1-2H3,(H,43,44)
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n/an/an/an/a 97n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450707
PNG
(2-({4-[2-(2-chloro-4-methoxyphenyl)-2- methyl-1,3-...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(OC)cc2Cl)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C32H34ClN3O6/c1-32(24-9-8-22(40-3)18-25(24)33)41-28-6-4-5-23(30(28)42-32)20-11-13-35(14-12-20)19-29-34-26-10-7-21(31(37)38)17-27(26)36(29)15-16-39-2/h4-10,17-18,20H,11-16,19H2,1-3H3,(H,37,38)
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n/an/an/an/a 3.40n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450712
PNG
(1-(2-methoxyethyl)-2-({4-[2-methyl-2-(2- methylphe...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccccc2C)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C32H35N3O5/c1-21-7-4-5-9-25(21)32(2)39-28-10-6-8-24(30(28)40-32)22-13-15-34(16-14-22)20-29-33-26-12-11-23(31(36)37)19-27(26)35(29)17-18-38-3/h4-12,19,22H,13-18,20H2,1-3H3,(H,36,37)
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n/an/an/an/a 360n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450713
PNG
(1-(2-methoxyethyl)-2-({4-[2-methyl-2- (pyridin-2-y...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccccn2)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C30H32N4O5/c1-30(26-8-3-4-13-31-26)38-25-7-5-6-22(28(25)39-30)20-11-14-33(15-12-20)19-27-32-23-10-9-21(29(35)36)18-24(23)34(27)16-17-37-2/h3-10,13,18,20H,11-12,14-17,19H2,1-2H3,(H,35,36)
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n/an/an/an/a>2.00E+4n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450715
PNG
(US10676465, Example 91 | US10676465, Example 92 | ...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(Cl)cn2)nc2ccc(cc12)C([O-])=O
Show InChI InChI=1S/C30H31ClN4O5/c1-30(26-9-7-21(31)17-32-26)39-25-5-3-4-22(28(25)40-30)19-10-12-34(13-11-19)18-27-33-23-8-6-20(29(36)37)16-24(23)35(27)14-15-38-2/h3-9,16-17,19H,10-15,18H2,1-2H3,(H,36,37)/p-1
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n/an/an/an/a 72n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450722
PNG
(US10676465, Example 98 | US10676465, Example 99 | ...)
Show SMILES CC1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4Cc4ncco4)C([O-])=O)CC3)c2O1)c1ccc(cc1F)C#N
Show InChI InChI=1S/C33H28FN5O5/c1-33(24-7-5-20(17-35)15-25(24)34)43-28-4-2-3-23(31(28)44-33)21-9-12-38(13-10-21)18-29-37-26-8-6-22(32(40)41)16-27(26)39(29)19-30-36-11-14-42-30/h2-8,11,14-16,21H,9-10,12-13,18-19H2,1H3,(H,40,41)/p-1
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n/an/an/an/a 2.80n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450624
PNG
(2-({4-[2-(4-Chloro-2-fluorophenyl)-1,3-benzodioxol...)
Show SMILES COCCn1c(CN2CCN(CC2)c2cccc3O[C@H](Oc23)c2ccc(Cl)cc2F)nc2ccc(cc12)C(=O)OC
Show InChI InChI=1S/C30H30ClFN4O5/c1-38-15-14-36-25-16-19(29(37)39-2)6-9-23(25)33-27(36)18-34-10-12-35(13-11-34)24-4-3-5-26-28(24)41-30(40-26)21-8-7-20(31)17-22(21)32/h3-9,16-17,30H,10-15,18H2,1-2H3/t30-/m1/s1
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n/an/an/an/a>2.00E+4n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450630
PNG
(US10676465, Example 7**)
Show SMILES C[C@]1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4C[C@@H]4CCO4)C([O-])=O)CC3)c2O1)c1ccc(Cl)cc1F
Show InChI InChI=1S/C32H31ClFN3O5/c1-32(24-7-6-21(33)16-25(24)34)41-28-4-2-3-23(30(28)42-32)19-9-12-36(13-10-19)18-29-35-26-8-5-20(31(38)39)15-27(26)37(29)17-22-11-14-40-22/h2-8,15-16,19,22H,9-14,17-18H2,1H3,(H,38,39)/p-1/t22-,32+/m0/s1
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n/an/an/an/a 0.260n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450635
PNG
(2-({4-[2-(4-Chloro-2-fluorophenyl)-2-methyl-1,3-be...)
Show SMILES CN(C)CCn1c(CN2CCC(CC2)c2cccc3O[C@@](C)(Oc23)c2ccc(Cl)cc2F)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C32H34ClFN4O4/c1-32(24-9-8-22(33)18-25(24)34)41-28-6-4-5-23(30(28)42-32)20-11-13-37(14-12-20)19-29-35-26-10-7-21(31(39)40)17-27(26)38(29)16-15-36(2)3/h4-10,17-18,20H,11-16,19H2,1-3H3,(H,39,40)/t32-/m0/s1
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n/an/an/an/a 29n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450637
PNG
(2-({4-[(2S)-2-(4-Chloro-2-fluorophenyl)-2-methyl-1...)
Show SMILES Cn1c(CN2CCC(CC2)c2cccc3O[C@@](C)(Oc23)c2ccc(Cl)cc2F)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C29H27ClFN3O4/c1-29(21-8-7-19(30)15-22(21)31)37-25-5-3-4-20(27(25)38-29)17-10-12-34(13-11-17)16-26-32-23-9-6-18(28(35)36)14-24(23)33(26)2/h3-9,14-15,17H,10-13,16H2,1-2H3,(H,35,36)/t29-/m0/s1
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n/an/an/an/a 79n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450641
PNG
(Ammonium 2-({4-[2-(4-chloro-2-fluorophenyl)-2-meth...)
Show SMILES CCn1cncc1Cn1c(CN2CCC(CC2)c2cccc3O[C@](C)(Oc23)c2ccc(Cl)cc2F)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C34H33ClFN5O4/c1-3-40-20-37-17-24(40)18-41-29-15-22(33(42)43)7-10-28(29)38-31(41)19-39-13-11-21(12-14-39)25-5-4-6-30-32(25)45-34(2,44-30)26-9-8-23(35)16-27(26)36/h4-10,15-17,20-21H,3,11-14,18-19H2,1-2H3,(H,42,43)/t34-/m1/s1
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n/an/an/an/a 210n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450643
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-1,3- benzodioxo...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(Oc23)c2ccc(Cl)cc2F)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C30H29ClFN3O5/c1-38-14-13-35-25-15-19(29(36)37)5-8-24(25)33-27(35)17-34-11-9-18(10-12-34)21-3-2-4-26-28(21)40-30(39-26)22-7-6-20(31)16-23(22)32/h2-8,15-16,18,30H,9-14,17H2,1H3,(H,36,37)
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n/an/an/an/a>2.00E+4n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450645
PNG
(1-(2-methoxyethyl)-2-{[4-(2-phenyl-1,3- benzodioxo...)
Show SMILES COCCn1c(CN2CCN(CC2)c2cccc3OC(Oc23)c2ccccc2)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C29H30N4O5/c1-36-17-16-33-24-18-21(28(34)35)10-11-22(24)30-26(33)19-31-12-14-32(15-13-31)23-8-5-9-25-27(23)38-29(37-25)20-6-3-2-4-7-20/h2-11,18,29H,12-17,19H2,1H3,(H,34,35)
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n/an/an/an/a 680n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450647
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(Cl)cc2F)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C31H31ClFN3O5/c1-31(23-8-7-21(32)17-24(23)33)40-27-5-3-4-22(29(27)41-31)19-10-12-35(13-11-19)18-28-34-25-9-6-20(30(37)38)16-26(25)36(28)14-15-39-2/h3-9,16-17,19H,10-15,18H2,1-2H3,(H,37,38)
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n/an/an/an/a 49n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450648
PNG
(2-{6-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-be...)
Show SMILES COCCn1c(nc2ccc(cc12)C(O)=O)C1CC11CCN(CC1)c1cccc2OC(C)(Oc12)c1ccc(Cl)cc1F
Show InChI InChI=1S/C32H31ClFN3O5/c1-31(21-8-7-20(33)17-23(21)34)41-27-5-3-4-25(28(27)42-31)36-12-10-32(11-13-36)18-22(32)29-35-24-9-6-19(30(38)39)16-26(24)37(29)14-15-40-2/h3-9,16-17,22H,10-15,18H2,1-2H3,(H,38,39)
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n/an/an/an/a>2.00E+4n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450657
PNG
(2-({4-[2-(4-cyanophenyl)-2-methyl-1,3- benzodioxol...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(cc2)C#N)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C32H32N4O5/c1-32(24-9-6-21(19-33)7-10-24)40-28-5-3-4-25(30(28)41-32)22-12-14-35(15-13-22)20-29-34-26-11-8-23(31(37)38)18-27(26)36(29)16-17-39-2/h3-11,18,22H,12-17,20H2,1-2H3,(H,37,38)
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n/an/an/an/a 7.80n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450657
PNG
(2-({4-[2-(4-cyanophenyl)-2-methyl-1,3- benzodioxol...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(cc2)C#N)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C32H32N4O5/c1-32(24-9-6-21(19-33)7-10-24)40-28-5-3-4-25(30(28)41-32)22-12-14-35(15-13-22)20-29-34-26-11-8-23(31(37)38)18-27(26)36(29)16-17-39-2/h3-11,18,22H,12-17,20H2,1-2H3,(H,37,38)
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n/an/an/an/a 110n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450658
PNG
(2-({4-[2-(2-fluoro-4-methoxyphenyl)-2- methyl-1,3-...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(OC)cc2F)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C32H34FN3O6/c1-32(24-9-8-22(40-3)18-25(24)33)41-28-6-4-5-23(30(28)42-32)20-11-13-35(14-12-20)19-29-34-26-10-7-21(31(37)38)17-27(26)36(29)15-16-39-2/h4-10,17-18,20H,11-16,19H2,1-3H3,(H,37,38)
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n/an/an/an/a 6.60n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450658
PNG
(2-({4-[2-(2-fluoro-4-methoxyphenyl)-2- methyl-1,3-...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(OC)cc2F)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C32H34FN3O6/c1-32(24-9-8-22(40-3)18-25(24)33)41-28-6-4-5-23(30(28)42-32)20-11-13-35(14-12-20)19-29-34-26-10-7-21(31(37)38)17-27(26)36(29)15-16-39-2/h4-10,17-18,20H,11-16,19H2,1-3H3,(H,37,38)
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n/an/an/an/a 170n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450665
PNG
(1-(2-methoxyethyl)-2-({4-[2-methyl-2-(6- methylpyr...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(C)nc2)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C31H34N4O5/c1-20-7-9-23(18-32-20)31(2)39-27-6-4-5-24(29(27)40-31)21-11-13-34(14-12-21)19-28-33-25-10-8-22(30(36)37)17-26(25)35(28)15-16-38-3/h4-10,17-18,21H,11-16,19H2,1-3H3,(H,36,37)
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n/an/an/an/a 120n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450665
PNG
(1-(2-methoxyethyl)-2-({4-[2-methyl-2-(6- methylpyr...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(C)nc2)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C31H34N4O5/c1-20-7-9-23(18-32-20)31(2)39-27-6-4-5-24(29(27)40-31)21-11-13-34(14-12-21)19-28-33-25-10-8-22(30(36)37)17-26(25)35(28)15-16-38-3/h4-10,17-18,21H,11-16,19H2,1-3H3,(H,36,37)
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n/an/an/an/a 1.70E+3n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450671
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES CC1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4CCN4CCCC4=O)C(O)=O)CC3)c2O1)c1ccc(Cl)cc1F
Show InChI InChI=1S/C34H34ClFN4O5/c1-34(25-9-8-23(35)19-26(25)36)44-29-5-2-4-24(32(29)45-34)21-11-14-38(15-12-21)20-30-37-27-10-7-22(33(42)43)18-28(27)40(30)17-16-39-13-3-6-31(39)41/h2,4-5,7-10,18-19,21H,3,6,11-17,20H2,1H3,(H,42,43)
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n/an/an/an/a 14n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450676
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES CC1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4CCn4cccn4)C(O)=O)CC3)c2O1)c1ccc(Cl)cc1F
Show InChI InChI=1S/C33H31ClFN5O4/c1-33(25-8-7-23(34)19-26(25)35)43-29-5-2-4-24(31(29)44-33)21-10-14-38(15-11-21)20-30-37-27-9-6-22(32(41)42)18-28(27)40(30)17-16-39-13-3-12-36-39/h2-9,12-13,18-19,21H,10-11,14-17,20H2,1H3,(H,41,42)
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n/an/an/an/a 3.10n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450689
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES CN(C)C(=O)Cn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(Cl)cc2F)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C32H32ClFN4O5/c1-32(23-9-8-21(33)16-24(23)34)42-27-6-4-5-22(30(27)43-32)19-11-13-37(14-12-19)17-28-35-25-10-7-20(31(40)41)15-26(25)38(28)18-29(39)36(2)3/h4-10,15-16,19H,11-14,17-18H2,1-3H3,(H,40,41)
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n/an/an/an/a 51n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450701
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES Cn1cnc(Cn2c(CN3CCC(CC3)c3cccc4OC(C)(Oc34)c3ccc(Cl)cc3F)nc3ccc(cc23)C(O)=O)c1
Show InChI InChI=1S/C33H31ClFN5O4/c1-33(25-8-7-22(34)15-26(25)35)43-29-5-3-4-24(31(29)44-33)20-10-12-39(13-11-20)18-30-37-27-9-6-21(32(41)42)14-28(27)40(30)17-23-16-38(2)19-36-23/h3-9,14-16,19-20H,10-13,17-18H2,1-2H3,(H,41,42)
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n/an/an/an/a 1.70E+3n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450703
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES CC1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4C[C@@H]4CCCO4)C(O)=O)CC3)c2O1)c1ccc(Cl)cc1F
Show InChI InChI=1S/C33H33ClFN3O5/c1-33(25-9-8-22(34)17-26(25)35)42-29-6-2-5-24(31(29)43-33)20-11-13-37(14-12-20)19-30-36-27-10-7-21(32(39)40)16-28(27)38(30)18-23-4-3-15-41-23/h2,5-10,16-17,20,23H,3-4,11-15,18-19H2,1H3,(H,39,40)/t23-,33?/m0/s1
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n/an/an/an/a 21n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450708
PNG
(1-(2-methoxyethyl)-2-({4-[2-methyl-2-(4- methylphe...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(C)cc2)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C32H35N3O5/c1-21-7-10-24(11-8-21)32(2)39-28-6-4-5-25(30(28)40-32)22-13-15-34(16-14-22)20-29-33-26-12-9-23(31(36)37)19-27(26)35(29)17-18-38-3/h4-12,19,22H,13-18,20H2,1-3H3,(H,36,37)
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n/an/an/an/a 100n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450722
PNG
(US10676465, Example 98 | US10676465, Example 99 | ...)
Show SMILES CC1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4Cc4ncco4)C([O-])=O)CC3)c2O1)c1ccc(cc1F)C#N
Show InChI InChI=1S/C33H28FN5O5/c1-33(24-7-5-20(17-35)15-25(24)34)43-28-4-2-3-23(31(28)44-33)21-9-12-38(13-10-21)18-29-37-26-8-6-22(32(40)41)16-27(26)39(29)19-30-36-11-14-42-30/h2-8,11,14-16,21H,9-10,12-13,18-19H2,1H3,(H,40,41)/p-1
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n/an/an/an/a 50n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450625
PNG
(US10676465, Example 2*)
Show SMILES COCCn1c(CN2CCN(CC2)c2cccc3O[C@@H](Oc23)c2ccc(Cl)cc2F)nc2ccc(cc12)C(=O)OC
Show InChI InChI=1S/C30H30ClFN4O5/c1-38-15-14-36-25-16-19(29(37)39-2)6-9-23(25)33-27(36)18-34-10-12-35(13-11-34)24-4-3-5-26-28(24)41-30(40-26)21-8-7-20(31)17-22(21)32/h3-9,16-17,30H,10-15,18H2,1-2H3/t30-/m0/s1
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n/an/an/an/a 6.60n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450631
PNG
(US10676465, Example 8***)
Show SMILES C[C@]1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4C[C@@H]4CCO4)C(O)=O)CC3)c2O1)c1ccc(cc1F)C#N
Show InChI InChI=1S/C33H31FN4O5/c1-33(25-7-5-20(17-35)15-26(25)34)42-29-4-2-3-24(31(29)43-33)21-9-12-37(13-10-21)19-30-36-27-8-6-22(32(39)40)16-28(27)38(30)18-23-11-14-41-23/h2-8,15-16,21,23H,9-14,18-19H2,1H3,(H,39,40)/t23-,33+/m0/s1
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n/an/an/an/a 0.300n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450633
PNG
(US10676465, Example 10)
Show SMILES C[C@@]1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4C[C@@H]4CCO4)C(O)=O)CC3)c2O1)c1ccc(Cl)cn1
Show InChI InChI=1S/C31H31ClN4O5/c1-31(27-8-6-21(32)16-33-27)40-26-4-2-3-23(29(26)41-31)19-9-12-35(13-10-19)18-28-34-24-7-5-20(30(37)38)15-25(24)36(28)17-22-11-14-39-22/h2-8,15-16,19,22H,9-14,17-18H2,1H3,(H,37,38)/t22-,31-/m0/s1
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n/an/an/an/a 17n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450640
PNG
(Ammonium 2-({4-[2-(4-chloro-2-fluorophenyl)-2-meth...)
Show SMILES CCn1cncc1Cn1c(CN2CCC(CC2)c2cccc3O[C@@](C)(Oc23)c2ccc(Cl)cc2F)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C34H33ClFN5O4/c1-3-40-20-37-17-24(40)18-41-29-15-22(33(42)43)7-10-28(29)38-31(41)19-39-13-11-21(12-14-39)25-5-4-6-30-32(25)45-34(2,44-30)26-9-8-23(35)16-27(26)36/h4-10,15-17,20-21H,3,11-14,18-19H2,1-2H3,(H,42,43)/t34-/m0/s1
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n/an/an/an/a 1.10n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450647
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(Cl)cc2F)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C31H31ClFN3O5/c1-31(23-8-7-21(32)17-24(23)33)40-27-5-3-4-22(29(27)41-31)19-10-12-35(13-11-19)18-28-34-25-9-6-20(30(37)38)16-26(25)36(28)14-15-39-2/h3-9,16-17,19H,10-15,18H2,1-2H3,(H,37,38)
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n/an/an/an/a 1.40n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450650
PNG
(2-({4-[2-(4-cyano-2-fluorophenyl)-1,3- benzodioxol...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(Oc23)c2ccc(cc2F)C#N)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C31H29FN4O5/c1-39-14-13-36-26-16-21(30(37)38)6-8-25(26)34-28(36)18-35-11-9-20(10-12-35)22-3-2-4-27-29(22)41-31(40-27)23-7-5-19(17-33)15-24(23)32/h2-8,15-16,20,31H,9-14,18H2,1H3,(H,37,38)
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n/an/an/an/a 1.00E+3n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450651
PNG
(1-(2-methoxyethyl)-2-[(4-{2-methyl-2-[3- (trifluor...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2cccc(c2)C(F)(F)F)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C32H32F3N3O5/c1-31(22-5-3-6-23(18-22)32(33,34)35)42-27-8-4-7-24(29(27)43-31)20-11-13-37(14-12-20)19-28-36-25-10-9-21(30(39)40)17-26(25)38(28)15-16-41-2/h3-10,17-18,20H,11-16,19H2,1-2H3,(H,39,40)
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n/an/an/an/a 480n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450653
PNG
(2-({4-[2-(3-fluoro-4-methoxyphenyl)-2- methyl-1,3-...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(OC)c(F)c2)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C32H34FN3O6/c1-32(22-8-10-27(40-3)24(33)18-22)41-28-6-4-5-23(30(28)42-32)20-11-13-35(14-12-20)19-29-34-25-9-7-21(31(37)38)17-26(25)36(29)15-16-39-2/h4-10,17-18,20H,11-16,19H2,1-3H3,(H,37,38)
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n/an/an/an/a 1.10E+3n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450662
PNG
(1-(2-methoxyethyl)-2-({4-[2-(3- methoxyphenyl)-2-m...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2cccc(OC)c2)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C32H35N3O6/c1-32(23-6-4-7-24(19-23)39-3)40-28-9-5-8-25(30(28)41-32)21-12-14-34(15-13-21)20-29-33-26-11-10-22(31(36)37)18-27(26)35(29)16-17-38-2/h4-11,18-19,21H,12-17,20H2,1-3H3,(H,36,37)
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n/an/an/an/a 200n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450663
PNG
(1-(2-methoxyethyl)-2-[(4-{2-methyl-2-[4- (trifluor...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(cc2)C(F)(F)F)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C32H32F3N3O5/c1-31(22-7-9-23(10-8-22)32(33,34)35)42-27-5-3-4-24(29(27)43-31)20-12-14-37(15-13-20)19-28-36-25-11-6-21(30(39)40)18-26(25)38(28)16-17-41-2/h3-11,18,20H,12-17,19H2,1-2H3,(H,39,40)
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n/an/an/an/a 130n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450664
PNG
(2-({4-[2-(3,4-difluorophenyl)-2-methyl- 1,3-benzod...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(F)c(C)c2)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C32H34FN3O5/c1-20-17-23(8-9-25(20)33)32(2)40-28-6-4-5-24(30(28)41-32)21-11-13-35(14-12-21)19-29-34-26-10-7-22(31(37)38)18-27(26)36(29)15-16-39-3/h4-10,17-18,21H,11-16,19H2,1-3H3,(H,37,38)
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n/an/an/an/a 91n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450668
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES CC1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4Cc4ccccn4)C(O)=O)CC3)c2O1)c1ccc(Cl)cc1F
Show InChI InChI=1S/C34H30ClFN4O4/c1-34(26-10-9-23(35)18-27(26)36)43-30-7-4-6-25(32(30)44-34)21-12-15-39(16-13-21)20-31-38-28-11-8-22(33(41)42)17-29(28)40(31)19-24-5-2-3-14-37-24/h2-11,14,17-18,21H,12-13,15-16,19-20H2,1H3,(H,41,42)
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n/an/an/an/a 9.90n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450669
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES CC1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4CCN4CCOC4=O)C(O)=O)CC3)c2O1)c1ccc(Cl)cc1F
Show InChI InChI=1S/C33H32ClFN4O6/c1-33(24-7-6-22(34)18-25(24)35)44-28-4-2-3-23(30(28)45-33)20-9-11-37(12-10-20)19-29-36-26-8-5-21(31(40)41)17-27(26)39(29)14-13-38-15-16-43-32(38)42/h2-8,17-18,20H,9-16,19H2,1H3,(H,40,41)
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n/an/an/an/a 57n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450670
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES CN(C)S(=O)(=O)CCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(Cl)cc2F)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C32H34ClFN4O6S/c1-32(24-9-8-22(33)18-25(24)34)43-28-6-4-5-23(30(28)44-32)20-11-13-37(14-12-20)19-29-35-26-10-7-21(31(39)40)17-27(26)38(29)15-16-45(41,42)36(2)3/h4-10,17-18,20H,11-16,19H2,1-3H3,(H,39,40)
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n/an/an/an/a 42n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450675
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES CNC(=O)Cn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(Cl)cc2F)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C31H30ClFN4O5/c1-31(22-8-7-20(32)15-23(22)33)41-26-5-3-4-21(29(26)42-31)18-10-12-36(13-11-18)16-27-35-24-9-6-19(30(39)40)14-25(24)37(27)17-28(38)34-2/h3-9,14-15,18H,10-13,16-17H2,1-2H3,(H,34,38)(H,39,40)
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n/an/an/an/a 32n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450683
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES Cn1cc(CCn2c(CN3CCC(CC3)c3cccc4OC(C)(Oc34)c3ccc(Cl)cc3F)nc3ccc(cc23)C(O)=O)nn1
Show InChI InChI=1S/C33H32ClFN6O4/c1-33(25-8-7-22(34)17-26(25)35)44-29-5-3-4-24(31(29)45-33)20-10-13-40(14-11-20)19-30-36-27-9-6-21(32(42)43)16-28(27)41(30)15-12-23-18-39(2)38-37-23/h3-9,16-18,20H,10-15,19H2,1-2H3,(H,42,43)
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n/an/an/an/a 240n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450686
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES Cn1cc(Cn2c(CN3CCC(CC3)c3cccc4OC(C)(Oc34)c3ccc(Cl)cc3F)nc3ccc(cc23)C(O)=O)nn1
Show InChI InChI=1S/C32H30ClFN6O4/c1-32(24-8-7-21(33)15-25(24)34)43-28-5-3-4-23(30(28)44-32)19-10-12-39(13-11-19)18-29-35-26-9-6-20(31(41)42)14-27(26)40(29)17-22-16-38(2)37-36-22/h3-9,14-16,19H,10-13,17-18H2,1-2H3,(H,41,42)
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n/an/an/an/a 5.20n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450688
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES CC1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4Cc4cccnc4)C(O)=O)CC3)c2O1)c1ccc(Cl)cc1F
Show InChI InChI=1S/C34H30ClFN4O4/c1-34(26-9-8-24(35)17-27(26)36)43-30-6-2-5-25(32(30)44-34)22-11-14-39(15-12-22)20-31-38-28-10-7-23(33(41)42)16-29(28)40(31)19-21-4-3-13-37-18-21/h2-10,13,16-18,22H,11-12,14-15,19-20H2,1H3,(H,41,42)
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n/an/an/an/a 1.20n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450698
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES CC1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4CCO)C(O)=O)CC3)c2O1)c1ccc(Cl)cc1F
Show InChI InChI=1S/C30H29ClFN3O5/c1-30(22-7-6-20(31)16-23(22)32)39-26-4-2-3-21(28(26)40-30)18-9-11-34(12-10-18)17-27-33-24-8-5-19(29(37)38)15-25(24)35(27)13-14-36/h2-8,15-16,18,36H,9-14,17H2,1H3,(H,37,38)
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n/an/an/an/a 65n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450700
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES CCn1nncc1Cn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(Cl)cc2F)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C33H32ClFN6O4/c1-3-41-23(17-36-38-41)18-40-28-15-21(32(42)43)7-10-27(28)37-30(40)19-39-13-11-20(12-14-39)24-5-4-6-29-31(24)45-33(2,44-29)25-9-8-22(34)16-26(25)35/h4-10,15-17,20H,3,11-14,18-19H2,1-2H3,(H,42,43)
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n/an/an/an/a 0.770n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450702
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES Cn1cnnc1Cn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(Cl)cc2F)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C32H30ClFN6O4/c1-32(23-8-7-21(33)15-24(23)34)43-27-5-3-4-22(30(27)44-32)19-10-12-39(13-11-19)16-28-36-25-9-6-20(31(41)42)14-26(25)40(28)17-29-37-35-18-38(29)2/h3-9,14-15,18-19H,10-13,16-17H2,1-2H3,(H,41,42)
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n/an/an/an/a 78n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450704
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES CC1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4Cc4ncco4)C(O)=O)CC3)c2O1)c1ccc(Cl)cc1F
Show InChI InChI=1S/C32H28ClFN4O5/c1-32(23-7-6-21(33)16-24(23)34)42-27-4-2-3-22(30(27)43-32)19-9-12-37(13-10-19)17-28-36-25-8-5-20(31(39)40)15-26(25)38(28)18-29-35-11-14-41-29/h2-8,11,14-16,19H,9-10,12-13,17-18H2,1H3,(H,39,40)
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n/an/an/an/a 1.10n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450713
PNG
(1-(2-methoxyethyl)-2-({4-[2-methyl-2- (pyridin-2-y...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccccn2)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C30H32N4O5/c1-30(26-8-3-4-13-31-26)38-25-7-5-6-22(28(25)39-30)20-11-14-33(15-12-20)19-27-32-23-10-9-21(29(35)36)18-24(23)34(27)16-17-37-2/h3-10,13,18,20H,11-12,14-17,19H2,1-2H3,(H,35,36)
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n/an/an/an/a 130n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450713
PNG
(1-(2-methoxyethyl)-2-({4-[2-methyl-2- (pyridin-2-y...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccccn2)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C30H32N4O5/c1-30(26-8-3-4-13-31-26)38-25-7-5-6-22(28(25)39-30)20-11-14-33(15-12-20)19-27-32-23-10-9-21(29(35)36)18-24(23)34(27)16-17-37-2/h3-10,13,18,20H,11-12,14-17,19H2,1-2H3,(H,35,36)
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n/an/an/an/a 2.90E+3n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450715
PNG
(US10676465, Example 91 | US10676465, Example 92 | ...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(Cl)cn2)nc2ccc(cc12)C([O-])=O
Show InChI InChI=1S/C30H31ClN4O5/c1-30(26-9-7-21(31)17-32-26)39-25-5-3-4-22(28(25)40-30)19-10-12-34(13-11-19)18-27-33-23-8-6-20(29(36)37)16-24(23)35(27)14-15-38-2/h3-9,16-17,19H,10-15,18H2,1-2H3,(H,36,37)/p-1
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n/an/an/an/a 1.40E+4n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450717
PNG
(US10676465, Example 93 | US10676465, Example 94 | ...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(cn2)C#N)nc2ccc(cc12)C([O-])=O
Show InChI InChI=1S/C31H31N5O5/c1-31(27-9-6-20(17-32)18-33-27)40-26-5-3-4-23(29(26)41-31)21-10-12-35(13-11-21)19-28-34-24-8-7-22(30(37)38)16-25(24)36(28)14-15-39-2/h3-9,16,18,21H,10-15,19H2,1-2H3,(H,37,38)/p-1
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n/an/an/an/a 12n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450725
PNG
(2-({4-[(2S)-2-(4-chloro-2-fluorophenyl)- 1,3-benzo...)
Show SMILES OC(=O)c1ccc2nc(CN3CCC(CC3)c3cccc4O[C@@H](Oc34)c3ccc(Cl)cc3F)n(C[C@@H]3CCO3)c2c1F
Show InChI InChI=1S/C31H28ClF2N3O5/c32-18-4-5-21(23(33)14-18)31-41-25-3-1-2-20(29(25)42-31)17-8-11-36(12-9-17)16-26-35-24-7-6-22(30(38)39)27(34)28(24)37(26)15-19-10-13-40-19/h1-7,14,17,19,31H,8-13,15-16H2,(H,38,39)/t19-,31-/m0/s1
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n/an/an/an/a 19n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450624
PNG
(2-({4-[2-(4-Chloro-2-fluorophenyl)-1,3-benzodioxol...)
Show SMILES COCCn1c(CN2CCN(CC2)c2cccc3O[C@H](Oc23)c2ccc(Cl)cc2F)nc2ccc(cc12)C(=O)OC
Show InChI InChI=1S/C30H30ClFN4O5/c1-38-15-14-36-25-16-19(29(37)39-2)6-9-23(25)33-27(36)18-34-10-12-35(13-11-34)24-4-3-5-26-28(24)41-30(40-26)21-8-7-20(31)17-22(21)32/h3-9,16-17,30H,10-15,18H2,1-2H3/t30-/m1/s1
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n/an/an/an/a 880n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450627
PNG
(Ammonium 2-({4-[(2R)-2-(4-chloro-2-fluorophenyl)-1...)
Show SMILES [O-]C(=O)c1ccc2nc(CN3CCC(CC3)c3cccc4O[C@H](Oc34)c3ccc(Cl)cc3F)n(C[C@@H]3CCO3)c2c1
Show InChI InChI=1S/C31H29ClFN3O5/c32-20-5-6-23(24(33)15-20)31-40-27-3-1-2-22(29(27)41-31)18-8-11-35(12-9-18)17-28-34-25-7-4-19(30(37)38)14-26(25)36(28)16-21-10-13-39-21/h1-7,14-15,18,21,31H,8-13,16-17H2,(H,37,38)/p-1/t21-,31+/m0/s1
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n/an/an/an/a 1.60E+3n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450645
PNG
(1-(2-methoxyethyl)-2-{[4-(2-phenyl-1,3- benzodioxo...)
Show SMILES COCCn1c(CN2CCN(CC2)c2cccc3OC(Oc23)c2ccccc2)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C29H30N4O5/c1-36-17-16-33-24-18-21(28(34)35)10-11-22(24)30-26(33)19-31-12-14-32(15-13-31)23-8-5-9-25-27(23)38-29(37-25)20-6-3-2-4-7-20/h2-11,18,29H,12-17,19H2,1H3,(H,34,35)
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n/an/an/an/a>2.00E+4n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450656
PNG
(2-({4-[2-(4-chlorophenyl)-2-methyl-1,3- benzodioxo...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(Cl)cc2)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C31H32ClN3O5/c1-31(22-7-9-23(32)10-8-22)39-27-5-3-4-24(29(27)40-31)20-12-14-34(15-13-20)19-28-33-25-11-6-21(30(36)37)18-26(25)35(28)16-17-38-2/h3-11,18,20H,12-17,19H2,1-2H3,(H,36,37)
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n/an/an/an/a 100n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450659
PNG
(1-(2-methoxyethyl)-2-({4-[2-methyl-2-(6- methylpyr...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2cccc(C)n2)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C31H34N4O5/c1-20-6-4-9-27(32-20)31(2)39-26-8-5-7-23(29(26)40-31)21-12-14-34(15-13-21)19-28-33-24-11-10-22(30(36)37)18-25(24)35(28)16-17-38-3/h4-11,18,21H,12-17,19H2,1-3H3,(H,36,37)
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n/an/an/an/a 760n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450666
PNG
(1-{2-[acetyl(methyl)amino]ethyl}-2-({4-[2- (4-chlo...)
Show SMILES CN(CCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(Cl)cc2F)nc2ccc(cc12)C(O)=O)C(C)=O
Show InChI InChI=1S/C33H34ClFN4O5/c1-20(40)37(3)15-16-39-28-17-22(32(41)42)7-10-27(28)36-30(39)19-38-13-11-21(12-14-38)24-5-4-6-29-31(24)44-33(2,43-29)25-9-8-23(34)18-26(25)35/h4-10,17-18,21H,11-16,19H2,1-3H3,(H,41,42)
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n/an/an/an/a 3.5n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450674
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES CCn1ccnc1Cn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(Cl)cc2F)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C34H33ClFN5O4/c1-3-40-16-13-37-30(40)20-41-28-17-22(33(42)43)7-10-27(28)38-31(41)19-39-14-11-21(12-15-39)24-5-4-6-29-32(24)45-34(2,44-29)25-9-8-23(35)18-26(25)36/h4-10,13,16-18,21H,3,11-12,14-15,19-20H2,1-2H3,(H,42,43)
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n/an/an/an/a 19n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450675
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES CNC(=O)Cn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(Cl)cc2F)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C31H30ClFN4O5/c1-31(22-8-7-20(32)15-23(22)33)41-26-5-3-4-21(29(26)42-31)18-10-12-36(13-11-18)16-27-35-24-9-6-19(30(39)40)14-25(24)37(27)17-28(38)34-2/h3-9,14-15,18H,10-13,16-17H2,1-2H3,(H,34,38)(H,39,40)
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n/an/an/an/a 570n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450680
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES Cn1ncnc1Cn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(Cl)cc2F)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C32H30ClFN6O4/c1-32(23-8-7-21(33)15-24(23)34)43-27-5-3-4-22(30(27)44-32)19-10-12-39(13-11-19)16-29-37-25-9-6-20(31(41)42)14-26(25)40(29)17-28-35-18-36-38(28)2/h3-9,14-15,18-19H,10-13,16-17H2,1-2H3,(H,41,42)
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n/an/an/an/a 15n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450681
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES CC1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4Cc4cocn4)C(O)=O)CC3)c2O1)c1ccc(Cl)cc1F
Show InChI InChI=1S/C32H28ClFN4O5/c1-32(24-7-6-21(33)14-25(24)34)42-28-4-2-3-23(30(28)43-32)19-9-11-37(12-10-19)16-29-36-26-8-5-20(31(39)40)13-27(26)38(29)15-22-17-41-18-35-22/h2-8,13-14,17-19H,9-12,15-16H2,1H3,(H,39,40)
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n/an/an/an/a 4n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450681
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES CC1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4Cc4cocn4)C(O)=O)CC3)c2O1)c1ccc(Cl)cc1F
Show InChI InChI=1S/C32H28ClFN4O5/c1-32(24-7-6-21(33)14-25(24)34)42-28-4-2-3-23(30(28)43-32)19-9-11-37(12-10-19)16-29-36-26-8-5-20(31(39)40)13-27(26)38(29)15-22-17-41-18-35-22/h2-8,13-14,17-19H,9-12,15-16H2,1H3,(H,39,40)
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n/an/an/an/a 23n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450682
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES CN(C)C(=O)CCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(Cl)cc2F)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C33H34ClFN4O5/c1-33(24-9-8-22(34)18-25(24)35)43-28-6-4-5-23(31(28)44-33)20-11-14-38(15-12-20)19-29-36-26-10-7-21(32(41)42)17-27(26)39(29)16-13-30(40)37(2)3/h4-10,17-18,20H,11-16,19H2,1-3H3,(H,41,42)
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n/an/an/an/a 74n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450682
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES CN(C)C(=O)CCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(Cl)cc2F)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C33H34ClFN4O5/c1-33(24-9-8-22(34)18-25(24)35)43-28-6-4-5-23(31(28)44-33)20-11-14-38(15-12-20)19-29-36-26-10-7-21(32(41)42)17-27(26)39(29)16-13-30(40)37(2)3/h4-10,17-18,20H,11-16,19H2,1-3H3,(H,41,42)
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n/an/an/an/a 680n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450684
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES CC1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4C4CCOC4)C(O)=O)CC3)c2O1)c1ccc(Cl)cc1F
Show InChI InChI=1S/C32H31ClFN3O5/c1-32(24-7-6-21(33)16-25(24)34)41-28-4-2-3-23(30(28)42-32)19-9-12-36(13-10-19)17-29-35-26-8-5-20(31(38)39)15-27(26)37(29)22-11-14-40-18-22/h2-8,15-16,19,22H,9-14,17-18H2,1H3,(H,38,39)
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n/an/an/an/a 10n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450690
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES CC1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4CCN4CCCC4)C(O)=O)CC3)c2O1)c1ccc(Cl)cc1F
Show InChI InChI=1S/C34H36ClFN4O4/c1-34(26-9-8-24(35)20-27(26)36)43-30-6-4-5-25(32(30)44-34)22-11-15-39(16-12-22)21-31-37-28-10-7-23(33(41)42)19-29(28)40(31)18-17-38-13-2-3-14-38/h4-10,19-20,22H,2-3,11-18,21H2,1H3,(H,41,42)
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n/an/an/an/a 710n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450691
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-2- methyl-1,3-b...)
Show SMILES COCc1cc(Cn2c(CN3CCC(CC3)c3cccc4OC(C)(Oc34)c3ccc(Cl)cc3F)nc3ccc(cc23)C(O)=O)[nH]n1
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n/an/an/an/a 73n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450706
PNG
(1-(2-methoxyethyl)-2-{[4-(2-methyl-2- phenyl-1,3-b...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccccc2)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C31H33N3O5/c1-31(23-7-4-3-5-8-23)38-27-10-6-9-24(29(27)39-31)21-13-15-33(16-14-21)20-28-32-25-12-11-22(30(35)36)19-26(25)34(28)17-18-37-2/h3-12,19,21H,13-18,20H2,1-2H3,(H,35,36)
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n/an/an/an/a 47n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450710
PNG
(2-({4-[2-(2-chlorophenyl)-2-methyl-1,3- benzodioxo...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccccc2Cl)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C31H32ClN3O5/c1-31(23-7-3-4-8-24(23)32)39-27-9-5-6-22(29(27)40-31)20-12-14-34(15-13-20)19-28-33-25-11-10-21(30(36)37)18-26(25)35(28)16-17-38-2/h3-11,18,20H,12-17,19H2,1-2H3,(H,36,37)
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n/an/an/an/a 24n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450711
PNG
(2-({4-[2-(3-cyanophenyl)-2-methyl-1,3- benzodioxol...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2cccc(c2)C#N)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C32H32N4O5/c1-32(24-6-3-5-21(17-24)19-33)40-28-8-4-7-25(30(28)41-32)22-11-13-35(14-12-22)20-29-34-26-10-9-23(31(37)38)18-27(26)36(29)15-16-39-2/h3-10,17-18,22H,11-16,20H2,1-2H3,(H,37,38)
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n/an/an/an/a 570n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450719
PNG
(US10676465, Example 95****)
Show SMILES CC1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4C[C@@H]4CCO4)C(O)=O)CC3)c2O1)c1ccc(Cl)cn1
Show InChI InChI=1S/C31H31ClN4O5/c1-31(27-8-6-21(32)16-33-27)40-26-4-2-3-23(29(26)41-31)19-9-12-35(13-10-19)18-28-34-24-7-5-20(30(37)38)15-25(24)36(28)17-22-11-14-39-22/h2-8,15-16,19,22H,9-14,17-18H2,1H3,(H,37,38)/t22-,31?/m0/s1
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n/an/an/an/a 220n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450719
PNG
(US10676465, Example 95****)
Show SMILES CC1(Oc2cccc(C3CCN(Cc4nc5ccc(cc5n4C[C@@H]4CCO4)C(O)=O)CC3)c2O1)c1ccc(Cl)cn1
Show InChI InChI=1S/C31H31ClN4O5/c1-31(27-8-6-21(32)16-33-27)40-26-4-2-3-23(29(26)41-31)19-9-12-35(13-10-19)18-28-34-24-7-5-20(30(37)38)15-25(24)36(28)17-22-11-14-39-22/h2-8,15-16,19,22H,9-14,17-18H2,1H3,(H,37,38)/t22-,31?/m0/s1
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n/an/an/an/a>1.30E+4n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450720
PNG
(2-({4-[2-(4-chloro-2-fluorophenyl)-7- fluoro-2-met...)
Show SMILES CC1(Oc2c(O1)c(ccc2F)C1CCN(Cc2nc3ccc(cc3n2C[C@@H]2CCO2)C(O)=O)CC1)c1ccc(Cl)cc1F
Show InChI InChI=1S/C32H30ClF2N3O5/c1-32(23-5-3-20(33)15-25(23)35)42-29-22(4-6-24(34)30(29)43-32)18-8-11-37(12-9-18)17-28-36-26-7-2-19(31(39)40)14-27(26)38(28)16-21-10-13-41-21/h2-7,14-15,18,21H,8-13,16-17H2,1H3,(H,39,40)/t21-,32?/m0/s1
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n/an/an/an/a 140n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450626
PNG
(2-({4-[2-(4-Chloro-2-fluorophenyl)-2-methyl-1,3-be...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc3OC(C)(Oc23)c2ccc(Cl)cc2F)nc2ncc(cc12)C(O)=O
Show InChI InChI=1S/C30H30ClFN4O5/c1-30(22-7-6-20(31)15-23(22)32)40-25-5-3-4-21(27(25)41-30)18-8-10-35(11-9-18)17-26-34-28-24(36(26)12-13-39-2)14-19(16-33-28)29(37)38/h3-7,14-16,18H,8-13,17H2,1-2H3,(H,37,38)
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n/an/an/an/a 45n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM450627
PNG
(Ammonium 2-({4-[(2R)-2-(4-chloro-2-fluorophenyl)-1...)
Show SMILES [O-]C(=O)c1ccc2nc(CN3CCC(CC3)c3cccc4O[C@H](Oc34)c3ccc(Cl)cc3F)n(C[C@@H]3CCO3)c2c1
Show InChI InChI=1S/C31H29ClFN3O5/c32-20-5-6-23(24(33)15-20)31-40-27-3-1-2-22(29(27)41-31)18-8-11-35(12-9-18)17-28-34-25-7-4-19(30(37)38)14-26(25)36(28)16-21-10-13-39-21/h1-7,14-15,18,21,31H,8-13,16-17H2,(H,37,38)/p-1/t21-,31+/m0/s1
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n/an/an/an/a>2.00E+4n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10676465 (2020)

More data for this
Ligand-Target Pair
* indicates data uncertainty>20%