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Compile Data Set for Download or QSAR

Found 1680 hits Enz. Inhib. hit(s) with Target = 'Glucagon receptor' AND taxid = 9606   
Target
(Institution)
LigandTarget
Links
Ligand
Links
Trg + Lig
Links
Ki
nM
ΔG°
kJ/mole
IC50
nM
Kd
nM
EC50/IC50
nM
koff
s-1
kon
M-1s-1
pHTemp
°C
Glucagon receptor


(Homo sapiens (Human))
BDBM50144020
PNG
(3-{4-[1-(4-Benzofuran-2-yl-phenylcarbamoyl)-heptyl...)
Show SMILES CCCCCCC(Oc1ccc(cc1)C(=O)NCCC(O)=O)C(=O)Nc1ccc(cc1)-c1cc2ccccc2o1
Show InChI InChI=1S/C32H34N2O6/c1-2-3-4-5-10-28(39-26-17-13-23(14-18-26)31(37)33-20-19-30(35)36)32(38)34-25-15-11-22(12-16-25)29-21-24-8-6-7-9-27(24)40-29/h6-9,11-18,21,28H,2-5,10,19-20H2,1H3,(H,33,37)(H,34,38)(H,35,36)
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3n/an/an/an/an/an/an/an/a



Abbott Laboratories

Curated by ChEMBL


Assay Description
In vitro binding affinity against human glucagon receptor (h-GlucR) was determined


Citation and Details
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50360584
PNG
(CHEMBL1933350)
Show SMILES CCC[C@@H]([C@@H](c1c[nH]c2c(F)cc(C)cc12)c1ccc(Cl)cc1)c1ccc(cc1)C(=O)NCCC(O)=O
Show InChI InChI=1S/C30H30ClFN2O3/c1-3-4-23(19-5-7-21(8-6-19)30(37)33-14-13-27(35)36)28(20-9-11-22(31)12-10-20)25-17-34-29-24(25)15-18(2)16-26(29)32/h5-12,15-17,23,28,34H,3-4,13-14H2,1-2H3,(H,33,37)(H,35,36)/t23-,28+/m1/s1
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4n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Displacement of [125I]Glucagon-Cex from human GCGR


Citation and Details
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50144008
PNG
(3-{4-[2-(4-Benzofuran-2-yl-phenylcarbamoyl)-2-(4-t...)
Show SMILES CC(C)(C)c1ccc(cc1)C(Cc1ccc(cc1)C(=O)NCCC(O)=O)C(=O)Nc1ccc(cc1)-c1cc2ccccc2o1
Show InChI InChI=1S/C37H36N2O5/c1-37(2,3)29-16-12-25(13-17-29)31(22-24-8-10-27(11-9-24)35(42)38-21-20-34(40)41)36(43)39-30-18-14-26(15-19-30)33-23-28-6-4-5-7-32(28)44-33/h4-19,23,31H,20-22H2,1-3H3,(H,38,42)(H,39,43)(H,40,41)
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4n/an/an/an/an/an/an/an/a



Abbott Laboratories

Curated by ChEMBL


Assay Description
In vitro binding affinity against human glucagon receptor (h-GlucR) was determined


Citation and Details
More data for this
Ligand-Target Pair
Glucagon


(Homo sapiens (Human))
BDBM2437
PNG
(US8507533, 157)
Show SMILES CC1(C)CC(C1)C(Nc1cnc(nc1)-n1cc(cn1)C(F)(F)F)c1ccc(cc1)C(=O)NCCC(O)=O
Show InChI InChI=1S/C25H27F3N6O3/c1-24(2)9-17(10-24)21(15-3-5-16(6-4-15)22(37)29-8-7-20(35)36)33-19-12-30-23(31-13-19)34-14-18(11-32-34)25(26,27)28/h3-6,11-14,17,21,33H,7-10H2,1-2H3,(H,29,37)(H,35,36)
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US Patent
5.55n/an/an/an/an/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
The Glucagon SPA assay is used to determine the ability of test compounds to block the binding of glucagon-cex to the glucagon receptors.


US Patent US8507533 (2013)

More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM2437
PNG
(US8507533, 157)
Show SMILES CC1(C)CC(C1)C(Nc1cnc(nc1)-n1cc(cn1)C(F)(F)F)c1ccc(cc1)C(=O)NCCC(O)=O
Show InChI InChI=1S/C25H27F3N6O3/c1-24(2)9-17(10-24)21(15-3-5-16(6-4-15)22(37)29-8-7-20(35)36)33-19-12-30-23(31-13-19)34-14-18(11-32-34)25(26,27)28/h3-6,11-14,17,21,33H,7-10H2,1-2H3,(H,29,37)(H,35,36)
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5.60n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Displacement of [125I]-glucagon from human glucagon receptor expressed in Chem-1 cell membranes after 6 to 10 hrs by scintillation proximity assay


Bioorg Med Chem Lett 25: 4057-64 (2015)

More data for this
Ligand-Target Pair
Glucagon


(Homo sapiens (Human))
BDBM100827
PNG
(US8507533, 138 | US8507533, 151 | US8507533, 374)
Show SMILES Cc1cc(OC(C2CCC2)c2ccc(cc2)C(=O)NCCC(O)=O)cc(C)c1-n1cc(cn1)C(F)(F)F
Show InChI InChI=1S/C27H28F3N3O4/c1-16-12-22(13-17(2)24(16)33-15-21(14-32-33)27(28,29)30)37-25(18-4-3-5-18)19-6-8-20(9-7-19)26(36)31-11-10-23(34)35/h6-9,12-15,18,25H,3-5,10-11H2,1-2H3,(H,31,36)(H,34,35)
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US Patent
5.75n/an/an/an/an/an/a7.4n/a



Pfizer Inc.

US Patent


Assay Description
The Glucagon SPA assay is used to determine the ability of test compounds to block the binding of glucagon-cex to the glucagon receptors.


US Patent US8507533 (2013)

More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50144002
PNG
(3-{4-[2-(4-tert-Butyl-phenyl)-2-(2',4'-dichloro-bi...)
Show SMILES CC(C)(C)c1ccc(cc1)C(Cc1ccc(cc1)C(=O)NCCC(O)=O)C(=O)Nc1ccc(cc1)-c1ccc(Cl)cc1Cl
Show InChI InChI=1S/C35H34Cl2N2O4/c1-35(2,3)26-12-8-24(9-13-26)30(20-22-4-6-25(7-5-22)33(42)38-19-18-32(40)41)34(43)39-28-15-10-23(11-16-28)29-17-14-27(36)21-31(29)37/h4-17,21,30H,18-20H2,1-3H3,(H,38,42)(H,39,43)(H,40,41)
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6n/an/an/an/an/an/an/an/a



Abbott Laboratories

Curated by ChEMBL


Assay Description
In vitro binding affinity against human glucagon receptor (h-GlucR) was determined


Citation and Details
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50144015
PNG
(3-{4-[2-(4-Benzofuran-2-yl-phenylcarbamoyl)-octyl]...)
Show SMILES CCCCCCC(Cc1ccc(cc1)C(=O)NCCC(O)=O)C(=O)Nc1ccc(cc1)-c1cc2ccccc2o1
Show InChI InChI=1S/C33H36N2O5/c1-2-3-4-5-9-27(21-23-11-13-25(14-12-23)32(38)34-20-19-31(36)37)33(39)35-28-17-15-24(16-18-28)30-22-26-8-6-7-10-29(26)40-30/h6-8,10-18,22,27H,2-5,9,19-21H2,1H3,(H,34,38)(H,35,39)(H,36,37)
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6n/an/an/an/an/an/an/an/a



Abbott Laboratories

Curated by ChEMBL


Assay Description
In vitro binding affinity against human glucagon receptor (h-GlucR) was determined


Citation and Details
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50144001
PNG
(3-{4-[1-(2',4'-Dichloro-biphenyl-4-ylcarbamoyl)-he...)
Show SMILES CCCCCCC(Oc1ccc(cc1)C(=O)NCCC(O)=O)C(=O)Nc1ccc(cc1)-c1ccc(Cl)cc1Cl
Show InChI InChI=1S/C30H32Cl2N2O5/c1-2-3-4-5-6-27(39-24-14-9-21(10-15-24)29(37)33-18-17-28(35)36)30(38)34-23-12-7-20(8-13-23)25-16-11-22(31)19-26(25)32/h7-16,19,27H,2-6,17-18H2,1H3,(H,33,37)(H,34,38)(H,35,36)
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6n/an/an/an/an/an/an/an/a



Abbott Laboratories

Curated by ChEMBL


Assay Description
In vitro binding affinity against human glucagon receptor (h-GlucR) was determined


Citation and Details
More data for this
Ligand-Target Pair
Glucagon


(Homo sapiens (Human))
BDBM100806
PNG
(US8507533, 114 | US8507533, 115 | US8507533, 330)
Show SMILES CC1(C)CC(C1)C(Nc1ccc(nc1)-n1cc(cn1)C(F)(F)F)c1ccc(cc1)C(=O)NCCC(O)=O
Show InChI InChI=1S/C26H28F3N5O3/c1-25(2)11-18(12-25)23(16-3-5-17(6-4-16)24(37)30-10-9-22(35)36)33-20-7-8-21(31-14-20)34-15-19(13-32-34)26(27,28)29/h3-8,13-15,18,23,33H,9-12H2,1-2H3,(H,30,37)(H,35,36)
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US Patent
7.60n/an/an/an/an/an/a7.4n/a



Pfizer Inc.

US Patent


Assay Description
The Glucagon SPA assay is used to determine the ability of test compounds to block the binding of glucagon-cex to the glucagon receptors.


US Patent US8507533 (2013)

More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50144016
PNG
(3-{4-[(Biphenyl-4-ylcarbamoyl)-(4-tert-butyl-pheny...)
Show SMILES CC(C)(C)c1ccc(cc1)C(Oc1ccc(cc1)C(=O)NCCC(O)=O)C(=O)Nc1ccc(cc1)-c1ccccc1
Show InChI InChI=1S/C34H34N2O5/c1-34(2,3)27-15-9-25(10-16-27)31(41-29-19-13-26(14-20-29)32(39)35-22-21-30(37)38)33(40)36-28-17-11-24(12-18-28)23-7-5-4-6-8-23/h4-20,31H,21-22H2,1-3H3,(H,35,39)(H,36,40)(H,37,38)
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9n/an/an/an/an/an/an/an/a



Abbott Laboratories

Curated by ChEMBL


Assay Description
In vitro binding affinity against human glucagon receptor (h-GlucR) was determined


Citation and Details
More data for this
Ligand-Target Pair
Glucagon


(Homo sapiens (Human))
BDBM2390
PNG
(US8507533, 146)
Show SMILES OC(=O)CCNC(=O)c1ccc(cc1)[C@@H](Nc1ccc(nc1)-n1cc(cn1)C(F)(F)F)C1CCCCC1
Show InChI InChI=1S/C26H28F3N5O3/c27-26(28,29)20-14-32-34(16-20)22-11-10-21(15-31-22)33-24(17-4-2-1-3-5-17)18-6-8-19(9-7-18)25(37)30-13-12-23(35)36/h6-11,14-17,24,33H,1-5,12-13H2,(H,30,37)(H,35,36)/t24-/m0/s1
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9.05n/an/an/an/an/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
The Glucagon SPA assay is used to determine the ability of test compounds to block the binding of glucagon-cex to the glucagon receptors.


US Patent US8507533 (2013)

More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50144004
PNG
(3-{4-[2-(Biphenyl-4-ylcarbamoyl)-2-(4-tert-butyl-p...)
Show SMILES CC(C)(C)c1ccc(cc1)C(Cc1ccc(cc1)C(=O)NCCC(O)=O)C(=O)Nc1ccc(cc1)-c1ccccc1
Show InChI InChI=1S/C35H36N2O4/c1-35(2,3)29-17-13-27(14-18-29)31(23-24-9-11-28(12-10-24)33(40)36-22-21-32(38)39)34(41)37-30-19-15-26(16-20-30)25-7-5-4-6-8-25/h4-20,31H,21-23H2,1-3H3,(H,36,40)(H,37,41)(H,38,39)
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11n/an/an/an/an/an/an/an/a



Abbott Laboratories

Curated by ChEMBL


Assay Description
In vitro binding affinity against human glucagon receptor (h-GlucR) was determined


Citation and Details
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50144006
PNG
(3-{4-[2-(4-tert-Butyl-phenyl)-2-(quinolin-3-ylcarb...)
Show SMILES CC(C)(C)c1ccc(cc1)C(Cc1ccc(cc1)C(=O)NCCC(O)=O)C(=O)Nc1cnc2ccccc2c1
Show InChI InChI=1S/C32H33N3O4/c1-32(2,3)25-14-12-22(13-15-25)27(31(39)35-26-19-24-6-4-5-7-28(24)34-20-26)18-21-8-10-23(11-9-21)30(38)33-17-16-29(36)37/h4-15,19-20,27H,16-18H2,1-3H3,(H,33,38)(H,35,39)(H,36,37)
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11n/an/an/an/an/an/an/an/a



Abbott Laboratories

Curated by ChEMBL


Assay Description
In vitro binding affinity against human glucagon receptor (h-GlucR) was determined


Citation and Details
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50433595
PNG
(CHEMBL2381827)
Show SMILES CCCC(Nc1cc(C)c(c(C)c1)-n1cc(cn1)C(F)(F)F)c1ccc(cc1)C(=O)NCCC(O)=O
Show InChI InChI=1S/C26H29F3N4O3/c1-4-5-22(18-6-8-19(9-7-18)25(36)30-11-10-23(34)35)32-21-12-16(2)24(17(3)13-21)33-15-20(14-31-33)26(27,28)29/h6-9,12-15,22,32H,4-5,10-11H2,1-3H3,(H,30,36)(H,34,35)
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12n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin


Citation and Details
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM123630
PNG
(US8748624, 144)
Show SMILES OC(=O)CCNC(=O)c1ccc(cn1)-c1cc(Cl)ccc1CNc1ccc(c(Cl)c1)-c1ccc(F)c(c1)C(F)(F)F
Show InChI InChI=1S/C29H21Cl2F4N3O3/c30-19-4-1-17(22(12-19)18-3-8-26(38-15-18)28(41)36-10-9-27(39)40)14-37-20-5-6-21(24(31)13-20)16-2-7-25(32)23(11-16)29(33,34)35/h1-8,11-13,15,37H,9-10,14H2,(H,36,41)(H,39,40)
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US Patent
12.4n/an/an/an/an/an/a7.4n/a



Janssen Pharmaceutica NV

US Patent


Assay Description
The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incuba...


US Patent US8748624 (2014)

More data for this
Ligand-Target Pair
Glucagon


(Homo sapiens (Human))
BDBM142039
PNG
(US8927577, 118 | US8927577, 20 | US8927577, 35)
Show SMILES Cc1cc2cc(F)ccc2nc1NC(C1CC(C)(C)C1)c1ccc(cc1)C(=O)NCCC(O)=O
Show InChI InChI=1/C27H30FN3O3/c1-16-12-19-13-21(28)8-9-22(19)30-25(16)31-24(20-14-27(2,3)15-20)17-4-6-18(7-5-17)26(34)29-11-10-23(32)33/h4-9,12-13,20,24H,10-11,14-15H2,1-3H3,(H,29,34)(H,30,31)(H,32,33)
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14n/an/an/an/an/an/a7.4n/a



Pfizer Inc.

US Patent


Assay Description
The Glucagon SPA assay is used to determine the ability of test compounds to block the binding of glucagon-cex to the glucagon receptor. Test compoun...


US Patent US8927577 (2015)

More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM142039
PNG
(US8927577, 118 | US8927577, 20 | US8927577, 35)
Show SMILES Cc1cc2cc(F)ccc2nc1NC(C1CC(C)(C)C1)c1ccc(cc1)C(=O)NCCC(O)=O
Show InChI InChI=1/C27H30FN3O3/c1-16-12-19-13-21(28)8-9-22(19)30-25(16)31-24(20-14-27(2,3)15-20)17-4-6-18(7-5-17)26(34)29-11-10-23(32)33/h4-9,12-13,20,24H,10-11,14-15H2,1-3H3,(H,29,34)(H,30,31)(H,32,33)
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14n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Displacement of [125I]-glucagon from human glucagon receptor expressed in Chem-1 cell membranes after 6 to 10 hrs by scintillation proximity assay


Bioorg Med Chem Lett 25: 4057-64 (2015)

More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50433577
PNG
(CHEMBL2381848)
Show SMILES CCC[C@H](Oc1cc(C)c(c(C)c1)-n1cc(cn1)C(F)(F)F)c1ccc(cc1)C(=O)NCCC(O)=O
Show InChI InChI=1S/C26H28F3N3O4/c1-4-5-22(18-6-8-19(9-7-18)25(35)30-11-10-23(33)34)36-21-12-16(2)24(17(3)13-21)32-15-20(14-31-32)26(27,28)29/h6-9,12-15,22H,4-5,10-11H2,1-3H3,(H,30,35)(H,33,34)/t22-/m0/s1
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14n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin


Citation and Details
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM123549
PNG
(US8748624, 35)
Show SMILES OC(=O)CCNC(=O)c1ccc(cn1)-c1cc(ccc1CNc1ccc(c(Cl)c1)-c1ccc(F)c(Cl)c1)C(F)(F)F
Show InChI InChI=1S/C29H21Cl2F4N3O3/c30-23-13-20(5-6-21(23)16-2-7-25(32)24(31)11-16)37-14-17-1-4-19(29(33,34)35)12-22(17)18-3-8-26(38-15-18)28(41)36-10-9-27(39)40/h1-8,11-13,15,37H,9-10,14H2,(H,36,41)(H,39,40)
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14.4n/an/an/an/an/an/a7.4n/a



Janssen Pharmaceutica NV

US Patent


Assay Description
The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incuba...


US Patent US8748624 (2014)

More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM123582
PNG
(US8748624, 74)
Show SMILES OC(=O)CCNC(=O)c1ccc(cn1)-c1cc(cc(Cl)c1CNc1ccc(c(Cl)c1)-c1ccc(Cl)cc1)C(F)(F)F
Show InChI InChI=1S/C29H21Cl3F3N3O3/c30-19-4-1-16(2-5-19)21-7-6-20(13-25(21)32)37-15-23-22(11-18(12-24(23)31)29(33,34)35)17-3-8-26(38-14-17)28(41)36-10-9-27(39)40/h1-8,11-14,37H,9-10,15H2,(H,36,41)(H,39,40)
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14.9n/an/an/an/an/an/a7.4n/a



Janssen Pharmaceutica NV

US Patent


Assay Description
The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incuba...


US Patent US8748624 (2014)

More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50119555
PNG
(CHEMBL3617571)
Show SMILES CC(C)C[C@H](Nc1ccc(cn1)C(=O)NCCC(O)=O)c1cnc(nc1)-c1ccc(cc1)C(F)(F)F
Show InChI InChI=1/C25H26F3N5O3/c1-15(2)11-20(33-21-8-5-17(12-30-21)24(36)29-10-9-22(34)35)18-13-31-23(32-14-18)16-3-6-19(7-4-16)25(26,27)28/h3-8,12-15,20H,9-11H2,1-2H3,(H,29,36)(H,30,33)(H,34,35)/t20-/s2
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15n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Displacement of [125I]-glucagon from human glucagon receptor expressed in Chem-1 cell membranes after 6 to 10 hrs by scintillation proximity assay


Bioorg Med Chem Lett 25: 4057-64 (2015)

More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM123633
PNG
(US8748624, 147)
Show SMILES OC(=O)CCNC(=O)c1ccc(cn1)-c1cc(Cl)ccc1CNc1ccc(cc1)-c1ccc(cc1Cl)C(F)(F)F
Show InChI InChI=1S/C29H22Cl2F3N3O3/c30-21-6-1-18(24(14-21)19-4-10-26(37-16-19)28(40)35-12-11-27(38)39)15-36-22-7-2-17(3-8-22)23-9-5-20(13-25(23)31)29(32,33)34/h1-10,13-14,16,36H,11-12,15H2,(H,35,40)(H,38,39)
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15.7n/an/an/an/an/an/a7.4n/a



Janssen Pharmaceutica NV

US Patent


Assay Description
The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incuba...


US Patent US8748624 (2014)

More data for this
Ligand-Target Pair
Glucagon


(Homo sapiens (Human))
BDBM100806
PNG
(US8507533, 114 | US8507533, 115 | US8507533, 330)
Show SMILES CC1(C)CC(C1)C(Nc1ccc(nc1)-n1cc(cn1)C(F)(F)F)c1ccc(cc1)C(=O)NCCC(O)=O
Show InChI InChI=1S/C26H28F3N5O3/c1-25(2)11-18(12-25)23(16-3-5-17(6-4-16)24(37)30-10-9-22(35)36)33-20-7-8-21(31-14-20)34-15-19(13-32-34)26(27,28)29/h3-8,13-15,18,23,33H,9-12H2,1-2H3,(H,30,37)(H,35,36)
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15.8n/an/an/an/an/an/a7.4n/a



Pfizer Inc.

US Patent


Assay Description
The Glucagon SPA assay is used to determine the ability of test compounds to block the binding of glucagon-cex to the glucagon receptors.


US Patent US8507533 (2013)

More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM123556
PNG
(US8748624, 42)
Show SMILES OC(=O)CCNC(=O)c1ccc(cn1)-c1cc(ccc1CNc1ccc(c(Cl)c1)-c1ccc(cc1Cl)C(F)(F)F)C(F)(F)F
Show InChI InChI=1S/C30H21Cl2F6N3O3/c31-24-12-19(30(36,37)38)4-6-21(24)22-7-5-20(13-25(22)32)40-14-16-1-3-18(29(33,34)35)11-23(16)17-2-8-26(41-15-17)28(44)39-10-9-27(42)43/h1-8,11-13,15,40H,9-10,14H2,(H,39,44)(H,42,43)
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16.5n/an/an/an/an/an/a7.4n/a



Janssen Pharmaceutica NV

US Patent


Assay Description
The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incuba...


US Patent US8748624 (2014)

More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM123637
PNG
(US8748624, 151)
Show SMILES Cc1cc(F)ccc1-c1ccc(NCc2ccc(Cl)cc2-c2ccc(nc2)C(=O)NCCC(O)=O)cc1
Show InChI InChI=1S/C29H25ClFN3O3/c1-18-14-23(31)7-10-25(18)19-3-8-24(9-4-19)33-16-20-2-6-22(30)15-26(20)21-5-11-27(34-17-21)29(37)32-13-12-28(35)36/h2-11,14-15,17,33H,12-13,16H2,1H3,(H,32,37)(H,35,36)
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16.5n/an/an/an/an/an/a7.4n/a



Janssen Pharmaceutica NV

US Patent


Assay Description
The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incuba...


US Patent US8748624 (2014)

More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM123559
PNG
(US8748624, 51)
Show SMILES OC(=O)CCNC(=O)c1ccc(cn1)-c1cc(Cl)ccc1CNc1ccc(c(Cl)c1)-c1ccc(Cl)cc1Cl
Show InChI InChI=1S/C28H21Cl4N3O3/c29-18-3-1-16(23(11-18)17-2-8-26(35-15-17)28(38)33-10-9-27(36)37)14-34-20-5-7-22(25(32)13-20)21-6-4-19(30)12-24(21)31/h1-8,11-13,15,34H,9-10,14H2,(H,33,38)(H,36,37)
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16.8n/an/an/an/an/an/a7.4n/a



Janssen Pharmaceutica NV

US Patent


Assay Description
The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incuba...


US Patent US8748624 (2014)

More data for this
Ligand-Target Pair
Glucagon


(Homo sapiens (Human))
BDBM100796
PNG
(US8507533, 101)
Show SMILES OC(=O)CCNC(=O)c1ccc(cc1)C(Nc1ccc(nc1)-n1cc(cn1)C(F)(F)F)C1CCCCC1
Show InChI InChI=1S/C26H28F3N5O3/c27-26(28,29)20-14-32-34(16-20)22-11-10-21(15-31-22)33-24(17-4-2-1-3-5-17)18-6-8-19(9-7-18)25(37)30-13-12-23(35)36/h6-11,14-17,24,33H,1-5,12-13H2,(H,30,37)(H,35,36)
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17n/an/an/an/an/an/a7.4n/a



Pfizer Inc.

US Patent


Assay Description
The Glucagon SPA assay is used to determine the ability of test compounds to block the binding of glucagon-cex to the glucagon receptors.


US Patent US8507533 (2013)

More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50360599
PNG
(CHEMBL1933365)
Show SMILES OC(=O)CCNC(=O)c1ccc(cc1)C(Nc1cnn(c1)-c1ccc(cc1)C(F)(F)F)C1CCCC1
Show InChI InChI=1S/C26H27F3N4O3/c27-26(28,29)20-9-11-22(12-10-20)33-16-21(15-31-33)32-24(17-3-1-2-4-17)18-5-7-19(8-6-18)25(36)30-14-13-23(34)35/h5-12,15-17,24,32H,1-4,13-14H2,(H,30,36)(H,34,35)
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17n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Displacement of [125I]Glucagon-Cex from human GCGR


Citation and Details
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM123557
PNG
(US8748624, 43)
Show SMILES Cc1cc(ccc1-c1ccc(NCc2ccc(cc2-c2ccc(nc2)C(=O)NCCC(O)=O)C(F)(F)F)cc1Cl)C(F)(F)F
Show InChI InChI=1S/C31H24ClF6N3O3/c1-17-12-20(30(33,34)35)5-7-23(17)24-8-6-22(14-26(24)32)40-15-18-2-4-21(31(36,37)38)13-25(18)19-3-9-27(41-16-19)29(44)39-11-10-28(42)43/h2-9,12-14,16,40H,10-11,15H2,1H3,(H,39,44)(H,42,43)
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17n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Displacement of [125I]-glucagon from full length human glucagon receptor expressed in HEK293 cell membranes after 2 hrs by scintillation counting ana...


Bioorg Med Chem Lett 25: 4057-64 (2015)

More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50360599
PNG
(CHEMBL1933365)
Show SMILES OC(=O)CCNC(=O)c1ccc(cc1)C(Nc1cnn(c1)-c1ccc(cc1)C(F)(F)F)C1CCCC1
Show InChI InChI=1S/C26H27F3N4O3/c27-26(28,29)20-9-11-22(12-10-20)33-16-21(15-31-33)32-24(17-3-1-2-4-17)18-5-7-19(8-6-18)25(36)30-14-13-23(34)35/h5-12,15-17,24,32H,1-4,13-14H2,(H,30,36)(H,34,35)
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17n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Displacement of [125I]Glucagon-Cex from human GCGR


Citation and Details
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM123557
PNG
(US8748624, 43)
Show SMILES Cc1cc(ccc1-c1ccc(NCc2ccc(cc2-c2ccc(nc2)C(=O)NCCC(O)=O)C(F)(F)F)cc1Cl)C(F)(F)F
Show InChI InChI=1S/C31H24ClF6N3O3/c1-17-12-20(30(33,34)35)5-7-23(17)24-8-6-22(14-26(24)32)40-15-18-2-4-21(31(36,37)38)13-25(18)19-3-9-27(41-16-19)29(44)39-11-10-28(42)43/h2-9,12-14,16,40H,10-11,15H2,1H3,(H,39,44)(H,42,43)
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17.2n/an/an/an/an/an/a7.4n/a



Janssen Pharmaceutica NV

US Patent


Assay Description
The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incuba...


US Patent US8748624 (2014)

More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM123651
PNG
(US8748624, 174)
Show SMILES OC(=O)CCNC(=O)c1ccc(cn1)-c1cc(ccc1CNc1ccc(cc1)-c1ccc(F)cc1)C1=CCCCC1
Show InChI InChI=1S/C34H32FN3O3/c35-29-13-8-24(9-14-29)25-10-15-30(16-11-25)37-21-27-7-6-26(23-4-2-1-3-5-23)20-31(27)28-12-17-32(38-22-28)34(41)36-19-18-33(39)40/h4,6-17,20,22,37H,1-3,5,18-19,21H2,(H,36,41)(H,39,40)
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18.3n/an/an/an/an/an/a7.4n/a



Janssen Pharmaceutica NV

US Patent


Assay Description
The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incuba...


US Patent US8748624 (2014)

More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM123558
PNG
(US8748624, 44)
Show SMILES OC(=O)CCNC(=O)c1ccc(cn1)-c1cc(ccc1CNc1ccc(cc1)-c1ccc(Cl)cc1)C(F)(F)F
Show InChI InChI=1S/C29H23ClF3N3O3/c30-23-8-2-18(3-9-23)19-4-10-24(11-5-19)35-16-20-1-7-22(29(31,32)33)15-25(20)21-6-12-26(36-17-21)28(39)34-14-13-27(37)38/h1-12,15,17,35H,13-14,16H2,(H,34,39)(H,37,38)
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18.4n/an/an/an/an/an/a7.4n/a



Janssen Pharmaceutica NV

US Patent


Assay Description
The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incuba...


US Patent US8748624 (2014)

More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM123634
PNG
(US8748624, 148)
Show SMILES Cc1cc(Cl)ccc1-c1ccc(NCc2ccc(Cl)cc2-c2ccc(nc2)C(=O)NCCC(O)=O)cc1
Show InChI InChI=1S/C29H25Cl2N3O3/c1-18-14-22(30)7-10-25(18)19-3-8-24(9-4-19)33-16-20-2-6-23(31)15-26(20)21-5-11-27(34-17-21)29(37)32-13-12-28(35)36/h2-11,14-15,17,33H,12-13,16H2,1H3,(H,32,37)(H,35,36)
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18.7n/an/an/an/an/an/a7.4n/a



Janssen Pharmaceutica NV

US Patent


Assay Description
The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incuba...


US Patent US8748624 (2014)

More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM123575
PNG
(US8748624, 67)
Show SMILES OC(=O)CCNC(=O)c1ccc(cn1)-c1cc(cc(Cl)c1CNc1ccc(cc1)-c1ccc(Cl)cc1)C(F)(F)F
Show InChI InChI=1S/C29H22Cl2F3N3O3/c30-21-6-1-17(2-7-21)18-3-8-22(9-4-18)36-16-24-23(13-20(14-25(24)31)29(32,33)34)19-5-10-26(37-15-19)28(40)35-12-11-27(38)39/h1-10,13-15,36H,11-12,16H2,(H,35,40)(H,38,39)
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18.8n/an/an/an/an/an/a7.4n/a



Janssen Pharmaceutica NV

US Patent


Assay Description
The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incuba...


US Patent US8748624 (2014)

More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM123544
PNG
(US8748624, 30)
Show SMILES Cc1cc(ccc1-c1ccc(NCc2ccc(cc2-c2ccc(nc2)C(=O)NCCC(O)=O)C(F)(F)F)cc1)C(F)(F)F
Show InChI InChI=1S/C31H25F6N3O3/c1-18-14-22(30(32,33)34)7-10-25(18)19-3-8-24(9-4-19)39-16-20-2-6-23(31(35,36)37)15-26(20)21-5-11-27(40-17-21)29(43)38-13-12-28(41)42/h2-11,14-15,17,39H,12-13,16H2,1H3,(H,38,43)(H,41,42)
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19.3n/an/an/an/an/an/a7.4n/a



Janssen Pharmaceutica NV

US Patent


Assay Description
The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incuba...


US Patent US8748624 (2014)

More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM123535
PNG
(US8748624, 21)
Show SMILES OC(=O)CCNC(=O)c1ccc(cn1)-c1cc(ccc1CNc1ccc(cc1)-c1ccc(Cl)cc1Cl)C(F)(F)F
Show InChI InChI=1S/C29H22Cl2F3N3O3/c30-21-6-9-23(25(31)14-21)17-2-7-22(8-3-17)36-15-18-1-5-20(29(32,33)34)13-24(18)19-4-10-26(37-16-19)28(40)35-12-11-27(38)39/h1-10,13-14,16,36H,11-12,15H2,(H,35,40)(H,38,39)
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19.4n/an/an/an/an/an/a7.4n/a



Janssen Pharmaceutica NV

US Patent


Assay Description
The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incuba...


US Patent US8748624 (2014)

More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM123593
PNG
(US8748624, 92)
Show SMILES OC(=O)CCNC(=O)c1ccc(cn1)-c1cc(Cl)ccc1CNc1ccc(c(F)c1)-c1ccc(Cl)cc1Cl
Show InChI InChI=1S/C28H21Cl3FN3O3/c29-18-3-1-16(23(11-18)17-2-8-26(35-15-17)28(38)33-10-9-27(36)37)14-34-20-5-7-22(25(32)13-20)21-6-4-19(30)12-24(21)31/h1-8,11-13,15,34H,9-10,14H2,(H,33,38)(H,36,37)
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19.4n/an/an/an/an/an/a7.4n/a



Janssen Pharmaceutica NV

US Patent


Assay Description
The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incuba...


US Patent US8748624 (2014)

More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM123581
PNG
(US8748624, 73)
Show SMILES Cc1cc(Cl)ccc1-c1ccc(NCc2c(Cl)cc(cc2-c2ccc(nc2)C(=O)NCCC(O)=O)C(F)(F)F)cc1
Show InChI InChI=1S/C30H24Cl2F3N3O3/c1-17-12-21(31)5-8-23(17)18-2-6-22(7-3-18)37-16-25-24(13-20(14-26(25)32)30(33,34)35)19-4-9-27(38-15-19)29(41)36-11-10-28(39)40/h2-9,12-15,37H,10-11,16H2,1H3,(H,36,41)(H,39,40)
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19.5n/an/an/an/an/an/a7.4n/a



Janssen Pharmaceutica NV

US Patent


Assay Description
The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incuba...


US Patent US8748624 (2014)

More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM123560
PNG
(US8748624, 52)
Show SMILES OC(=O)CCNC(=O)c1ccc(cn1)-c1cc(Cl)ccc1CNc1ccc(c(Cl)c1)-c1ccc(F)cc1
Show InChI InChI=1S/C28H22Cl2FN3O3/c29-20-5-1-18(15-33-22-8-9-23(25(30)14-22)17-2-6-21(31)7-3-17)24(13-20)19-4-10-26(34-16-19)28(37)32-12-11-27(35)36/h1-10,13-14,16,33H,11-12,15H2,(H,32,37)(H,35,36)
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19.9n/an/an/an/an/an/a7.4n/a



Janssen Pharmaceutica NV

US Patent


Assay Description
The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incuba...


US Patent US8748624 (2014)

More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM123644
PNG
(US8748624, 158)
Show SMILES CC(C)c1ccc(CNc2ccc(cc2)-c2ccc(F)cc2)c(c1)-c1ccc(nc1)C(=O)NCCC(O)=O
Show InChI InChI=1S/C31H30FN3O3/c1-20(2)23-3-4-24(18-34-27-12-7-22(8-13-27)21-5-10-26(32)11-6-21)28(17-23)25-9-14-29(35-19-25)31(38)33-16-15-30(36)37/h3-14,17,19-20,34H,15-16,18H2,1-2H3,(H,33,38)(H,36,37)
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20n/an/an/an/an/an/a7.4n/a



Janssen Pharmaceutica NV

US Patent


Assay Description
The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incuba...


US Patent US8748624 (2014)

More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50119557
PNG
(CHEMBL3617575)
Show SMILES Cc1cc(Cl)ccc1-c1ccc(NCc2cc(Cl)cc(c2-c2ccc(nc2)C(=O)NCCC(O)=O)C(F)(F)F)cc1
Show InChI InChI=1S/C30H24Cl2F3N3O3/c1-17-12-21(31)5-8-24(17)18-2-6-23(7-3-18)37-16-20-13-22(32)14-25(30(33,34)35)28(20)19-4-9-26(38-15-19)29(41)36-11-10-27(39)40/h2-9,12-15,37H,10-11,16H2,1H3,(H,36,41)(H,39,40)
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20n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Displacement of [125I]-glucagon from full length human glucagon receptor expressed in HEK293 cell membranes after 2 hrs by scintillation counting ana...


Bioorg Med Chem Lett 25: 4057-64 (2015)

More data for this
Ligand-Target Pair
Glucagon


(Homo sapiens (Human))
BDBM100827
PNG
(US8507533, 138 | US8507533, 151 | US8507533, 374)
Show SMILES Cc1cc(OC(C2CCC2)c2ccc(cc2)C(=O)NCCC(O)=O)cc(C)c1-n1cc(cn1)C(F)(F)F
Show InChI InChI=1S/C27H28F3N3O4/c1-16-12-22(13-17(2)24(16)33-15-21(14-32-33)27(28,29)30)37-25(18-4-3-5-18)19-6-8-20(9-7-19)26(36)31-11-10-23(34)35/h6-9,12-15,18,25H,3-5,10-11H2,1-2H3,(H,31,36)(H,34,35)
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20.2n/an/an/an/an/an/a7.4n/a



Pfizer Inc.

US Patent


Assay Description
The Glucagon SPA assay is used to determine the ability of test compounds to block the binding of glucagon-cex to the glucagon receptors.


US Patent US8507533 (2013)

More data for this
Ligand-Target Pair
Glucagon


(Homo sapiens (Human))
BDBM2376
PNG
(US8507533, 137)
Show SMILES CCC[C@H](Nc1ccc(nc1)-n1cc(cn1)C(C)(C)C)c1ccc(cc1)C(=O)NCCC(O)=O
Show InChI InChI=1S/C26H33N5O3/c1-5-6-22(18-7-9-19(10-8-18)25(34)27-14-13-24(32)33)30-21-11-12-23(28-16-21)31-17-20(15-29-31)26(2,3)4/h7-12,15-17,22,30H,5-6,13-14H2,1-4H3,(H,27,34)(H,32,33)/t22-/m0/s1
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20.2n/an/an/an/an/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
The Glucagon SPA assay is used to determine the ability of test compounds to block the binding of glucagon-cex to the glucagon receptors.


US Patent US8507533 (2013)

More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM123580
PNG
(US8748624, 72)
Show SMILES OC(=O)CCNC(=O)c1ccc(cn1)-c1cc(cc(Cl)c1CNc1ccc(cc1)-c1ccc(Cl)cc1Cl)C(F)(F)F
Show InChI InChI=1S/C29H21Cl3F3N3O3/c30-19-4-7-21(25(32)13-19)16-1-5-20(6-2-16)37-15-23-22(11-18(12-24(23)31)29(33,34)35)17-3-8-26(38-14-17)28(41)36-10-9-27(39)40/h1-8,11-14,37H,9-10,15H2,(H,36,41)(H,39,40)
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20.3n/an/an/an/an/an/a7.4n/a



Janssen Pharmaceutica NV

US Patent


Assay Description
The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incuba...


US Patent US8748624 (2014)

More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM123555
PNG
(US8748624, 41)
Show SMILES OC(=O)CCNC(=O)c1ccc(cn1)-c1cc(ccc1CNc1ccc(cc1)-c1cccc(c1Cl)C(F)(F)F)C(F)(F)F
Show InChI InChI=1S/C30H22ClF6N3O3/c31-27-22(2-1-3-24(27)30(35,36)37)17-5-9-21(10-6-17)39-15-18-4-8-20(29(32,33)34)14-23(18)19-7-11-25(40-16-19)28(43)38-13-12-26(41)42/h1-11,14,16,39H,12-13,15H2,(H,38,43)(H,41,42)
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20.4n/an/an/an/an/an/a7.4n/a



Janssen Pharmaceutica NV

US Patent


Assay Description
The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incuba...


US Patent US8748624 (2014)

More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM123647
PNG
(US8748624, 170)
Show SMILES OC(=O)CCNC(=O)c1ccc(cn1)-c1cc(Cl)ccc1CNc1ccc(c(Cl)c1)-c1cccc(c1)C(F)(F)F
Show InChI InChI=1S/C29H22Cl2F3N3O3/c30-21-6-4-18(24(13-21)19-5-9-26(37-16-19)28(40)35-11-10-27(38)39)15-36-22-7-8-23(25(31)14-22)17-2-1-3-20(12-17)29(32,33)34/h1-9,12-14,16,36H,10-11,15H2,(H,35,40)(H,38,39)
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20.7n/an/an/an/an/an/a7.4n/a



Janssen Pharmaceutica NV

US Patent


Assay Description
The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incuba...


US Patent US8748624 (2014)

More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM123547
PNG
(US8748624, 33)
Show SMILES OC(=O)CCNC(=O)c1ccc(cn1)-c1cc(ccc1CNc1ccc(c(Cl)c1)-c1ccc(F)cc1Cl)C(F)(F)F
Show InChI InChI=1S/C29H21Cl2F4N3O3/c30-24-12-19(32)4-6-21(24)22-7-5-20(13-25(22)31)37-14-16-1-3-18(29(33,34)35)11-23(16)17-2-8-26(38-15-17)28(41)36-10-9-27(39)40/h1-8,11-13,15,37H,9-10,14H2,(H,36,41)(H,39,40)
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21.3n/an/an/an/an/an/a7.4n/a



Janssen Pharmaceutica NV

US Patent


Assay Description
The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incuba...


US Patent US8748624 (2014)

More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM123599
PNG
(US8748624, 102)
Show SMILES OC(=O)CCNC(=O)c1ccc(cn1)-c1cc(F)c(F)cc1CNc1ccc(c(Cl)c1)-c1ccc(F)c(c1)C(F)(F)F
Show InChI InChI=1S/C29H20ClF6N3O3/c30-22-11-18(3-4-19(22)15-1-5-23(31)21(9-15)29(34,35)36)38-14-17-10-24(32)25(33)12-20(17)16-2-6-26(39-13-16)28(42)37-8-7-27(40)41/h1-6,9-13,38H,7-8,14H2,(H,37,42)(H,40,41)
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21.3n/an/an/an/an/an/a7.4n/a



Janssen Pharmaceutica NV

US Patent


Assay Description
The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incuba...


US Patent US8748624 (2014)

More data for this
Ligand-Target Pair
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