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Patent code US10954225

Compile Data Set for Download or QSAR
Found 28 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
Glutamate receptor ionotropic, NMDA 2B


(Rattus norvegicus (Rat))
BDBM423269
PNG
(US10501451, Example 2, P-1 | US10501451, Example 2...)
Show SMILES Cc1ccc(CN2OCC(N3CCC(CC3)c3ccc(O)cc3)C2=O)cc1
Show InChI InChI=1S/C22H26N2O3/c1-16-2-4-17(5-3-16)14-24-22(26)21(15-27-24)23-12-10-19(11-13-23)18-6-8-20(25)9-7-18/h2-9,19,21,25H,10-15H2,1H3
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2.79n/an/an/an/an/an/an/an/a



Bristol-Myers Squibb Company

US Patent


Assay Description
To perform the competition binding assay, thawed membrane homogenate was added to each well of a 96-well plate (20 μg/well). The experimental co...


US Patent US10954225 (2021)

More data for this
Ligand-Target Pair
Glutamate receptor ionotropic, NMDA 2B


(Rattus norvegicus (Rat))
BDBM423291
PNG
(US10501451, Example 14, P-1 | US10501451, Example ...)
Show SMILES Oc1ccc(cc1F)C1CCN(CC1F)C1CCON(Cc2ccc(Cl)cc2)C1=O
Show InChI InChI=1S/C22H23ClF2N2O3/c23-16-4-1-14(2-5-16)12-27-22(29)20(8-10-30-27)26-9-7-17(19(25)13-26)15-3-6-21(28)18(24)11-15/h1-6,11,17,19-20,28H,7-10,12-13H2
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2.80n/an/an/an/an/an/an/an/a



Bristol-Myers Squibb Company

US Patent


Assay Description
To perform the competition binding assay, thawed membrane homogenate was added to each well of a 96-well plate (20 μg/well). The experimental co...


US Patent US10954225 (2021)

More data for this
Ligand-Target Pair
Glutamate receptor ionotropic, NMDA 2B


(Rattus norvegicus (Rat))
BDBM423285
PNG
(US10501451, Example 11, P-1 | US10501451, Example ...)
Show SMILES Cc1ccc(CN2OCCC(N3CCC(C(F)C3)c3ccc(O)c(F)c3)C2=O)cc1
Show InChI InChI=1S/C23H26F2N2O3/c1-15-2-4-16(5-3-15)13-27-23(29)21(9-11-30-27)26-10-8-18(20(25)14-26)17-6-7-22(28)19(24)12-17/h2-7,12,18,20-21,28H,8-11,13-14H2,1H3
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Bristol-Myers Squibb Company

US Patent


Assay Description
To perform the competition binding assay, thawed membrane homogenate was added to each well of a 96-well plate (20 μg/well). The experimental co...


US Patent US10954225 (2021)

More data for this
Ligand-Target Pair
Glutamate receptor ionotropic, NMDA 2B


(Rattus norvegicus (Rat))
BDBM423283
PNG
(US10501451, Example 10, P-1 | US10501451, Example ...)
Show SMILES Cc1ccc(CN2OCC(N3CCN(CC3)c3ccc(O)cn3)C2=O)cc1
Show InChI InChI=1S/C20H24N4O3/c1-15-2-4-16(5-3-15)13-24-20(26)18(14-27-24)22-8-10-23(11-9-22)19-7-6-17(25)12-21-19/h2-7,12,18,25H,8-11,13-14H2,1H3
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Bristol-Myers Squibb Company

US Patent


Assay Description
To perform the competition binding assay, thawed membrane homogenate was added to each well of a 96-well plate (20 μg/well). The experimental co...


US Patent US10954225 (2021)

More data for this
Ligand-Target Pair
Glutamate receptor ionotropic, NMDA 2B


(Rattus norvegicus (Rat))
BDBM423287
PNG
(US10501451, Example 12, P-1 | US10501451, Example ...)
Show SMILES Oc1ccc(cc1)[C@@H]1CCN(C[C@H]1F)C1CCON(Cc2ccc(Cl)cc2)C1=O
Show InChI InChI=1S/C22H24ClFN2O3/c23-17-5-1-15(2-6-17)13-26-22(28)21(10-12-29-26)25-11-9-19(20(24)14-25)16-3-7-18(27)8-4-16/h1-8,19-21,27H,9-14H2/t19-,20+,21?/m0/s1
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3.90n/an/an/an/an/an/an/an/a



Bristol-Myers Squibb Company

US Patent


Assay Description
To perform the competition binding assay, thawed membrane homogenate was added to each well of a 96-well plate (20 μg/well). The experimental co...


US Patent US10954225 (2021)

More data for this
Ligand-Target Pair
Glutamate receptor ionotropic, NMDA 2B


(Rattus norvegicus (Rat))
BDBM423289
PNG
(US10501451, Example 13, P-1 | US10501451, Example ...)
Show SMILES Oc1ccc(cc1F)C1CCN(CC1F)C1CCON(Cc2ccc(F)cc2)C1=O
Show InChI InChI=1S/C22H23F3N2O3/c23-16-4-1-14(2-5-16)12-27-22(29)20(8-10-30-27)26-9-7-17(19(25)13-26)15-3-6-21(28)18(24)11-15/h1-6,11,17,19-20,28H,7-10,12-13H2
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Bristol-Myers Squibb Company

US Patent


Assay Description
To perform the competition binding assay, thawed membrane homogenate was added to each well of a 96-well plate (20 μg/well). The experimental co...


US Patent US10954225 (2021)

More data for this
Ligand-Target Pair
Glutamate receptor ionotropic, NMDA 2B


(Rattus norvegicus (Rat))
BDBM423267
PNG
(US10501451, Example 1, P-1 | US10501451, Example 1...)
Show SMILES Oc1ccc(cc1)C1CCN(CC1)C1CON(Cc2ccc(F)cc2)C1=O
Show InChI InChI=1S/C21H23FN2O3/c22-18-5-1-15(2-6-18)13-24-21(26)20(14-27-24)23-11-9-17(10-12-23)16-3-7-19(25)8-4-16/h1-8,17,20,25H,9-14H2
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Bristol-Myers Squibb Company

US Patent


Assay Description
To perform the competition binding assay, thawed membrane homogenate was added to each well of a 96-well plate (20 μg/well). The experimental co...


US Patent US10954225 (2021)

More data for this
Ligand-Target Pair
Glutamate receptor ionotropic, NMDA 2B


(Rattus norvegicus (Rat))
BDBM423273
PNG
(US10501451, Example 5, P-1 | US10501451, Example 5...)
Show SMILES Cc1ccc(CN2OCCC(N3CC[C@H]([C@H](F)C3)c3ccc(O)cc3)C2=O)cc1
Show InChI InChI=1S/C23H27FN2O3/c1-16-2-4-17(5-3-16)14-26-23(28)22(11-13-29-26)25-12-10-20(21(24)15-25)18-6-8-19(27)9-7-18/h2-9,20-22,27H,10-15H2,1H3/t20-,21+,22?/m0/s1
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US Patent


Assay Description
To perform the competition binding assay, thawed membrane homogenate was added to each well of a 96-well plate (20 μg/well). The experimental co...


US Patent US10954225 (2021)

More data for this
Ligand-Target Pair
Glutamate receptor ionotropic, NMDA 2B


(Rattus norvegicus (Rat))
BDBM423277
PNG
(US10501451, Example 7, P-1 | US10501451, Example 7...)
Show SMILES Cc1ccc(CN2OCCC(N3CC[C@@H]([C@@H](F)C3)c3ccc(O)cc3)C2=O)cc1
Show InChI InChI=1S/C23H27FN2O3/c1-16-2-4-17(5-3-16)14-26-23(28)22(11-13-29-26)25-12-10-20(21(24)15-25)18-6-8-19(27)9-7-18/h2-9,20-22,27H,10-15H2,1H3/t20-,21+,22?/m1/s1
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US Patent


Assay Description
To perform the competition binding assay, thawed membrane homogenate was added to each well of a 96-well plate (20 μg/well). The experimental co...


US Patent US10954225 (2021)

More data for this
Ligand-Target Pair
Glutamate receptor ionotropic, NMDA 2B


(Rattus norvegicus (Rat))
BDBM423272
PNG
((Racemic Mixture) | US10501451, Example 4 | US1095...)
Show SMILES Cc1ccc(CN2OCCC(N3CCC(CC3)c3ccc(O)cc3)C2=O)cc1
Show InChI InChI=1S/C23H28N2O3/c1-17-2-4-18(5-3-17)16-25-23(27)22(12-15-28-25)24-13-10-20(11-14-24)19-6-8-21(26)9-7-19/h2-9,20,22,26H,10-16H2,1H3
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5.49n/an/an/an/an/an/an/an/a



Bristol-Myers Squibb Company

US Patent


Assay Description
To perform the competition binding assay, thawed membrane homogenate was added to each well of a 96-well plate (20 μg/well). The experimental co...


US Patent US10954225 (2021)

More data for this
Ligand-Target Pair
Glutamate receptor ionotropic, NMDA 2B


(Rattus norvegicus (Rat))
BDBM423275
PNG
(US10501451, Example 6, P-1 | US10501451, Example 6...)
Show SMILES Cc1ccc(CN2OCCC(N3CCC(CC3)c3ccc(O)cn3)C2=O)cc1
Show InChI InChI=1S/C22H27N3O3/c1-16-2-4-17(5-3-16)15-25-22(27)21(10-13-28-25)24-11-8-18(9-12-24)20-7-6-19(26)14-23-20/h2-7,14,18,21,26H,8-13,15H2,1H3
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6.53n/an/an/an/an/an/an/an/a



Bristol-Myers Squibb Company

US Patent


Assay Description
To perform the competition binding assay, thawed membrane homogenate was added to each well of a 96-well plate (20 μg/well). The experimental co...


US Patent US10954225 (2021)

More data for this
Ligand-Target Pair
Glutamate receptor ionotropic, NMDA 2B


(Rattus norvegicus (Rat))
BDBM423275
PNG
(US10501451, Example 6, P-1 | US10501451, Example 6...)
Show SMILES Cc1ccc(CN2OCCC(N3CCC(CC3)c3ccc(O)cn3)C2=O)cc1
Show InChI InChI=1S/C22H27N3O3/c1-16-2-4-17(5-3-16)15-25-22(27)21(10-13-28-25)24-11-8-18(9-12-24)20-7-6-19(26)14-23-20/h2-7,14,18,21,26H,8-13,15H2,1H3
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Bristol-Myers Squibb Company

US Patent


Assay Description
To perform the competition binding assay, thawed membrane homogenate was added to each well of a 96-well plate (20 μg/well). The experimental co...


US Patent US10954225 (2021)

More data for this
Ligand-Target Pair
Glutamate receptor ionotropic, NMDA 2B


(Rattus norvegicus (Rat))
BDBM423283
PNG
(US10501451, Example 10, P-1 | US10501451, Example ...)
Show SMILES Cc1ccc(CN2OCC(N3CCN(CC3)c3ccc(O)cn3)C2=O)cc1
Show InChI InChI=1S/C20H24N4O3/c1-15-2-4-16(5-3-15)13-24-20(26)18(14-27-24)22-8-10-23(11-9-22)19-7-6-17(25)12-21-19/h2-7,12,18,25H,8-11,13-14H2,1H3
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Bristol-Myers Squibb Company

US Patent


Assay Description
To perform the competition binding assay, thawed membrane homogenate was added to each well of a 96-well plate (20 μg/well). The experimental co...


US Patent US10954225 (2021)

More data for this
Ligand-Target Pair
Glutamate receptor ionotropic, NMDA 2B


(Rattus norvegicus (Rat))
BDBM423281
PNG
(US10501451, Example 9, P-1 | US10501451, Example 9...)
Show SMILES Cc1ccc(CN2OCC(N3CCC(CC3)c3ccc(O)cn3)C2=O)cc1
Show InChI InChI=1S/C21H25N3O3/c1-15-2-4-16(5-3-15)13-24-21(26)20(14-27-24)23-10-8-17(9-11-23)19-7-6-18(25)12-22-19/h2-7,12,17,20,25H,8-11,13-14H2,1H3
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Bristol-Myers Squibb Company

US Patent


Assay Description
To perform the competition binding assay, thawed membrane homogenate was added to each well of a 96-well plate (20 μg/well). The experimental co...


US Patent US10954225 (2021)

More data for this
Ligand-Target Pair
Glutamate receptor ionotropic, NMDA 2B


(Rattus norvegicus (Rat))
BDBM488170
PNG
(US10954225, Example 15,P-1 | US10954225, Example 1...)
Show SMILES Oc1ccc(cc1)C1CCN(C[C@H]1F)C1CCON(Cc2ccc(F)cc2)C1=O
Show InChI InChI=1S/C22H24F2N2O3/c23-17-5-1-15(2-6-17)13-26-22(28)21(10-12-29-26)25-11-9-19(20(24)14-25)16-3-7-18(27)8-4-16/h1-8,19-21,27H,9-14H2/t19?,20-,21?/m1/s1
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Bristol-Myers Squibb Company

US Patent


Assay Description
To perform the competition binding assay, thawed membrane homogenate was added to each well of a 96-well plate (20 μg/well). The experimental co...


US Patent US10954225 (2021)

More data for this
Ligand-Target Pair
Glutamate receptor ionotropic, NMDA 2B


(Rattus norvegicus (Rat))
BDBM423271
PNG
((Racemic Mixture) | US10501451, Example 3 | US1095...)
Show SMILES Oc1ccc(nc1)C1CCN(CC1)C1CON(Cc2ccc(F)cc2)C1=O
Show InChI InChI=1S/C20H22FN3O3/c21-16-3-1-14(2-4-16)12-24-20(26)19(13-27-24)23-9-7-15(8-10-23)18-6-5-17(25)11-22-18/h1-6,11,15,19,25H,7-10,12-13H2
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Bristol-Myers Squibb Company

US Patent


Assay Description
To perform the competition binding assay, thawed membrane homogenate was added to each well of a 96-well plate (20 μg/well). The experimental co...


US Patent US10954225 (2021)

More data for this
Ligand-Target Pair
Glutamate receptor ionotropic, NMDA 2B


(Rattus norvegicus (Rat))
BDBM423279
PNG
(US10501451, Example 8, P-1 | US10501451, Example 8...)
Show SMILES Cc1ccc(CN2OCCC(N3CCN(CC3)c3ccc(O)cn3)C2=O)cc1
Show InChI InChI=1S/C21H26N4O3/c1-16-2-4-17(5-3-16)15-25-21(27)19(8-13-28-25)23-9-11-24(12-10-23)20-7-6-18(26)14-22-20/h2-7,14,19,26H,8-13,15H2,1H3
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Bristol-Myers Squibb Company

US Patent


Assay Description
To perform the competition binding assay, thawed membrane homogenate was added to each well of a 96-well plate (20 μg/well). The experimental co...


US Patent US10954225 (2021)

More data for this
Ligand-Target Pair
Glutamate receptor ionotropic, NMDA 2B


(Rattus norvegicus (Rat))
BDBM423285
PNG
(US10501451, Example 11, P-1 | US10501451, Example ...)
Show SMILES Cc1ccc(CN2OCCC(N3CCC(C(F)C3)c3ccc(O)c(F)c3)C2=O)cc1
Show InChI InChI=1S/C23H26F2N2O3/c1-15-2-4-16(5-3-15)13-27-23(29)21(9-11-30-27)26-10-8-18(20(25)14-26)17-6-7-22(28)19(24)12-17/h2-7,12,18,20-21,28H,8-11,13-14H2,1H3
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Bristol-Myers Squibb Company

US Patent


Assay Description
To perform the competition binding assay, thawed membrane homogenate was added to each well of a 96-well plate (20 μg/well). The experimental co...


US Patent US10954225 (2021)

More data for this
Ligand-Target Pair
Glutamate receptor ionotropic, NMDA 2B


(Rattus norvegicus (Rat))
BDBM423279
PNG
(US10501451, Example 8, P-1 | US10501451, Example 8...)
Show SMILES Cc1ccc(CN2OCCC(N3CCN(CC3)c3ccc(O)cn3)C2=O)cc1
Show InChI InChI=1S/C21H26N4O3/c1-16-2-4-17(5-3-16)15-25-21(27)19(8-13-28-25)23-9-11-24(12-10-23)20-7-6-18(26)14-22-20/h2-7,14,19,26H,8-13,15H2,1H3
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US Patent


Assay Description
To perform the competition binding assay, thawed membrane homogenate was added to each well of a 96-well plate (20 μg/well). The experimental co...


US Patent US10954225 (2021)

More data for this
Ligand-Target Pair
Glutamate receptor ionotropic, NMDA 2B


(Rattus norvegicus (Rat))
BDBM423291
PNG
(US10501451, Example 14, P-1 | US10501451, Example ...)
Show SMILES Oc1ccc(cc1F)C1CCN(CC1F)C1CCON(Cc2ccc(Cl)cc2)C1=O
Show InChI InChI=1S/C22H23ClF2N2O3/c23-16-4-1-14(2-5-16)12-27-22(29)20(8-10-30-27)26-9-7-17(19(25)13-26)15-3-6-21(28)18(24)11-15/h1-6,11,17,19-20,28H,7-10,12-13H2
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Bristol-Myers Squibb Company

US Patent


Assay Description
To perform the competition binding assay, thawed membrane homogenate was added to each well of a 96-well plate (20 μg/well). The experimental co...


US Patent US10954225 (2021)

More data for this
Ligand-Target Pair
Glutamate receptor ionotropic, NMDA 2B


(Rattus norvegicus (Rat))
BDBM423269
PNG
(US10501451, Example 2, P-1 | US10501451, Example 2...)
Show SMILES Cc1ccc(CN2OCC(N3CCC(CC3)c3ccc(O)cc3)C2=O)cc1
Show InChI InChI=1S/C22H26N2O3/c1-16-2-4-17(5-3-16)14-24-22(26)21(15-27-24)23-12-10-19(11-13-23)18-6-8-20(25)9-7-18/h2-9,19,21,25H,10-15H2,1H3
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112n/an/an/an/an/an/an/an/a



Bristol-Myers Squibb Company

US Patent


Assay Description
To perform the competition binding assay, thawed membrane homogenate was added to each well of a 96-well plate (20 μg/well). The experimental co...


US Patent US10954225 (2021)

More data for this
Ligand-Target Pair
Glutamate receptor ionotropic, NMDA 2B


(Rattus norvegicus (Rat))
BDBM423277
PNG
(US10501451, Example 7, P-1 | US10501451, Example 7...)
Show SMILES Cc1ccc(CN2OCCC(N3CC[C@@H]([C@@H](F)C3)c3ccc(O)cc3)C2=O)cc1
Show InChI InChI=1S/C23H27FN2O3/c1-16-2-4-17(5-3-16)14-26-23(28)22(11-13-29-26)25-12-10-20(21(24)15-25)18-6-8-19(27)9-7-18/h2-9,20-22,27H,10-15H2,1H3/t20-,21+,22?/m1/s1
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US Patent


Assay Description
To perform the competition binding assay, thawed membrane homogenate was added to each well of a 96-well plate (20 μg/well). The experimental co...


US Patent US10954225 (2021)

More data for this
Ligand-Target Pair
Glutamate receptor ionotropic, NMDA 2B


(Rattus norvegicus (Rat))
BDBM423281
PNG
(US10501451, Example 9, P-1 | US10501451, Example 9...)
Show SMILES Cc1ccc(CN2OCC(N3CCC(CC3)c3ccc(O)cn3)C2=O)cc1
Show InChI InChI=1S/C21H25N3O3/c1-15-2-4-16(5-3-15)13-24-21(26)20(14-27-24)23-10-8-17(9-11-23)19-7-6-18(25)12-22-19/h2-7,12,17,20,25H,8-11,13-14H2,1H3
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US Patent
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Bristol-Myers Squibb Company

US Patent


Assay Description
To perform the competition binding assay, thawed membrane homogenate was added to each well of a 96-well plate (20 μg/well). The experimental co...


US Patent US10954225 (2021)

More data for this
Ligand-Target Pair
Glutamate receptor ionotropic, NMDA 2B


(Rattus norvegicus (Rat))
BDBM423273
PNG
(US10501451, Example 5, P-1 | US10501451, Example 5...)
Show SMILES Cc1ccc(CN2OCCC(N3CC[C@H]([C@H](F)C3)c3ccc(O)cc3)C2=O)cc1
Show InChI InChI=1S/C23H27FN2O3/c1-16-2-4-17(5-3-16)14-26-23(28)22(11-13-29-26)25-12-10-20(21(24)15-25)18-6-8-19(27)9-7-18/h2-9,20-22,27H,10-15H2,1H3/t20-,21+,22?/m0/s1
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Bristol-Myers Squibb Company

US Patent


Assay Description
To perform the competition binding assay, thawed membrane homogenate was added to each well of a 96-well plate (20 μg/well). The experimental co...


US Patent US10954225 (2021)

More data for this
Ligand-Target Pair
Glutamate receptor ionotropic, NMDA 2B


(Rattus norvegicus (Rat))
BDBM423287
PNG
(US10501451, Example 12, P-1 | US10501451, Example ...)
Show SMILES Oc1ccc(cc1)[C@@H]1CCN(C[C@H]1F)C1CCON(Cc2ccc(Cl)cc2)C1=O
Show InChI InChI=1S/C22H24ClFN2O3/c23-17-5-1-15(2-6-17)13-26-22(28)21(10-12-29-26)25-11-9-19(20(24)14-25)16-3-7-18(27)8-4-16/h1-8,19-21,27H,9-14H2/t19-,20+,21?/m0/s1
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Bristol-Myers Squibb Company

US Patent


Assay Description
To perform the competition binding assay, thawed membrane homogenate was added to each well of a 96-well plate (20 μg/well). The experimental co...


US Patent US10954225 (2021)

More data for this
Ligand-Target Pair
Glutamate receptor ionotropic, NMDA 2B


(Rattus norvegicus (Rat))
BDBM423267
PNG
(US10501451, Example 1, P-1 | US10501451, Example 1...)
Show SMILES Oc1ccc(cc1)C1CCN(CC1)C1CON(Cc2ccc(F)cc2)C1=O
Show InChI InChI=1S/C21H23FN2O3/c22-18-5-1-15(2-6-18)13-24-21(26)20(14-27-24)23-11-9-17(10-12-23)16-3-7-19(25)8-4-16/h1-8,17,20,25H,9-14H2
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Bristol-Myers Squibb Company

US Patent


Assay Description
To perform the competition binding assay, thawed membrane homogenate was added to each well of a 96-well plate (20 μg/well). The experimental co...


US Patent US10954225 (2021)

More data for this
Ligand-Target Pair
Glutamate receptor ionotropic, NMDA 2B


(Rattus norvegicus (Rat))
BDBM423289
PNG
(US10501451, Example 13, P-1 | US10501451, Example ...)
Show SMILES Oc1ccc(cc1F)C1CCN(CC1F)C1CCON(Cc2ccc(F)cc2)C1=O
Show InChI InChI=1S/C22H23F3N2O3/c23-16-4-1-14(2-5-16)12-27-22(29)20(8-10-30-27)26-9-7-17(19(25)13-26)15-3-6-21(28)18(24)11-15/h1-6,11,17,19-20,28H,7-10,12-13H2
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Bristol-Myers Squibb Company

US Patent


Assay Description
To perform the competition binding assay, thawed membrane homogenate was added to each well of a 96-well plate (20 μg/well). The experimental co...


US Patent US10954225 (2021)

More data for this
Ligand-Target Pair
Glutamate receptor ionotropic, NMDA 2B


(Rattus norvegicus (Rat))
BDBM488170
PNG
(US10954225, Example 15,P-1 | US10954225, Example 1...)
Show SMILES Oc1ccc(cc1)C1CCN(C[C@H]1F)C1CCON(Cc2ccc(F)cc2)C1=O
Show InChI InChI=1S/C22H24F2N2O3/c23-17-5-1-15(2-6-17)13-26-22(28)21(10-12-29-26)25-11-9-19(20(24)14-25)16-3-7-18(27)8-4-16/h1-8,19-21,27H,9-14H2/t19?,20-,21?/m1/s1
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Bristol-Myers Squibb Company

US Patent


Assay Description
To perform the competition binding assay, thawed membrane homogenate was added to each well of a 96-well plate (20 μg/well). The experimental co...


US Patent US10954225 (2021)

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