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Vasopressin V1a receptor Inhibitors (IC50, Ki)

Structure
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Compound Name
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Standard Type
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Standard Values (in nM)
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ArgipressinKi1.13 [1]
LixivaptanIC50150.0 [1], 180.0 [2], 230.0 [3], 5000.0 [4]
LixivaptanKi44.0 [1], 6000.0 [2]
RelcovaptanIC5013.0 [1]
RelcovaptanKi0.19 [1], 0.52 [2], 0.7 [3], 0.85 [4], 1.48 [5]
4-[(3,5-Dihydroxyphenyl)methyl]-N-[[2-methyl-4-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepine-5-carbonyl)phenyl]methyl]piperazine-1-carboxamideIC507.0 [1], 613.0 [2]
Way-vna-932IC50778.0 [1], 1660.0 [2]
Way-vna-932Ki344.0 [1], 465.0 [2]
OxytocinIC5010000.0 [1]
OxytocinKi20.0 [1], 34.9 [2], 120.0 [3]
1-(1-(4-(3-Acetylaminopropoxy)benzoyl)-4-piperidyl)-3,4-dihydro-2(1H)-quinolinoneKi350.0 [1], 10000.0 [2], 14000.0 [3], 52000.0 [4]
2-Phenyl-4'-[(2,3,4,5-tetrahydro-1H-1-benzoazepine-1-yl)carbonyl]benzanilideIC502.74 [1]
2-Phenyl-4'-[(2,3,4,5-tetrahydro-1H-1-benzoazepine-1-yl)carbonyl]benzanilideKi2.74 [1], 14.1 [2]
(2S)-N-[(2S)-4-Amino-1-[[(2S)-1-[(3S)-3-[[(2S)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]-2-[[(2S)-2-[[(2R)-3-(4-hydroxyphenyl)-2-[[2-(4-hydroxyphenyl)acetyl]-methylamino]propanoyl]amino]-3-phenylpropanoyl]amino]pentanediamideKi0.03 [1], 0.04 [2], 0.21 [3], 0.28 [4]
Vasopressin, 1-(1-mercaptocyclohexaneacetic acid)-2-(O-methyl-L-tyrosine)-8-L-arginine-IC500.63 [1], 0.99 [2], 1.9 [3]
NelivaptanKi22.0 [1], 58.88 [2], 94.0 [3]
CID 6918320Ki1995.26 [1], 3200.0 [2]
2-(4-Fluoro-2-methylphenyl)-5-[4-(6-methoxypyridin-3-yl)-5-methyl-1,2,4-triazol-3-yl]pyrazineKi388.0 [1]
7-[4-[(3,5-Dimethoxyphenyl)methyl]piperazin-1-yl]-1-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepin-5-yl)heptan-1-oneIC5010000.0 [1]
7-[4-[(3,5-Dimethoxyphenyl)methyl]piperazin-1-yl]-1-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepin-5-yl)heptan-1-oneKi194.7 [1], 195.0 [2]
4-[(3,5-Dimethoxyphenyl)methyl]-N-[[2-methyl-4-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepine-5-carbonyl)phenyl]methyl]piperazine-1-carboxamideIC501113.0 [1]
4-[(3,5-Dimethoxyphenyl)methyl]-N-[[2-methyl-4-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepine-5-carbonyl)phenyl]methyl]piperazine-1-carboxamideKi62.0 [1]
8-[4-[(3,5-Dihydroxyphenyl)methyl]piperazin-1-yl]-1-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepin-5-yl)octan-1-oneIC504667.0 [1]
8-[4-[(3,5-Dihydroxyphenyl)methyl]piperazin-1-yl]-1-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepin-5-yl)octan-1-oneKi64.0 [1], 64.1 [2]
LIT-001 (free base)IC50100.0 [1], 2200.0 [2], 5900.0 [3]
LIT-001 (free base)Ki1253.0 [1]
1-[4-[(5-Fluoro-2-methylbenzoyl)amino]benzoyl]-N-(2-piperidin-1-ylethyl)spiro[3,5-dihydro-2H-1-benzazepine-4,3'-cyclopentene]-1'-carboxamideIC5010.0 [1], 16.0 [2], 48.0 [3], 71.0 [4]
AtosibanKi0.15 [1], 0.63 [2], 4.7 [3]
(2S)-2-(4-Methyl-1,4-diazepane-1-carbothioyl)-N-[[2-methyl-4-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepine-5-carbonyl)phenyl]methyl]pyrrolidine-1-carboxamideIC508.0 [1]
(2S)-2-(4-Methyl-1,4-diazepane-1-carbothioyl)-N-[[2-methyl-4-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepine-5-carbonyl)phenyl]methyl]pyrrolidine-1-carboxamideKi196.0 [1], 330.0 [2]
3-[4-[(4-Chlorophenyl)-[2-[(2-hydroxy-1H-indol-3-yl)diazenyl]-2-oxoethyl]sulfamoyl]phenyl]-N-[3-(dimethylamino)propyl]propanamideKi0.65 [1], 42.0 [2]
(2R)-N-[(1R,5S)-8-Azabicyclo[3.2.1]octan-3-yl]-3-(4-chlorophenyl)-2-[[2-(4-chlorophenyl)acetyl]amino]propanamideIC5054.95 [1]
(2R)-N-[(1R,5S)-8-Azabicyclo[3.2.1]octan-3-yl]-3-(4-chlorophenyl)-2-[[2-(4-chlorophenyl)acetyl]amino]propanamideKi0.23 [1]
N-(2-Pyridin-2-ylpyrazol-3-yl)-4-(trifluoromethyl)benzenesulfonamideIC5010000.0 [1]
N-(2-Pyridin-2-ylpyrazol-3-yl)-4-(trifluoromethyl)benzenesulfonamideKi10000.0 [1]
4-Chloro-N-(2-pyridin-2-ylpyrazol-3-yl)benzenesulfonamideIC5010000.0 [1]
4-Chloro-N-(2-pyridin-2-ylpyrazol-3-yl)benzenesulfonamideKi10000.0 [1]
(2S)-N-[(2S)-4-Amino-1-[[(2S)-1-[(4R)-4-[[(2S)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]carbamoyl]-1,3-selenazolidin-3-yl]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]-2-[[(2S)-2-[[(2R)-2-[3-(4-hydroxyphenyl)propanoylamino]-3-(4-methoxyphenyl)propanoyl]amino]-3-phenylpropanoyl]amino]pentanediamideKi0.4 [1], 0.9 [2], 3.8 [3]
4-Chloro-N-(2-methylpyrazol-3-yl)benzenesulfonamideIC5010000.0 [1]
4-Chloro-N-(2-methylpyrazol-3-yl)benzenesulfonamideKi10000.0 [1]
N-(2-Methylpyrazol-3-yl)-4-(trifluoromethyl)benzenesulfonamideIC5010000.0 [1]
N-(2-Methylpyrazol-3-yl)-4-(trifluoromethyl)benzenesulfonamideKi10000.0 [1]
ConivaptanIC503.0 [1]
ConivaptanKi0.43 [1]
SatavaptanKi304.0 [1], 2949.0 [2]
Unii-ER33G946JTKi180.0 [1]
CligosibanKi1120.0 [1]
Unii-4V7CN33O10IC505.0 [1], 38.0 [2]
CID 6918854Ki6309.57 [1]
1-[1-[2-[2-(2-Fluoroethoxy)-4-(1-methylsulfonylpiperidin-4-yl)oxyphenyl]acetyl]piperidin-4-yl]-3,4-dihydroquinolin-2-oneKi8700.0 [1]
[6-Chloro-1-[2-(dimethylamino)ethyl]indol-3-yl]-spiro[1H-2-benzofuran-3,4'-piperidine]-1'-ylmethanoneKi1.0 [1]
(2R)-2-[(2R,5R)-5-(2,3-Dihydro-1H-inden-2-yl)-2-(2-methylpropyl)-3,6-dioxopiperazin-1-yl]-2-(4-fluorophenyl)-N-propan-2-ylacetamideKi6309.57 [1]
(2R)-2-[(2R,5R)-5-(2,3-Dihydro-1H-inden-2-yl)-2-(2-methylpropyl)-3,6-dioxopiperazin-1-yl]-2-[4-(dimethylamino)phenyl]-N-propan-2-ylacetamideKi39810.72 [1]
2,4-Dichloro-N-[4-(6,11-dihydropyrrolo[2,1-c][1,4]benzodiazepine-5-carbonyl)phenyl]benzamideIC5015.0 [1]
N-[[5-[4-(2-Oxo-4H-3,1-benzoxazin-1-yl)piperidine-1-carbonyl]-1-benzofuran-2-yl]methyl]-2-[2-oxo-5-(trifluoromethyl)pyridin-1-yl]acetamideKi1258.93 [1], 1260.0 [2]
2-(N-(4-Ethoxyphenyl)sulfonyl-4-methylanilino)-N-[(2-hydroxy-1H-indol-3-yl)imino]acetamideKi1410.0 [1]
(2R)-2-(2,4-Difluorophenyl)-2-[(2R,5R)-5-(2,3-dihydro-1H-inden-2-yl)-2-(2-methylpropyl)-3,6-dioxopiperazin-1-yl]-N,N-dimethylacetamideKi630.96 [1], 6309.57 [2]
5-[3-[3-(2-Chloro-4-fluorophenoxy)azetidin-1-yl]-5-methyl-1,2,4-triazol-4-yl]-2-methoxypyridineKi2400.0 [1], 2430.0 [2]
5-[3-[3-(4-Fluoro-2-methylphenoxy)azetidin-1-yl]-5-methyl-1,2,4-triazol-4-yl]-2-methoxypyridineKi608.0 [1]
(4-Benzyl-4-hydroxypiperidin-1-yl)-(2-ethoxynaphthalen-1-yl)methanoneKi2830.0 [1]
(2S)-1-[(4R,7S,10S,13S,16S,19R)-19-Amino-7-(2-amino-2-oxoethyl)-10-(3-amino-3-oxopropyl)-13-benzyl-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]-N-[(2R)-1-[(2-amino-2-oxoethyl)amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]pyrrolidine-2-carboxamideKi3.4 [1], 3.8 [2]
[2-Chloro-4-(3-methylpyrazol-1-yl)phenyl]-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepin-5-yl)methanoneKi27.0 [1]
Benzyl 2-(2-methyl-1,3-dioxolan-2-yl)-2-[(3S,4R)-2-oxo-3-[(4S)-2-oxo-4-phenyl-1,3-oxazolidin-3-yl]-4-[(E)-2-phenylethenyl]azetidin-1-yl]acetateIC5045.0 [1]
(6-Chloro-1H-indol-3-yl)-spiro[1H-2-benzofuran-3,4'-piperidine]-1'-ylmethanoneKi4.0 [1]
(1-Benzyl-2-methylindol-3-yl)-spiro[1H-2-benzofuran-3,4'-piperidine]-1'-ylmethanoneKi2.0 [1]
(2-Ethoxynaphthalen-1-yl)-spiro[1H-2-benzofuran-3,4'-piperidine]-1'-ylmethanoneKi81.0 [1]
(2Z)-2-[1-[2-Chloro-4-(3-methylpyrazol-1-yl)benzoyl]-4,4-difluoro-2,3-dihydro-1-benzazepin-5-ylidene]-N-(2-hydroxyethyl)acetamideKi28.0 [1]
4-[2-[2-[3-Methyl-5-(4-phenylphenyl)-1,2,4-triazol-4-yl]phenoxy]ethyl]morpholineKi28.0 [1]
5-[3-(Ethoxymethyl)-5-(4-ethoxy-3-methylphenyl)-1,2,4-triazol-4-yl]-2-methoxypyridineKi549.0 [1], 594.0 [2]
N-(Cyclohexylmethyl)-1-[2-[1-(2,4-dimethoxyphenyl)sulfonyl-3,4-dihydro-2H-quinolin-2-yl]ethylsulfonyl]piperidin-4-amineKi188.0 [1], 5623.41 [2]
(4-Benzyl-4-hydroxypiperidin-1-yl)-(1-benzyl-2-methylindol-3-yl)methanoneKi295.0 [1]
N-[4-[(12S)-6-Chloro-2,10-diazatetracyclo[11.2.1.02,12.04,9]hexadeca-4(9),5,7-triene-10-carbonyl]phenyl]-2-(trifluoromethyl)benzamideIC504.0 [1]
N-[4-[(12S)-6-Chloro-2,10-diazatetracyclo[11.2.1.02,12.04,9]hexadeca-4(9),5,7-triene-10-carbonyl]phenyl]-2-(trifluoromethyl)benzamideKi40.0 [1]
N-[4-[(4As)-1,2,4,4a,5,11-hexahydro-[1,4]thiazino[3,4-c][1,4]benzodiazepine-6-carbonyl]phenyl]-2-phenylbenzamideKi84.0 [1], 1400.0 [2]
N-[2-(Dimethylamino)ethyl]-1-[4-[(2-phenylbenzoyl)amino]benzoyl]spiro[3,5-dihydro-2H-1-benzazepine-4,3'-cyclopentene]-1'-carboxamideIC504.0 [1], 5.0 [2]
(4R)-1-[4-[(2-Chloro-5-fluorobenzoyl)amino]-3-ethoxybenzoyl]spiro[3,5-dihydro-2H-1-benzazepine-4,3'-cyclopentene]-1'-carboxylic acidIC508.0 [1], 50.0 [2]
1-[4-[(2-Chloro-5-fluorobenzoyl)amino]-3-methoxybenzoyl]spiro[3,5-dihydro-2H-1-benzazepine-4,3'-cyclopentene]-1'-carboxylic acidIC5019.0 [1], 89.0 [2]
(4R)-1-[4-[(2-Chloro-5-fluorobenzoyl)amino]benzoyl]spiro[3,5-dihydro-2H-1-benzazepine-4,3'-cyclopentene]-1'-carboxylic acidIC5013.0 [1], 380.0 [2]
8-[4-[(3,5-Dimethoxyphenyl)methyl]piperazin-1-yl]-1-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepin-5-yl)octan-1-oneIC507674.0 [1]
8-[4-[(3,5-Dimethoxyphenyl)methyl]piperazin-1-yl]-1-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepin-5-yl)octan-1-oneKi248.0 [1]
5-[4-[(3,5-Dimethoxyphenyl)methyl]piperazin-1-yl]-1-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepin-5-yl)pentan-1-oneIC5010000.0 [1]
5-[4-[(3,5-Dimethoxyphenyl)methyl]piperazin-1-yl]-1-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepin-5-yl)pentan-1-oneKi409.0 [1]
6-[4-[(3,5-Dimethoxyphenyl)methyl]piperazin-1-yl]-1-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepin-5-yl)hexan-1-oneIC508203.0 [1]
6-[4-[(3,5-Dimethoxyphenyl)methyl]piperazin-1-yl]-1-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepin-5-yl)hexan-1-oneKi266.0 [1]
5-[4-[(3,5-Dihydroxyphenyl)methyl]piperazin-1-yl]-1-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepin-5-yl)pentan-1-oneIC5010000.0 [1]
5-[4-[(3,5-Dihydroxyphenyl)methyl]piperazin-1-yl]-1-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepin-5-yl)pentan-1-oneKi466.0 [1]
6-[4-[(3,5-Dihydroxyphenyl)methyl]piperazin-1-yl]-1-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepin-5-yl)hexan-1-oneIC5010000.0 [1]
6-[4-[(3,5-Dihydroxyphenyl)methyl]piperazin-1-yl]-1-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepin-5-yl)hexan-1-oneKi449.0 [1]
7-[4-[(3,5-Dihydroxyphenyl)methyl]piperazin-1-yl]-1-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepin-5-yl)heptan-1-oneIC5010000.0 [1]
7-[4-[(3,5-Dihydroxyphenyl)methyl]piperazin-1-yl]-1-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepin-5-yl)heptan-1-oneKi130.0 [1]
2-[4-[4-[(3,5-Dihydroxyphenyl)methyl]piperazin-1-yl]phenyl]-1-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepin-5-yl)ethanoneIC5010000.0 [1]
2-[4-[4-[(3,5-Dihydroxyphenyl)methyl]piperazin-1-yl]phenyl]-1-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepin-5-yl)ethanoneKi795.1 [1]
2-[2-[4-[(3,5-Dimethoxyphenyl)methyl]piperazin-1-yl]phenyl]-1-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepin-5-yl)ethanoneIC5010000.0 [1]
2-[2-[4-[(3,5-Dimethoxyphenyl)methyl]piperazin-1-yl]phenyl]-1-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepin-5-yl)ethanoneKi6807.0 [1]
2-[2-[4-[(3,5-Dihydroxyphenyl)methyl]piperazin-1-yl]phenyl]-1-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepin-5-yl)ethanoneIC5010000.0 [1]
2-[2-[4-[(3,5-Dihydroxyphenyl)methyl]piperazin-1-yl]phenyl]-1-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepin-5-yl)ethanoneKi1938.0 [1]
2-[4-[4-[(3,5-Dimethoxyphenyl)methyl]piperazin-1-yl]phenyl]-1-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepin-5-yl)ethanoneIC5010000.0 [1]
2-[4-[4-[(3,5-Dimethoxyphenyl)methyl]piperazin-1-yl]phenyl]-1-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepin-5-yl)ethanoneKi1910.0 [1]
3-[2-[4-[(3,5-Dihydroxyphenyl)methyl]piperazin-1-yl]phenyl]-1-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepin-5-yl)propan-1-oneIC5010000.0 [1]
Items per page: 1 - 10 of 99
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References

This online tool may be cited as follows

MLA

"Quest Database™ Vasopressin V1a receptor Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 21 Feb. 2025, https://www.aatbio.com/data-sets/vasopressin-v1a-receptor-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2025, February 21). Quest Database™ Vasopressin V1a receptor Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/vasopressin-v1a-receptor-inhibitors-ic50-ki.
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