General Information of the Protein
Protein ID
PT01839
Protein Name
Vasopressin V1a receptor
Secondarily
Protein Name
AVPR V1a
Antidiuretic hormone receptor 1a
Vascular/hepatic-type arginine vasopressin receptor
Gene Name
AVPR1A
Secondarily
Gene Name
AVPR1
Sequence
MRLSAGPDAGPSGNSSPWWPLATGAGNTSREAEALGEGNGPPRDVRNEELAKLEIAVLAVTFAVAVLGNSSVLLALHRTPRKTSRMHLFIRHLSLADLAVAFFQVLPQMCWDITYRFRGPDWLCRVVKHLQVFGMFASAYMLVVMTADRYIAVCHPLKTLQQPARRSRLMIAAAWVLSFVLSTPQYFVFSMIEVNNVTKARDCWATFIQPWGSRAYVTWMTGGIFVAPVVILGTCYGFICYNIWCNVRGKTASRQSKGAEQAGVAFQKGFLLAPCVSSVKSISRAKIRTVKMTFVIVTAYIVCWAPFFIIQMWSVWDPMSVWTESENPTITITALLGSLNSCCNPWIYMFFSGHLLQDCVQSFPCCQNMKEKFNKEDTDSMSRRQTFYSNNRSPTNSTGMWKDSPKSSKSIKFIPVST
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Organism
Homo sapiens, Human
Protein Classification
Membrane receptor
>
Family A G protein-coupled receptor
>
Peptide receptor (family A GPCR)
>
Short peptide receptor (family A GPCR)
>
Vasopressin and oxytocin receptor
Function
Receptor for arginine vasopressin. The activity of this receptor is mediated by G proteins which activate a phosphatidyl-inositol-calcium second messenger system. Has been involved in social behaviors, including affiliation and attachment.
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Uniprot ID
P37288
HGNC ID
HGNC:895
Subcellular Location
Cell membrane
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000094 , 1321N1
Compound ID Compound Name Compound Formula
CP0471688
CHEMBL4799793
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C22H23ClN4O
 2
1
IC50 = 1 nM
   TI
   LI
   LO
   TS
2
Ki = 0.8 nM
   TI
   LI
   LO
   TS
CP0546313
CHEMBL5070261
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C22H23ClN4O2
 1
1
IC50 = 1.1 nM
   TI
   LI
   LO
   TS
CP0576666
(5S)-8-chloro-1-(4-pyridin-2-yloxycyclohexyl)-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-ol
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C22H23ClN4O2
 1
1
IC50 = 1.2 nM
   TI
   LI
   LO
   TS
CP0492304
8-bromo-1-(4-pyridin-2-yloxycyclohexyl)-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine
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C22H23BrN4O
 2
1
IC50 = 1.3 nM
   TI
   LI
   LO
   TS
2
Ki = 0.6 nM
   TI
   LI
   LO
   TS
CP0496263
3-[4-(8-bromo-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-1-yl)cyclohexyl]-5-methyl-1,2-oxazole
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C21H23BrN4O
 2
1
IC50 = 1.7 nM
   TI
   LI
   LO
   TS
2
Ki = 0.6 nM
   TI
   LI
   LO
   TS
CP0575713
CHEMBL5070075
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C22H23ClN4O2
 1
1
IC50 = 1.8 nM
   TI
   LI
   LO
   TS
CP0576681
CHEMBL5081323
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C23H26N4O2
 1
1
IC50 = 1.9 nM
   TI
   LI
   LO
   TS
CP0244529
[6-chloro-1-[2-(dimethylamino)ethyl]indol-3-yl]-spiro[1H-2-benzofuran-3,4'-piperidine]-1'-ylmethanone
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C25H28ClN3O2
 2
1
IC50 = 2 nM
   TI
   LI
   LO
   TS
2
Ki = 5.5 nM
   TI
   LI
   LO
   TS
CP0514919
3-[4-(8-chloro-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-1-yl)cyclohexyl]-5-methyl-1,2-oxazole
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C21H23ClN4O
 2
1
IC50 = 2.2 nM
   TI
   LI
   LO
   TS
2
Ki = 0.7 nM
   TI
   LI
   LO
   TS
CP0496262
[(3S)-6-chloro-1-[4-(2-methylphenyl)piperazine-1-carbonyl]-3,4-dihydro-2H-quinolin-3-yl]-pyrrolidin-1-ylmethanone
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C26H31ClN4O2
 2
1
IC50 = 2.4 nM
   TI
   LI
   LO
   TS
2
Ki = 0.6 nM
   TI
   LI
   LO
   TS
CP0512154
[(3S)-6-chloro-1-[4-(2-methylphenyl)piperazine-1-carbonyl]-3,4-dihydro-2H-quinolin-3-yl]-cyclopentylmethanone
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C27H32ClN3O2
 2
1
IC50 = 2.4 nM
   TI
   LI
   LO
   TS
2
Ki = 0.6 nM
   TI
   LI
   LO
   TS
CP0569560
8-ethynyl-1-(1-pyridin-2-ylpiperidin-4-yl)-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine
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C23H23N5
 2
1
IC50 = 2.7 nM
   TI
   LI
   LO
   TS
2
Ki = 0.45 nM
   TI
   LI
   LO
   TS
CP0447818
Balovaptan
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C22H24ClN5O
 2
1
IC50 = 3 nM
   TI
   LI
   LO
   TS
2
Ki = 0.7 nM
   TI
   LI
   LO
   TS
CP0531357
8-chloro-1-(1-pyridin-2-ylpiperidin-4-yl)-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine
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C21H22ClN5
 2
1
IC50 = 3.2 nM
   TI
   LI
   LO
   TS
2
Ki = 1.4 nM
   TI
   LI
   LO
   TS
CP0559965
[6-chloro-1-[4-(2-methylphenyl)piperazine-1-carbonyl]-2,4-dihydroquinazolin-3-yl]-cyclopropylmethanone
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C24H27ClN4O2
 2
1
IC50 = 10 nM
   TI
   LI
   LO
   TS
2
Ki = 3.3 nM
   TI
   LI
   LO
   TS
CP0486121
[6-chloro-1-[4-(2-methylphenyl)piperazine-1-carbonyl]-2,4-dihydroquinazolin-3-yl]-cyclopentylmethanone
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C26H31ClN4O2
 2
1
IC50 = 11 nM
   TI
   LI
   LO
   TS
2
Ki = 1 nM
   TI
   LI
   LO
   TS
CP0552838
1-[6-chloro-1-[4-(2-methylphenyl)piperazine-1-carbonyl]-2,4-dihydroquinazolin-3-yl]-2-methylpropan-1-one
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C24H29ClN4O2
 2
1
IC50 = 11 nM
   TI
   LI
   LO
   TS
2
Ki = 2.6 nM
   TI
   LI
   LO
   TS
CP0543613
8-bromo-1-(1-pyridin-2-ylpiperidin-4-yl)-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine
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C21H22BrN5
 2
1
IC50 = 13 nM
   TI
   LI
   LO
   TS
2
Ki = 0.7 nM
   TI
   LI
   LO
   TS
CP0492303
1-(4-pyridin-2-yloxycyclohexyl)-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine
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C22H24N4O
 2
1
IC50 = 20 nM
   TI
   LI
   LO
   TS
2
Ki = 2.3 nM
   TI
   LI
   LO
   TS
CP0570581
(6-chloro-3-methylsulfonyl-2,4-dihydroquinazolin-1-yl)-[4-(2-methylphenyl)piperazin-1-yl]methanone
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C21H25ClN4O3S
 2
1
IC50 = 20 nM
   TI
   LI
   LO
   TS
2
Ki = 5.3 nM
   TI
   LI
   LO
   TS
CP0531356
3-[4-(5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-1-yl)cyclohexyl]-5-methyl-1,2-oxazole
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C21H24N4O
 2
1
IC50 = 25 nM
   TI
   LI
   LO
   TS
2
Ki = 1.6 nM
   TI
   LI
   LO
   TS
CP0572743
[(3R)-6-chloro-1-[4-(2-methylphenyl)piperazine-1-carbonyl]-3,4-dihydro-2H-quinolin-3-yl]-cyclopentylmethanone
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C27H32ClN3O2
 2
1
IC50 = 25 nM
   TI
   LI
   LO
   TS
2
Ki = 2.3 nM
   TI
   LI
   LO
   TS
CP0190845
8-chloro-5-methyl-1-(1-pyridin-2-ylpiperidin-4-yl)-4,6-dihydro-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine
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C21H23ClN6
 1
1
IC50 = 31 nM
   TI
   LI
   LO
   TS
CP0512179
1-[6-chloro-1-[4-(2-methylphenyl)piperazine-1-carbonyl]-2,4-dihydroquinazolin-3-yl]-2-hydroxyethanone
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C22H25ClN4O3
 2
1
IC50 = 35 nM
   TI
   LI
   LO
   TS
2
Ki = 4 nM
   TI
   LI
   LO
   TS
CP0546885
[7-chloro-4-[4-(2-methylphenyl)piperazine-1-carbonyl]-3,4-dihydro-1H-isoquinolin-2-yl]-cyclopentylmethanone
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C27H32ClN3O2
 2
1
IC50 = 35 nM
   TI
   LI
   LO
   TS
2
Ki = 6 nM
   TI
   LI
   LO
   TS
CP0572741
[6-chloro-1-[4-(2-methylphenyl)piperazine-1-carbonyl]-2,4-dihydroquinazolin-3-yl]-phenylmethanone
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C27H27ClN4O2
 2
1
IC50 = 35 nM
   TI
   LI
   LO
   TS
2
Ki = 3 nM
   TI
   LI
   LO
   TS
CP0546891
(2R)-4-oxo-2-[(3S,4R)-2-oxo-3-[(4S)-2-oxo-4-phenyl-1,3-oxazolidin-3-yl]-4-[(E)-2-phenylethenyl]azetidin-1-yl]-N-[(1S)-1-phenylethyl]-4-(4-piperidin-1-ylpiperidin-1-yl)butanamide
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C42H49N5O5
 2
1
IC50 = 40 nM
   TI
   LI
   LO
   TS
2
Ki = 0.9 nM
   TI
   LI
   LO
   TS
CP0559964
(6-chloro-3,4-dihydro-2H-quinazolin-1-yl)-[4-(2-methylphenyl)piperazin-1-yl]methanone
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C20H23ClN4O
 2
1
IC50 = 40 nM
   TI
   LI
   LO
   TS
2
Ki = 3 nM
   TI
   LI
   LO
   TS
CP0511983
1-[6-chloro-1-[4-(2-methylphenyl)piperazine-1-carbonyl]-2,4-dihydroquinazolin-3-yl]ethanone
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C22H25ClN4O2
 2
1
IC50 = 50 nM
   TI
   LI
   LO
   TS
2
Ki = 6 nM
   TI
   LI
   LO
   TS
CP0563079
(6-chloro-4-methyl-2,3-dihydroquinoxalin-1-yl)-[4-(3-chloropyridin-2-yl)piperazin-1-yl]methanone
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C19H21Cl2N5O
 2
1
IC50 = 55 nM
   TI
   LI
   LO
   TS
2
Ki = 2 nM
   TI
   LI
   LO
   TS
CP0471687
7-chloro-1-(4-pyridin-2-yloxycyclohexyl)-4,5-dihydro-[1,2,4]triazolo[4,3-a]quinoline
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C21H21ClN4O
 2
1
IC50 = 70 nM
   TI
   LI
   LO
   TS
2
Ki = 9 nM
   TI
   LI
   LO
   TS
CP0574295
(6-chloro-3,4-dihydro-2H-quinoxalin-1-yl)-[4-(2-methylphenyl)piperazin-1-yl]methanone
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C20H23ClN4O
 2
1
IC50 = 80 nM
   TI
   LI
   LO
   TS
2
Ki = 4.1 nM
   TI
   LI
   LO
   TS
CP0512193
(6-chloro-3-methyl-2,4-dihydroquinazolin-1-yl)-[4-(2-methylphenyl)piperazin-1-yl]methanone
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C21H25ClN4O
 2
1
IC50 = 85 nM
   TI
   LI
   LO
   TS
2
Ki = 3 nM
   TI
   LI
   LO
   TS
CP0489622
3-[4-(7-chloro-4,5-dihydro-[1,2,4]triazolo[4,3-a]quinolin-1-yl)cyclohexyl]-5-methyl-1,2-oxazole
   Show/Hide
C20H21ClN4O
 2
1
IC50 = 100 nM
   TI
   LI
   LO
   TS
2
Ki = 13 nM
   TI
   LI
   LO
   TS
CP0552856
1-(1-pyridin-2-ylpiperidin-4-yl)-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine
   Show/Hide
C21H23N5
 2
1
IC50 = 117 nM
   TI
   LI
   LO
   TS
2
Ki = 15 nM
   TI
   LI
   LO
   TS
CP0511984
1-[7-chloro-4-[4-(2-methylphenyl)piperazine-1-carbonyl]-3,4-dihydro-1H-isoquinolin-2-yl]-2-methylpropan-1-one
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C25H30ClN3O2
 2
1
IC50 = 135 nM
   TI
   LI
   LO
   TS
2
Ki = 5 nM
   TI
   LI
   LO
   TS
CP0471315
(6-chloro-3,4-dihydro-2H-quinoxalin-1-yl)-[4-(3-chloropyridin-2-yl)piperazin-1-yl]methanone
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C18H19Cl2N5O
 2
1
IC50 = 170 nM
   TI
   LI
   LO
   TS
2
Ki = 6 nM
   TI
   LI
   LO
   TS
CP0511985
[7-chloro-4-[4-(2-methylphenyl)piperazine-1-carbonyl]-3,4-dihydro-1H-isoquinolin-2-yl]-cyclopropylmethanone
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C25H28ClN3O2
 1
1
IC50 = 180 nM
   TI
   LI
   LO
   TS
CP0486505
(6-chloro-3,4-dihydro-2H-quinolin-1-yl)-[4-(2-methylphenyl)piperazin-1-yl]methanone
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C21H24ClN3O
 2
1
IC50 = 200 nM
   TI
   LI
   LO
   TS
2
Ki = 4 nM
   TI
   LI
   LO
   TS
CP0484991
methyl 2-[7-chloro-1-(4-pyridin-2-yloxycyclohexyl)-4,5-dihydro-[1,2,4]triazolo[4,3-a]quinolin-4-yl]acetate
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C24H25ClN4O3
 2
1
IC50 = 220 nM
   TI
   LI
   LO
   TS
2
Ki = 28 nM
   TI
   LI
   LO
   TS
CP0514922
8-ethyl-1-(1-pyridin-2-ylpiperidin-4-yl)-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine
   Show/Hide
C23H27N5
 2
1
IC50 = 252 nM
   TI
   LI
   LO
   TS
2
Ki = 15 nM
   TI
   LI
   LO
   TS
CP0484989
(6-chloro-3,4-dihydro-2H-quinoxalin-1-yl)-(1-pyridin-2-ylpiperidin-4-yl)methanone
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C19H21ClN4O
 2
1
IC50 = 260 nM
   TI
   LI
   LO
   TS
2
Ki = 1.4 nM
   TI
   LI
   LO
   TS
CP0512001
(6-chloro-4-methyl-2,3-dihydroquinoxalin-1-yl)-(1-pyridin-2-ylpiperidin-4-yl)methanone
   Show/Hide
C20H23ClN4O
 2
1
IC50 = 260 nM
   TI
   LI
   LO
   TS
2
Ki = 14 nM
   TI
   LI
   LO
   TS
CP0546894
(6-chloro-3,4-dihydro-2H-quinoxalin-1-yl)-spiro[1H-2-benzofuran-3,4'-piperidine]-1'-ylmethanone
   Show/Hide
C21H22ClN3O2
 2
1
IC50 = 280 nM
   TI
   LI
   LO
   TS
2
Ki = 4 nM
   TI
   LI
   LO
   TS
CP0512003
(6-chloro-4-methyl-2,3-dihydroquinoxalin-1-yl)-[4-(2-methylphenyl)piperazin-1-yl]methanone
   Show/Hide
C21H25ClN4O
 2
1
IC50 = 300 nM
   TI
   LI
   LO
   TS
2
Ki = 7 nM
   TI
   LI
   LO
   TS
CP0573494
(6-chloro-3,4-dihydro-2H-quinoxalin-1-yl)-[4-(2-methylphenyl)piperidin-1-yl]methanone
   Show/Hide
C21H24ClN3O
 2
1
IC50 = 380 nM
   TI
   LI
   LO
   TS
2
Ki = 3 nM
   TI
   LI
   LO
   TS
CP0512176
(7-chloro-2,3,4,5-tetrahydro-1-benzazepin-1-yl)-[4-(2-methylphenyl)piperazin-1-yl]methanone
   Show/Hide
C22H26ClN3O
 2
1
IC50 = 390 nM
   TI
   LI
   LO
   TS
2
Ki = 5 nM
   TI
   LI
   LO
   TS
CP0578723
CHEMBL5085869
   Show/Hide
C23H26N4O2
 1
1
IC50 = 390 nM
   TI
   LI
   LO
   TS
CP0564874
(6-chloro-3,4-dihydro-2H-quinoxalin-1-yl)-[4-(3-methylpyridin-2-yl)piperazin-1-yl]methanone
   Show/Hide
C19H22ClN5O
 2
1
IC50 = 450 nM
   TI
   LI
   LO
   TS
2
Ki = 2 nM
   TI
   LI
   LO
   TS
CP0392030
N-[4-(7-chloro-5-hydroxy-2,3,4,5-tetrahydro-1-benzazepine-1-carbonyl)-3-methylphenyl]-2-methylbenzamide
   Show/Hide
C26H25ClN2O3
 1
1
IC50 = 470 nM
   TI
   LI
   LO
   TS
CP0471169
3-[4-(13-chloro-6,7,9-triazatetracyclo[8.4.0.02,4.05,9]tetradeca-1(10),5,7,11,13-pentaen-8-yl)cyclohexyl]-5-methyl-1,2-oxazole
   Show/Hide
C21H21ClN4O
 2
1
IC50 = 500 nM
   TI
   LI
   LO
   TS
2
Ki = 100 nM
   TI
   LI
   LO
   TS
CP0514921
3-[4-[(2S,4R)-13-chloro-6,7,9-triazatetracyclo[8.4.0.02,4.05,9]tetradeca-1(10),5,7,11,13-pentaen-8-yl]cyclohexyl]-5-methyl-1,2-oxazole
   Show/Hide
C21H21ClN4O
 2
1
IC50 = 635 nM
   TI
   LI
   LO
   TS
2
Ki = 55 nM
   TI
   LI
   LO
   TS
CP0560389
(6-chloro-3,4-dihydro-2H-quinoxalin-1-yl)-[(2R)-2-methyl-4-(3-methylpyridin-2-yl)piperazin-1-yl]methanone
   Show/Hide
C20H24ClN5O
 2
1
IC50 = 750 nM
   TI
   LI
   LO
   TS
2
Ki = 70 nM
   TI
   LI
   LO
   TS
CP0512184
N-[2-chloro-5-[4-(2-methylphenyl)piperazine-1-carbonyl]phenyl]thiophene-2-carboxamide
   Show/Hide
C23H22ClN3O2S
 2
1
IC50 = 800 nM
   TI
   LI
   LO
   TS
2
Ki = 170 nM
   TI
   LI
   LO
   TS
CP0573493
(5-chloro-2,3-dihydroindol-1-yl)-[4-(2-methylphenyl)piperazin-1-yl]methanone
   Show/Hide
C20H22ClN3O
 2
1
IC50 = 880 nM
   TI
   LI
   LO
   TS
2
Ki = 15 nM
   TI
   LI
   LO
   TS
CP0575175
(6-chloro-3,4-dihydro-2H-quinoxalin-1-yl)-[(3S)-3-methyl-4-pyridin-2-ylpiperazin-1-yl]methanone
   Show/Hide
C19H22ClN5O
 2
1
IC50 = 1000 nM
   TI
   LI
   LO
   TS
2
Ki = 62 nM
   TI
   LI
   LO
   TS
CP0514920
7-chloro-1-(1-pyridin-2-ylpiperidin-4-yl)-4,5-dihydro-[1,2,4]triazolo[4,3-a]quinoline
   Show/Hide
C20H20ClN5
 2
1
IC50 = 1400 nM
   TI
   LI
   LO
   TS
2
Ki = 71 nM
   TI
   LI
   LO
   TS
CP0512191
1-[7-chloro-4-[4-(2-methylphenyl)piperazine-1-carbonyl]-2,3-dihydroquinoxalin-1-yl]ethanone
   Show/Hide
C22H25ClN4O2
 2
1
IC50 = 1400 nM
   TI
   LI
   LO
   TS
2
Ki = 13 nM
   TI
   LI
   LO
   TS
CP0574441
(7-chloro-3,4-dihydro-2H-quinoxalin-1-yl)-[4-(2-methylphenyl)piperazin-1-yl]methanone
   Show/Hide
C20H23ClN4O
 2
1
IC50 = 1400 nM
   TI
   LI
   LO
   TS
2
Ki = 560 nM
   TI
   LI
   LO
   TS
CP0486122
3,4-dihydro-2H-quinoxalin-1-yl-[4-(2-methylphenyl)piperazin-1-yl]methanone
   Show/Hide
C20H24N4O
 2
1
IC50 = 2800 nM
   TI
   LI
   LO
   TS
2
Ki = 70 nM
   TI
   LI
   LO
   TS
CP0568276
(6-chloro-3,4-dihydro-2H-quinoxalin-1-yl)-(4-pyridin-2-ylpiperazin-1-yl)methanone
   Show/Hide
C18H20ClN5O
 2
1
IC50 = 6800 nM
   TI
   LI
   LO
   TS
2
Ki = 160 nM
   TI
   LI
   LO
   TS
CP0574435
(4-benzylpiperazin-1-yl)-(6-chloro-3,4-dihydro-2H-quinoxalin-1-yl)methanone
   Show/Hide
C20H23ClN4O
 2
1
IC50 = 8300 nM
   TI
   LI
   LO
   TS
2
Ki = 164 nM
   TI
   LI
   LO
   TS
CP0546884
[6-chloro-1-[4-(2-methylphenyl)piperazine-1-carbonyl]-2,4-dihydroquinazolin-3-yl]-cyclohexylmethanone
   Show/Hide
C27H33ClN4O2
 1
1
Ki = 5 nM
   TI
   LI
   LO
   TS
CP0486504
[6-chloro-1-[4-(2-methylphenyl)piperazine-1-carbonyl]-2,4-dihydroquinazolin-3-yl]-[1-(4-fluorophenyl)cyclopropyl]methanone
   Show/Hide
C30H30ClFN4O2
 1
1
Ki = 23 nM
   TI
   LI
   LO
   TS
CP0484990
13-chloro-8-(4-pyridin-2-yloxycyclohexyl)-6,7,9-triazatetracyclo[8.4.0.02,4.05,9]tetradeca-1(10),5,7,11,13-pentaene
   Show/Hide
C22H21ClN4O
 1
1
Ki = 180 nM
   TI
   LI
   LO
   TS
CP0559208
13-chloro-8-(1-pyridin-2-ylpiperidin-4-yl)-6,7,9-triazatetracyclo[8.4.0.02,4.05,9]tetradeca-1(10),5,7,11,13-pentaene
   Show/Hide
C21H20ClN5
 1
1
Ki = 260 nM
   TI
   LI
   LO
   TS
CP0575174
(6-chloro-3,4-dihydro-2H-quinoxalin-1-yl)-[(3R)-3-methyl-4-pyridin-2-ylpiperazin-1-yl]methanone
   Show/Hide
C19H22ClN5O
 1
1
Ki = 310 nM
   TI
   LI
   LO
   TS
CP0554973
methyl 13-chloro-8-(4-pyridin-2-yloxycyclohexyl)-6,7,9-triazatetracyclo[8.4.0.02,4.05,9]tetradeca-1(10),5,7,11,13-pentaene-4-carboxylate
   Show/Hide
C24H23ClN4O3
 1
1
Ki = 400 nM
   TI
   LI
   LO
   TS
CP0575176
1-[7-fluoro-4-[4-(2-methylphenyl)piperazine-1-carbonyl]-2,3-dihydroquinoxalin-1-yl]ethanone
   Show/Hide
C22H25FN4O2
 1
1
Ki = 440 nM
   TI
   LI
   LO
   TS
CP0489621
3-[4-[(2R,4S)-13-chloro-6,7,9-triazatetracyclo[8.4.0.02,4.05,9]tetradeca-1(10),5,7,11,13-pentaen-8-yl]cyclohexyl]-5-methyl-1,2-oxazole
   Show/Hide
C21H21ClN4O
 1
1
Ki = 570 nM
   TI
   LI
   LO
   TS
CP0480036
7-chloro-4-methoxy-1-(1-pyridin-2-ylpiperidin-4-yl)-[1,2,4]triazolo[4,3-a]quinoxaline
   Show/Hide
C20H19ClN6O
 1
1
Ki = 700 nM
   TI
   LI
   LO
   TS
CP0418699
7-chloro-4,4-dimethyl-1-(1-pyridin-2-ylpiperidin-4-yl)-5H-[1,2,4]triazolo[4,3-a]quinoxaline
   Show/Hide
C21H23ClN6
 1
1
Ki = 800 nM
   TI
   LI
   LO
   TS
CP0553108
1-[7-chloro-4,4-dimethyl-1-(1-pyridin-2-ylpiperidin-4-yl)-[1,2,4]triazolo[4,3-a]quinoxalin-5-yl]ethanone
   Show/Hide
C23H25ClN6O
 1
1
Ki = 2400 nM
   TI
   LI
   LO
   TS
CP0553881
6-chloro-1-(1-pyridin-2-ylpiperidin-4-yl)-3H-[1,2,4]triazolo[4,3-a]benzimidazole
   Show/Hide
C18H17ClN6
 1
1
Ki = 5200 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0055934
(2S)-N-[(2S)-1-[(2-amino-2-oxoethyl)amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-1-[(10R,13S,16S,19S,22S)-13-(2-amino-2-oxoethyl)-16-(3-amino-3-oxopropyl)-19-benzyl-22-[(4-methoxyphenyl)methyl]-12,15,18,21,24-pentaoxo-7,8-dithia-11,14,17,20,23-pentazaspiro[5.19]pentacosane-10-carbonyl]pyrrolidine-2-carboxamide
   Show/Hide
C52H74N14O12S2
 3
1 IC50 = 0.63 nM
2 IC50 = 1.9 nM
3 Ki = 0.39 nM
CP0154510
(4S)-N-[2-(dimethylamino)ethyl]-1-[4-[(2-phenylbenzoyl)amino]benzoyl]spiro[3,5-dihydro-2H-1-benzazepine-4,3'-cyclopentene]-1'-carboxamide
   Show/Hide
C39H40N4O3
 1
1 IC50 = 2 nM
CP0206403
1N-{4-[6-chloro-16-methyl-(12S)-2,10-diazatetracyclo[11.2.1.02,12.04,9]hexadeca-4(9),5,7-trien-10-ylcarbonyl]phenyl}-2-trifluoromethylbenzamide
   Show/Hide
C29H25ClF3N3O2
 1
1 IC50 = 4 nM
CP0041307
(4R)-N-[2-(dimethylamino)ethyl]-1-[4-[(2-fluorobenzoyl)amino]benzoyl]spiro[3,5-dihydro-2H-1-benzazepine-4,3'-cyclopentene]-1'-carboxamide
   Show/Hide
C33H35FN4O3
 1
1 IC50 = 4 nM
CP0197121
3'N-(2-hydroxyethyl)-1-[4-(2-fluorophenylcarboxamido)benzoyl]spiro[2,3,4,5-tetrahydro-1H-benzo[b]azepine-4,1'-(2'-cyclopentene)]-3'-carboxamide
   Show/Hide
C31H30FN3O4
 1
1 IC50 = 4 nM
CP0279457
4-{2-[1-[4-(2-fluorophenylcarboxamido)benzoyl]spiro[2,3,4,5-tetrahydro-1H-benzo[b]azepine-4,1'-(2'-cyclopentene)]-3-ylcarboxamido]ethyl}-1,4-oxazinane
   Show/Hide
C35H37FN4O4
 1
1 IC50 = 4 nM
CP0219489
1N-{4-[6-chloro-16-methyl-(12S)-2,10-diazatetracyclo[11.2.1.02,12.04,9]hexadeca-4(9),5,7-trien-10-ylcarbonyl]phenyl}-2-chlorobenzamide
   Show/Hide
C28H25Cl2N3O2
 1
1 IC50 = 5 nM
CP0056752
3'N-(2-dimethylaminoethyl)-1-[4-(5-fluoro-2-methylphenylcarboxamido)benzoyl]spiro[2,3,4,5-tetrahydro-1H-benzo[b]azepine-4,1'-(2'-cyclopentene)]-3'-carboxamide
   Show/Hide
C34H37FN4O3
 1
1 IC50 = 5 nM
CP0124484
3'N-(2-dimethylaminoethyl)-1-[4-(2-phenylphenylcarboxamido)benzoyl]spiro[2,3,4,5-tetrahydro-1H-benzo[b]azepine-4,1'-(2'-cyclopentene)]-3'-carboxamide
   Show/Hide
C39H40N4O3
 1
1 IC50 = 5 nM
CP0154509
3'N-(3-dimethylaminopropyl)-1-[4-(2-phenylphenylcarboxamido)benzoyl]spiro[2,3,4,5-tetrahydro-1H-benzo[b]azepine-4,1'-(2'-cyclopentene)]-3'-carboxamide
   Show/Hide
C40H42N4O3
 1
1 IC50 = 5 nM
CP0280289
3'N-(3-dimethylaminopropyl)-1-[4-(5-fluoro-2-methylphenylcarboxamido)benzoyl]spiro[2,3,4,5-tetrahydro-1H-benzo[b]azepine-4,1'-(2'-cyclopentene)]-3'-carboxamide
   Show/Hide
C35H39FN4O3
 1
1 IC50 = 5 nM
CP0281438
3'N-(2-hydroxyethyl)-1-[4-(2-phenylphenylcarboxamido)benzoyl]spiro[2,3,4,5-tetrahydro-1H-benzo[b]azepine-4,1'-(2'-cyclopentene)]-3'-carboxamide
   Show/Hide
C37H35N3O4
 1
1 IC50 = 6 nM
CP0289902
methyl 2-[[1-[4-[(5-fluoro-2-methylbenzoyl)amino]benzoyl]spiro[3,5-dihydro-2H-1-benzazepine-4,3'-cyclopentene]-1'-carbonyl]amino]acetate
   Show/Hide
C33H32FN3O5
 1
1 IC50 = 7 nM
CP0304375
3'N-(2-hexahydro-1-pyridinylethyl)-1-[4-(2-fluorophenylcarboxamido)benzoyl]spiro[2,3,4,5-tetrahydro-1H-benzo[b]azepine-4,1'-(2'-cyclopentene)]-3'-carboxamide
   Show/Hide
C36H39FN4O3
 1
1 IC50 = 7 nM
CP0105811
3'N-(2-tetrahydro-1H-1-pyrrolylethyl)-1-[4-(2-fluorophenylcarboxamido)benzoyl]spiro[2,3,4,5-tetrahydro-1H-benzo[b]azepine-4,1'-(2'-cyclopentene)]-3'-carboxamide
   Show/Hide
C35H37FN4O3
 1
1 IC50 = 8 nM
CP0194057
3'N-(2-dimethylaminoethyl)-1-[4-(2-fluorophenylcarboxamido)benzoyl]spiro[2,3,4,5-tetrahydro-1H-benzo[b]azepine-4,1'-(2'-cyclopentene)]-3'-carboxamide
   Show/Hide
C33H35FN4O3
 1
1 IC50 = 8 nM
CP0042892
3'N-(2-hexahydro-1-pyridinylethyl)-1-[4-(5-fluoro-2-methylphenylcarboxamido)benzoyl]spiro[2,3,4,5-tetrahydro-1H-benzo[b]azepine-4,1'-(2'-cyclopentene)]-3'-carboxamide
   Show/Hide
C37H41FN4O3
 2
1 IC50 = 10 nM
2 IC50 = 16 nM
CP0304035
3'N-(2-tetrahydro-1H-1-pyrrolylethyl)-1-[4-(5-fluoro-2-methylphenylcarboxamido)benzoyl]spiro[2,3,4,5-tetrahydro-1H-benzo[b]azepine-4,1'-(2'-cyclopentene)]-3'-carboxamide
   Show/Hide
C36H39FN4O3
 1
1 IC50 = 19 nM
CP0106503
3-chloro-4-[16-methyl-(12S)-2,10-diazatetracyclo[11.2.1.02,12.04,9]hexadeca-4(9),5,7-trien-10-ylcarbonyl]-1-(2-phenylphenylcarboxamido)benzene
   Show/Hide
C34H30ClN3O2
 1
1 IC50 = 24 nM
CP0196743
1N-{4-[6-chloro-16-methyl-(12S)-2,10-diazatetracyclo[11.2.1.02,12.04,9]hexadeca-4(9),5,7-trien-10-ylcarbonyl]phenyl}-2-(4-methylphenyl)benzamide
   Show/Hide
C35H32ClN3O2
 1
1 IC50 = 24 nM
CP0154159
2-[1-[4-(2-phenylphenylcarboxamido)benzoyl]spiro[2,3,4,5-tetrahydro-1H-benzo[b]azepine-4,1'-(2'-cyclopentene)]-3-ylcarboxamido]acetic acid
   Show/Hide
C37H33N3O5
 1
1 IC50 = 24 nM
CP0062116
1N-{4-[6-chloro-16-ethyl-(12S)-2,10-diazatetracyclo[11.2.1.02,12.04,9]hexadeca-4(9),5,7-trien-10-ylcarbonyl]phenyl}-2-chlorobenzamide
   Show/Hide
C29H27Cl2N3O2
 1
1 IC50 = 35 nM
CP0104567
1N-{4-[6-chloro-16-methyl-(12S)-2,10-diazatetracyclo[11.2.1.02,12.04,9]hexadeca-4(9),5,7-trien-10-ylcarbonyl]phenyl}-2-fluorobenzamide
   Show/Hide
C28H25ClFN3O2
 1
1 IC50 = 68 nM
CP0040044
3-chloro-4-(10,11-dihydro-5H-benzo[e]pyrrolo[1,2-a][1,4]diazepin-10-ylcarbonyl)-1-(5-fluoro-2-methylphenylcarboxamido)benzene
   Show/Hide
C27H21ClFN3O2
 4
1 IC50 = 150 nM
2 IC50 = 180 nM
3 IC50 = 230 nM
4 Ki = 44 nM
CP0365138
2-Methyl-N-[4-(2,3,4,5-tetrahydro-benzo[b][1,4]diazepine-1-carbonyl)-phenyl]-benzamide
   Show/Hide
C24H23N3O2
 1
1 IC50 = 250 nM
CP0177122
(2S)-5-amino-2-{[(2S)-1-{[(4R,7S,10S,13S,16R)-13-[(2S)-butan-2-yl]-7-(carbamoylmethyl)-16-[(4-ethoxyphenyl)methyl]-10-[(1R)-1-hydroxyethyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentaazacycloicosan-4-yl]carbonyl}pyrrolidin-2-yl]formamido}-N-(carbamoylmethyl)pentanamide
   Show/Hide
C43H67N11O12S2
 2
1 Ki = 0.15 nM
2 Ki = 4.7 nM
CP0244529
[6-chloro-1-[2-(dimethylamino)ethyl]indol-3-yl]-spiro[1H-2-benzofuran-3,4'-piperidine]-1'-ylmethanone
   Show/Hide
C25H28ClN3O2
 1
1 Ki = 1 nM
CP0162813
(2S)-1-[(2R,3S)-5-chloro-3-(2-chlorophenyl)-1-(3,4-dimethoxybenzenesulfonyl)-3-hydroxy-2,3-dihydro-1H-indole-2-carbonyl]-pyrrolidine-2-carboxamide
   Show/Hide
C28H27Cl2N3O7S
 1
1 Ki = 2 nM
CP0246508
(1-benzyl-2-methylindol-3-yl)-spiro[1H-2-benzofuran-3,4'-piperidine]-1'-ylmethanone
   Show/Hide
C29H28N2O2
 1
1 Ki = 2 nM
CP0441646
(6-chloro-1H-indol-3-yl)-spiro[1H-2-benzofuran-3,4'-piperidine]-1'-ylmethanone
   Show/Hide
C21H19ClN2O2
 1
1 Ki = 4 nM
CP0260717
2-phenyl-N-[4-(2,3,4,5-tetrahydro-1-benzazepine-1-carbonyl)phenyl]benzamide
   Show/Hide
C30H26N2O2
 1
1 Ki = 14.1 nM
CP0195952
(2S,4R)-1-((R)-5-chloro-1-(2,4-dimethoxyphenylsulfonyl)-3-(2-methoxyphenyl)-2-oxoindolin-3-yl)-4-hydroxy-N,N-dimethylpyrrolidine-2-carboxamide
   Show/Hide
C30H32ClN3O8S
 1
1 Ki = 22 nM
CP0117986
(2S)-1-[(4R,7S,10S,13S,16S,19R)-19-amino-7-(2-amino-2-oxoethyl)-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]-N-[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]pyrrolidine-2-carboxamide
   Show/Hide
C43H66N12O12S2
 2
1 Ki = 34.9 nM
2 Ki = 120 nM
CP0308266
(2-ethoxynaphthalen-1-yl)-spiro[1H-2-benzofuran-3,4'-piperidine]-1'-ylmethanone
   Show/Hide
C25H25NO3
 1
1 Ki = 81 nM
CP0219136
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-carboxamide
   Show/Hide
C32H35N7O4
 2
1 Ki = 113 nM
2 Ki > 1000 nM
CP0219211
(4-benzyl-4-hydroxypiperidin-1-yl)-(1-benzyl-2-methylindol-3-yl)methanone
   Show/Hide
C29H30N2O2
 1
1 Ki = 295 nM
CP0053149
N-[3-[4-[4-(2-oxo-3,4-dihydroquinolin-1-yl)piperidine-1-carbonyl]phenoxy]propyl]acetamide
   Show/Hide
C26H31N3O4
 1
1 Ki = 350 nM
CP0083253
(5H,11H-benzo[e]pyrrolo[1,2-a][1,4]diazepin-10-yl)-[2-chloro-4-(3-methyl-pyrazol-1-yl)-phenyl]-methanone
   Show/Hide
C23H19ClN4O
 1
1 Ki = 465 nM
CP0214389
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]acetamide
   Show/Hide
C31H27F3N4O6
 1
1 Ki = 1258.93 nM
CP0106713
(4-benzyl-4-hydroxypiperidin-1-yl)-(2-ethoxynaphthalen-1-yl)methanone
   Show/Hide
C25H27NO3
 1
1 Ki = 2830 nM
CP0041007
1-(1-(4-(1-acetylpiperidin-4-yloxy)-2-methoxybenzoyl)piperidin-4-yl)-1H-benzo[d][1,3]oxazin-2(4H)-one
   Show/Hide
C28H33N3O6
 2
1 Ki = 3200 nM
2 Ki < 1995.26 nM
Clinical Information about the Protein
Target 1 ( Vasopressin V1a receptor (V1AR) )
Target Type Successful Target
Disease 10 Target-related Diseases  10
1 Euvolemic hyponatremia [ICD-11: 5C72]
2 Diabetic complication [ICD-11: 5A2Y]
3 Hyponatraemia [ICD-11: 5C72]
4 Autism spectrum disorder [ICD-11: 6A02]
5 Sepsis [ICD-11: 1G40-1G41]
6 Atopic dermatitis [ICD-11: EA80]
7 Anxiety disorder [ICD-11: 6B00-6B0Z]
8 Dysmenorrhea [ICD-11: GA34.3]
9 Cardiac disease [ICD-11: BA00-BE2Z]
10 Female sexual arousal dysfunction [ICD-11: HA01.1]
Approved Drug(s) 4 Approved Drugs  4
1 Conivaptan Approved
Euvolemic hyponatremia
2 Desmopressin Approved
Diabetic complication
3 Mozavaptan Approved
Hyponatraemia
4 Oxytocin Approved
Autism spectrum disorder
Clinical Trial Drug(s) 5 Clinical Trial Drugs  5
1 FE-202158 Phase 2
Sepsis
2 PMX-53 Phase 2
Atopic dermatitis
3 SRX-246 Phase 2
Anxiety disorder
4 SSR149415 Phase 2
Anxiety disorder
5 SRX-251 Phase 1
Dysmenorrhea
Discontinued Drug(s) 3 Discontinued Drugs  3
1 OPC-21268 Discontinued in Phase 2
Cardiac disease
2 PF-3274167 Discontinued in Phase 1
Female sexual arousal dysfunction
3 JTV-605 Terminated
Dysmenorrhea