Reaction Details |
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Target | Vasopressin V1a receptor |
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Ligand | BDBM50354894 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_772742 (CHEMBL1837354) |
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IC50 | 6.7±n/a nM |
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Citation | Johnson, PS; Ryckmans, T; Bryans, J; Beal, DM; Dack, KN; Feeder, N; Harrison, A; Lewis, M; Mason, HJ; Mills, J; Newman, J; Pasquinet, C; Rawson, DJ; Roberts, LR; Russell, R; Spark, D; Stobie, A; Underwood, TJ; Ward, R; Wheeler, S Discovery of PF-184563, a potent and selective V1a antagonist for the treatment of dysmenorrhoea. The influence of compound flexibility on microsomal stability. Bioorg Med Chem Lett21:5684-7 (2011) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Vasopressin V1a receptor |
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Name: | Vasopressin V1a receptor |
Synonyms: | AVPR V1a | AVPR1 | AVPR1A | Antidiuretic hormone receptor 1a | V1AR_HUMAN | V1aR | VASOPRESSIN V1A | Vascular/hepatic-type arginine vasopressin receptor | Vasopressin V1 receptor | Vasopressin V1a receptor | Vasopressin receptor |
Type: | Receptor |
Mol. Mass.: | 46820.18 |
Organism: | Homo sapiens (Human) |
Description: | P37288 |
Residue: | 418 |
Sequence: | MRLSAGPDAGPSGNSSPWWPLATGAGNTSREAEALGEGNGPPRDVRNEELAKLEIAVLAV
TFAVAVLGNSSVLLALHRTPRKTSRMHLFIRHLSLADLAVAFFQVLPQMCWDITYRFRGP
DWLCRVVKHLQVFGMFASAYMLVVMTADRYIAVCHPLKTLQQPARRSRLMIAAAWVLSFV
LSTPQYFVFSMIEVNNVTKARDCWATFIQPWGSRAYVTWMTGGIFVAPVVILGTCYGFIC
YNIWCNVRGKTASRQSKGAEQAGVAFQKGFLLAPCVSSVKSISRAKIRTVKMTFVIVTAY
IVCWAPFFIIQMWSVWDPMSVWTESENPTITITALLGSLNSCCNPWIYMFFSGHLLQDCV
QSFPCCQNMKEKFNKEDTDSMSRRQTFYSNNRSPTNSTGMWKDSPKSSKSIKFIPVST
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BDBM50354894 |
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n/a |
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Name | BDBM50354894 |
Synonyms: | CHEMBL1837037 |
Type | Small organic molecule |
Emp. Form. | C21H23ClN6 |
Mol. Mass. | 394.901 |
SMILES | CN1Cc2nnc(C3CCN(CC3)c3ccccn3)n2-c2ccc(Cl)cc2C1 |
Structure |
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