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TargetVasopressin V1a receptor
LigandBDBM50114031
Substrate/Competitorn/a
Meas. Tech.ChEMBL_772742
IC50 13±n/a nM
Citation Johnson PSRyckmans TBryans JBeal DMDack KNFeeder NHarrison ALewis MMason HJMills JNewman JPasquinet CRawson DJRoberts LRRussell RSpark DStobie AUnderwood TJWard RWheeler 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 Lett 21:5684-7 (2011) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Vasopressin V1a receptor
Name:Vasopressin V1a receptor
Synonyms:AVPR V1a | AVPR1 | AVPR1A | Antidiuretic hormone receptor 1a | V1aR | VASOPRESSIN V1A | Vascular/hepatic-type arginine vasopressin receptor | Vasopressin V1 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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  Blast E-value cutoff:
BDBM50114031
n/a
NameBDBM50114031
Synonyms:(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 | (S)-1-((2R,3S)-5-chloro-3-(2-chlorophenyl)-1-(3,4-dimethoxyphenylsulfonyl)-3-hydroxyindoline-2-carbonyl)pyrrolidine-2-carboxamide | 1-[5-Chloro-3-(2-chloro-phenyl)-1-(3,4-dimethoxy-benzenesulfonyl)-3-hydroxy-2,3-dihydro-1H-indole-2-carbonyl]-pyrrolidine-2-carboxylic acid amide | CHEMBL419667 | Relcovaptan
TypeSmall organic molecule
Emp. Form.C28H27Cl2N3O7S
Mol. Mass.620.501
SMILESCOc1ccc(cc1OC)S(=O)(=O)N1[C@@H](C(=O)N2CCC[C@H]2C(N)=O)[C@](O)(c2cc(Cl)ccc12)c1ccccc1Cl |r|
Structure
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