Target
Vasopressin V1a receptor
Ligand
BDBM50114031
Substrate
n/a
Meas. Tech.
ChEMBL_772742 (CHEMBL1837354)
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 
Target
Name:
Vasopressin V1a receptor
Synonyms:
Vasopressin receptor | Vasopressin V1a receptor | AVPR V1a | Antidiuretic hormone receptor 1a | V1aR | VASOPRESSIN V1A | Vascular/hepatic-type arginine vasopressin receptor | Vasopressin V1 receptor | V1AR_HUMAN | AVPR1A | AVPR1
Type:
Receptor
Mol. Mass.:
46820.18
Organism:
Human
Description:
P37288
Residue:
418
Sequence:
MRLSAGPDAGPSGNSSPWWPLATGAGNTSREAEALGEGNGPPRDVRNEELAKLEIAVLAVTFAVAVLGNSSVLLALHRTPRKTSRMHLFIRHLSLADLAVAFFQVLPQMCWDITYRFRGPDWLCRVVKHLQVFGMFASAYMLVVMTADRYIAVCHPLKTLQQPARRSRLMIAAAWVLSFVLSTPQYFVFSMIEVNNVTKARDCWATFIQPWGSRAYVTWMTGGIFVAPVVILGTCYGFICYNIWCNVRGKTASRQSKGAEQAGVAFQKGFLLAPCVSSVKSISRAKIRTVKMTFVIVTAYIVCWAPFFIIQMWSVWDPMSVWTESENPTITITALLGSLNSCCNPWIYMFFSGHLLQDCVQSFPCCQNMKEKFNKEDTDSMSRRQTFYSNNRSPTNSTGMWKDSPKSSKSIKFIPVST
  
Inhibitor
Name:
BDBM50114031
Synonyms:
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 | (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 | Relcovaptan | CHEMBL419667
Type:
Small organic molecule
Emp. Form.:
TBD
Mol. Mass.:
TBD
SMILES:
TBD
Structure:
Search PDB for entries with ligand similarity: