Ki Summary

Reaction Details

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Target

Vasopressin V1b receptor

Ligand

BDBM50299343

Substrate

n/a

1.3±n/a nM

Comments

PDSP_2325

Citation

Serradeil-Le Gal, C; Wagnon, J; Simiand, J; Griebel, G; Lacour, C; Guillon, G; Barberis, C; Brossard, G; Soubrié, P; Nisato, D; Pascal, M; Pruss, R; Scatton, B; Maffrand, JP; Le Fur, G Characterization of (2S,4R)-1-[5-chloro-1-[(2,4-dimethoxyphenyl)sulfonyl]-3-(2-methoxy-phenyl)-2-oxo-2,3-dihydro-1H-indol-3-yl]-4-hydroxy-N,N-dimethyl-2-pyrrolidine carboxamide (SSR149415), a selective and orally active vasopressin V1b receptor antagonist. J Pharmacol Exp Ther 300:1122-30 (2002) [PubMed] Article

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Target

Name:

Vasopressin V1b receptor

Synonyms:

Avpr1b | V1BR_RAT | VASOPRESSIN V1B | Vasopressin V1b receptor | Vasopressin receptor

Type:

Enzyme Catalytic Domain

Mol. Mass.:

47104.48

Organism:

RAT

Description:

VASOPRESSIN V1B AVPR1B RAT::P48974

Residue:

425

Sequence:

MNSEPSWTATPSPGGTLPVPNATTPWLGRDEELAKVEIGILATVLVLATGGNLAVLLTLGRHGHKRSRMHLFVLHLALTDLGVALFQVLPQLLWDITYRFQGSDLLCRAVKYLQVLSMFASTYMLLAMTLDRYLAVCHPLRSLRQPSQSTYPLIAAPWLLAAILSLPQVFIFSLREVIQGSGVLDCWADFYFSWGPRAYITWTTMAIFVLPVAVLSACYGLICHEIYKNLKVKTQAGREERRGWRTWDKSSSSAVATAATRGLPSRVSSISTISRAKIRTVKMTFVIVLAYIACWAPFFSVQMWSVWDENAPNEDSTNVAFTISMLLGNLSSCCNPWIYMGFNSRLLPRSLSHHACCTGSKPQVHRQLSTSSLTSRRTTLLTHACGSPTLRLSLNLSLRAKPRPAGSLKDLEQVDGEATMETSIF

Inhibitor

Name:

BDBM50299343

Synonyms:

(2S,4R)-1-((R)-5-chloro-1-(2,4-dimethoxyphenylsulfonyl)-3-(2-methoxyphenyl)-2-oxoindolin-3-yl)-4-hydroxy-N,N-dimethylpyrrolidine-2-carboxamide | (2S,4R)-1-[5-Chloro-1-[(2,4-dimethoxyphenyl)sulfonyl]-3-(2-methoxy-phenyl)-2-oxo-2,3-dihydro-1H-indol-3-yl]-4-hydroxy-N,Ndimethyl-2-pyrrolidine carboxamide | CHEMBL582857 | SR-149415 | SSR149415

Type:

Small organic molecule

Emp. Form.:

C30H32ClN3O8S

Mol. Mass.:

630.108

SMILES:

COc1ccc(c(OC)c1)S(=O)(=O)N1C(=O)[C@@](N2C[C@H](O)C[C@H]2C(=O)N(C)C)(c2cc(Cl)ccc12)c1ccccc1OC |r|

Structure: