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Target
Gonadotropin-releasing hormone receptor
Ligand
BDBM50098391
Substrate
n/a
Meas. Tech.
ChEMBL_71735 (CHEMBL680258)
IC50
4±n/a nM
Citation
DeVita, RJ; Walsh, TF; Young, JR; Jiang, J; Ujjainwalla, F; Toupence, RB; Parikh, M; Huang, SX; Fair, JA; Goulet, MT; Wyvratt, MJ; Lo, JL; Ren, N; Yudkovitz, JB; Yang, YT; Cheng, K; Cui, J; Mount, G; Rohrer, SP; Schaeffer, JM; Rhodes, L; Drisko, JE; McGowan, E; MacIntyre, DE; Vincent, S; Carlin, JR; Cameron, J; Smith, RG A potent, nonpeptidyl 1H-quinolone antagonist for the gonadotropin-releasing hormone receptor. J Med Chem 44:917-22 (2001) [PubMed] Article
More Info.:
Target
Name:
Gonadotropin-releasing hormone receptor
Synonyms:
GNRHR_RAT | GnRH receptor | GnRH-R | Gnrhr
Type:
PROTEIN
Mol. Mass.:
37767.60
Organism:
Rattus norvegicus
Description:
ChEMBL_1335047
Residue:
327
Sequence:
MANNASLEQDQNHCSAINNSIPLTQGKLPTLTLSGKIRVTVTFFLFLLSTAFNASFLVKLQRWTQKRKKGKKLSRMKVLLKHLTLANLLETLIVMPLDGMWNITVQWYAGEFLCKVLSYLKLFSMYAPAFMMVVISLDRSLAVTQPLAVQSKSKLERSMTSLAWILSIVFAGPQLYIFRMIYLADGSGPAVFSQCVTHCSFPQWWHEAFYNFFTFSCLFIIPLLIMLICNAKIIFALTRVLHQDPRKLQLNQSKNNIPRARLRTLKMTVAFGTSFVICWTPYYVLGIWYWFDPEMLNRVSEPVNHFFFLFAFLNPCFDPLIYGYFSL
Inhibitor
Name:
BDBM50098391
Synonyms:
(S)-4-(2-(azetidin-2-yl)ethoxy)-7-chloro-2-oxo-N-(pyrimidin-4-yl)-3-(3,4,5-trimethylphenyl)-1,2-dihydroquinoline-6-carboxamide | 4-((S)-2-Azetidin-2-yl-ethoxy)-7-chloro-2-oxo-3-(3,4,5-trimethyl-phenyl)-1,2-dihydro-quinoline-6-carboxylic acid pyrimidin-4-ylamide | 4-(2-Azetidin-2-yl-ethoxy)-7-chloro-2-oxo-3-(3,4,5-trimethyl-phenyl)-1,2-dihydro-quinoline-6-carboxylic acid pyrimidin-4-ylamide | CHEMBL120432
Type:
Small organic molecule
Emp. Form.:
C28H28ClN5O3
Mol. Mass.:
518.007
SMILES:
Cc1cc(cc(C)c1C)-c1c(OCC[C@@H]2CCN2)c2cc(C(=O)Nc3ccncn3)c(Cl)cc2[nH]c1=O |r|