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Target
Gonadotropin-releasing hormone receptor
Ligand
BDBM50127187
Substrate
n/a
Meas. Tech.
ChEMBL_71588 (CHEMBL684202)
Ki
11±n/a nM
Citation
 Zhu, YF; Guo, Z; Gross, TD; Gao, Y; Connors, PJ; Struthers, RS; Xie, Q; Tucci, FC; Reinhart, GJ; Wu, D; Saunders, J; Chen, C Design and structure-activity relationships of 2-alkyl-3-aminomethyl-6-(3-methoxyphenyl)-7-methyl-8-(2-fluorobenzyl)imidazolo[1,2-a]pyrimid-5-ones as potent GnRH receptor antagonists. J Med Chem 46:1769-72 (2003) [PubMed]  Article 
Target
Name:
Gonadotropin-releasing hormone receptor
Synonyms:
GNRHR | GNRHR_HUMAN | GRHR | GnRH receptor | GnRH-R | Gonadotropin releasing hormone 1 (GnRHR1) | Gonadotropin-releasing hormone receptor | Gonadotropin-releasing hormone receptor (GnRH)
Type:
Enzyme
Mol. Mass.:
37749.45
Organism:
Homo sapiens (Human)
Description:
P30968
Residue:
328
Sequence:
MANSASPEQNQNHCSAINNSIPLMQGNLPTLTLSGKIRVTVTFFLFLLSATFNASFLLKLQKWTQKKEKGKKLSRMKLLLKHLTLANLLETLIVMPLDGMWNITVQWYAGELLCKVLSYLKLFSMYAPAFMMVVISLDRSLAITRPLALKSNSKVGQSMVGLAWILSSVFAGPQLYIFRMIHLADSSGQTKVFSQCVTHCSFSQWWHQAFYNFFTFSCLFIIPLFIMLICNAKIIFTLTRVLHQDPHELQLNQSKNNIPRARLKTLKMTVAFATSFTVCWTPYYVLGIWYWFDPEMLNRLSDPVNHFFFLFAFLNPCFDPLIYGYFSL
  
Inhibitor
Name:
BDBM50127187
Synonyms:
2-tert-Butyl-8-(2-fluoro-benzyl)-6-(3-methoxy-phenyl)-7-methyl-3-[(methyl-pyridin-2-ylmethyl-amino)-methyl]-8H-imidazo[1,2-a]pyrimidin-5-one | CHEMBL49297
Type:
Small organic molecule
Emp. Form.:
C33H36FN5O2
Mol. Mass.:
553.6696
SMILES:
COc1cccc(c1)-c1c(C)n(Cc2ccccc2F)c2nc(c(CN(C)Cc3ccccn3)n2c1=O)C(C)(C)C
Structure:
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