Reaction Details Report a problem with these data
Target
Gonadotropin-releasing hormone receptor
Ligand
BDBM50261251
Substrate
n/a
Meas. Tech.
ChEMBL_625917 (CHEMBL1115143)
IC50
10±n/a nM
Citation
Vera, MD; Lundquist, JT; Chengalvala, MV; Cottom, JE; Feingold, IB; Garrick, LM; Green, DM; Hauze, DB; Mann, CW; Mehlmann, JF; Rogers, JF; Shanno, L; Wrobel, JE; Pelletier, JC Synthesis and biological evaluation of piperazinyl heterocyclic antagonists of the gonadotropin releasing hormone (GnRH) receptor. Bioorg Med Chem Lett 20:2512-5 (2010) [PubMed] Article
More Info.:
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:
BDBM50261251
Synonyms:
2-(4-tert-butylphenyl)-4-(4-((2-ethyl-4-methyl-1H-imidazol-5-yl)methyl)piperazin-1-yl)-1H-benzo[d]imidazole | 2-(4-tert-butylphenyl)-4-(4-((2-ethyl-5-methyl-1H-imidazol-4-yl)methyl)piperazin-1-yl)-1H-benzo[d]imidazole | CHEMBL468565
Type:
Small organic molecule
Emp. Form.:
C28H36N6
Mol. Mass.:
456.6256
SMILES:
CCc1nc(C)c(CN2CCN(CC2)c2cccc3[nH]c(nc23)-c2ccc(cc2)C(C)(C)C)[nH]1