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Target
Gonadotropin-releasing hormone receptor
Ligand
BDBM50244211
Substrate
n/a
Meas. Tech.
ChEMBL_554183 (CHEMBL963640)
IC50
9.4±n/a nM
Citation
 Pelletier, JC; Chengalvala, M; Cottom, J; Feingold, I; Garrick, L; Green, D; Hauze, D; Huselton, C; Jetter, J; Kao, W; Kopf, GS; Lundquist, JT; Mann, C; Mehlmann, J; Rogers, J; Shanno, L; Wrobel, J 2-phenyl-4-piperazinylbenzimidazoles: orally active inhibitors of the gonadotropin releasing hormone (GnRH) receptor. Bioorg Med Chem 16:6617-40 (2008) [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:
BDBM50244211
Synonyms:
6-((4-(2-(4-tert-butylphenyl)-1H-benzo[d]imidazol-4-yl)piperazin-1-yl)methyl)quinoxaline-2,3(1H,4H)-dione | 6-{4-[2-(4-tert-Butyl-phenyl)-1H-benzoimidazol-4-yl]-piperazin-1-ylmethyl}-1,4-dihydro-quinoxaline-2,3-dione | CHEMBL459215
Type:
Small organic molecule
Emp. Form.:
C30H32N6O2
Mol. Mass.:
508.6141
SMILES:
CC(C)(C)c1ccc(cc1)-c1nc2c(cccc2[nH]1)N1CCN(Cc2ccc3[nH]c(=O)c(=O)[nH]c3c2)CC1
Structure:
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