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Target
Gonadotropin-releasing hormone receptor
Ligand
BDBM50256836
Substrate
n/a
Meas. Tech.
ChEMBL_562460 (CHEMBL1010963)
IC50
1.8±n/a nM
Citation
 Pelletier, JC; Chengalvala, MV; Cottom, JE; Feingold, IB; Green, DM; Hauze, DB; Huselton, CA; Jetter, JW; Kopf, GS; Lundquist, JT; Magolda, RL; Mann, CW; Mehlmann, JF; Rogers, JF; Shanno, LK; Adams, WR; Tio, CO; Wrobel, JE Discovery of 6-({4-[2-(4-tert-butylphenyl)-1H-benzimidazol-4-yl]piperazin-1-yl}methyl)quinoxaline (WAY-207024): an orally active antagonist of the gonadotropin releasing hormone receptor (GnRH-R). J Med Chem 52:2148-52 (2009) [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:
BDBM50256836
Synonyms:
7-((4-(2-(4-tert-butylphenyl)-1H-benzo[d]imidazol-4-yl)piperazin-1-yl)methyl)pyrido[2,3-b]pyrazine-2,3(1H,4H)-dione | CHEMBL473807
Type:
Small organic molecule
Emp. Form.:
C29H31N7O2
Mol. Mass.:
509.6021
SMILES:
CC(C)(C)c1ccc(cc1)-c1nc2c(cccc2[nH]1)N1CCN(Cc2cnc3[nH]c(=O)c(=O)[nH]c3c2)CC1
Structure:
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