Target
Gonadotropin-releasing hormone receptor
Ligand
BDBM50225093
Substrate
n/a
Meas. Tech.
ChEMBL_458546 (CHEMBL942804)
IC50
216±n/a nM
Citation
 Arnould, JCDelouvrié, BBoutron, PDossetter, AGFoote, KMHamon, AHancox, UHarris, CSHutton, MLamorlette, MMatusiak, Z Synthesis and structure-activity relationships of thieno[2,3-b]pyrroles as antagonists of the GnRH receptor. Bioorg Med Chem Lett 17:6448-54 (2007) [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:
BDBM50225093
Synonyms:
1-(7-aza-bicyclo[2.2.1]heptan-7-yl)-2-(5-(3,5-dimethylphenyl)-4-(2-(4-(4-methoxypiperidine-1-carbonyl)piperidin-1-yl)ethyl)-6H-thieno[2,3-b]pyrrol-2-yl)-2-methylpropan-1-one | CHEMBL250389
Type:
Small organic molecule
Emp. Form.:
C38H52N4O3S
Mol. Mass.:
644.909
SMILES:
COC1CCN(CC1)C(=O)C1CCN(CCc2c([nH]c3sc(cc23)C(C)(C)C(=O)N2C3CCC2CC3)-c2cc(C)cc(C)c2)CC1 |THB:27:29:31.32:34.35|
Structure:
Search PDB for entries with ligand similarity: