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Target
Gonadotropin-releasing hormone receptor
Ligand
BDBM50548486
Substrate
n/a
Meas. Tech.
ChEMBL_2022368 (CHEMBL4676181)
IC50
10.0±n/a nM
Citation
 Panknin, O; Wagenfeld, A; Bone, W; Bender, E; Nowak-Reppel, K; Fernández-Montalván, AE; Nubbemeyer, R; Bäurle, S; Ring, S; Schmees, N; Prien, O; Schäfer, M; Friedrich, C; Zollner, TM; Steinmeyer, A; Mueller, T; Langer, G Discovery and Characterization of BAY 1214784, an Orally Available Spiroindoline Derivative Acting as a Potent and Selective Antagonist of the Human Gonadotropin-Releasing Hormone Receptor as Proven in a First-In-Human Study in Postmenopausal Women. J Med Chem 63:11854-11881 (2020) [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:
BDBM50548486
Synonyms:
CHEMBL4741994
Type:
Small organic molecule
Emp. Form.:
C31H31ClFN3O4S
Mol. Mass.:
596.112
SMILES:
CC(=O)N1CCC2(CC1)C(CC=C)N(c1ccc(cc21)C(=O)NCc1ccccc1Cl)S(=O)(=O)c1ccc(F)cc1
Structure:
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