| Reaction Details |
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 | Report a problem with these data |
| Target | Gonadotropin-releasing hormone receptor |
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| Ligand | BDBM50548486 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_2022368 (CHEMBL4676181) |
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| IC50 | 10.0±n/a nM |
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| 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 Chem63:11854-11881 (2020) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| Gonadotropin-releasing hormone receptor |
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| Name: | Gonadotropin-releasing hormone receptor |
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| Synonyms: | GNRHR | GNRHR_HUMAN | GRHR | GnRH receptor | GnRH-R | Gonadotropin releasing hormone 1 (GnRHR1) | Gonadotropin-releasing hormone receptor | Gonadotropin-releasing hormone receptor (GnRH) |
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| Type: | Enzyme |
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| Mol. Mass.: | 37749.45 |
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| Organism: | Homo sapiens (Human) |
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| Description: | P30968 |
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| Residue: | 328 |
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| Sequence: | MANSASPEQNQNHCSAINNSIPLMQGNLPTLTLSGKIRVTVTFFLFLLSATFNASFLLKL
QKWTQKKEKGKKLSRMKLLLKHLTLANLLETLIVMPLDGMWNITVQWYAGELLCKVLSYL
KLFSMYAPAFMMVVISLDRSLAITRPLALKSNSKVGQSMVGLAWILSSVFAGPQLYIFRM
IHLADSSGQTKVFSQCVTHCSFSQWWHQAFYNFFTFSCLFIIPLFIMLICNAKIIFTLTR
VLHQDPHELQLNQSKNNIPRARLKTLKMTVAFATSFTVCWTPYYVLGIWYWFDPEMLNRL
SDPVNHFFFLFAFLNPCFDPLIYGYFSL
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| BDBM50548486 |
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| n/a |
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| Name | BDBM50548486 |
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| Synonyms: | CHEMBL4741994 |
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| Type | Small organic molecule |
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| Emp. Form. | C31H31ClFN3O4S |
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| Mol. Mass. | 596.112 |
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| SMILES | CC(=O)N1CCC2(CC1)C(CC=C)N(c1ccc(cc21)C(=O)NCc1ccccc1Cl)S(=O)(=O)c1ccc(F)cc1 |
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| Structure | 
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