Reaction Details |
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Target | Gonadotropin-releasing hormone receptor |
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Ligand | BDBM50256834 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_562459 (CHEMBL1010962) |
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IC50 | 7.4±n/a nM |
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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 Chem52:2148-52 (2009) [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 |
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: | MANSASPEQNQNHCSAINNSIPLMQGNLPTLTLSGKIRVTVTFFLFLLSATFNASFLLKL
QKWTQKKEKGKKLSRMKLLLKHLTLANLLETLIVMPLDGMWNITVQWYAGELLCKVLSYL
KLFSMYAPAFMMVVISLDRSLAITRPLALKSNSKVGQSMVGLAWILSSVFAGPQLYIFRM
IHLADSSGQTKVFSQCVTHCSFSQWWHQAFYNFFTFSCLFIIPLFIMLICNAKIIFTLTR
VLHQDPHELQLNQSKNNIPRARLKTLKMTVAFATSFTVCWTPYYVLGIWYWFDPEMLNRL
SDPVNHFFFLFAFLNPCFDPLIYGYFSL
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BDBM50256834 |
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n/a |
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Name | BDBM50256834 |
Synonyms: | 7-((4-(2-(4-tert-butylphenyl)-1H-benzo[d]imidazol-4-yl)piperazin-1-yl)methyl)-1-methylquinoxaline-2,3(1H,4H)-dione | CHEMBL513998 |
Type | Small organic molecule |
Emp. Form. | C31H34N6O2 |
Mol. Mass. | 522.6407 |
SMILES | Cn1c2cc(CN3CCN(CC3)c3cccc4[nH]c(nc34)-c3ccc(cc3)C(C)(C)C)ccc2[nH]c(=O)c1=O |
Structure |
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