Reaction Details |
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Target | Gonadotropin-releasing hormone receptor |
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Ligand | BDBM50260759 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_495151 (CHEMBL1008930) |
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Ki | 1.2±n/a nM |
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Citation | Chen, C; Wu, D; Guo, Z; Xie, Q; Reinhart, GJ; Madan, A; Wen, J; Chen, T; Huang, CQ; Chen, M; Chen, Y; Tucci, FC; Rowbottom, M; Pontillo, J; Zhu, YF; Wade, W; Saunders, J; Bozigian, H; Struthers, RS Discovery of sodium R-(+)-4-{2-[5-(2-fluoro-3-methoxyphenyl)-3-(2-fluoro-6-[trifluoromethyl]benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenylethylamino}butyrate (elagolix), a potent and orally available nonpeptide antagonist of the human gonadotropin-releasing hormone receptor. J Med Chem51:7478-85 (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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BDBM50260759 |
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n/a |
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Name | BDBM50260759 |
Synonyms: | (R)-4-(2-(3-(2-fluoro-6-(trifluoromethyl)benzyl)-5-(2-fluoro-3-methoxyphenyl)-2,6-dioxo-2,3-dihydropyrimidin-1(6H)-yl)-1-phenylethylamino)butanoic acid | (R)-4-{2-[5-(2-Fluoro-3-methoxyphenyl)-3-(2-fluoro-6-[trifluoromethyl]benzyl)-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenylethylamino}butyric Acid | CHEMBL509075 |
Type | Small organic molecule |
Emp. Form. | C31H28F5N3O5 |
Mol. Mass. | 617.5631 |
SMILES | COc1cccc(c1F)-c1cn(Cc2c(F)cccc2C(F)(F)F)c(=O)n(C[C@H](NCCCC(O)=O)c2ccccc2)c1=O |r| |
Structure |
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