Reaction Details |
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Target | Gonadotropin-releasing hormone receptor |
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Ligand | BDBM50166451 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_552282 (CHEMBL995612) |
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Ki | 0.9±n/a nM |
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Citation | Chen, C; Chen, Y; Pontillo, J; Guo, Z; Huang, CQ; Wu, D; Madan, A; Chen, T; Wen, J; Xie, Q; Tucci, FC; Rowbottom, M; Zhu, YF; Wade, W; Saunders, J; Bozigian, H; Struthers, RS Potent and orally bioavailable zwitterion GnRH antagonists with low CYP3A4 inhibitory activity. Bioorg Med Chem Lett18:3301-5 (2008) [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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BDBM50166451 |
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n/a |
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Name | BDBM50166451 |
Synonyms: | (R)-1-(2-fluoro-6-(methylsulfonyl)benzyl)-3-(2-amino-2-phenylethyl)-5-(2-fluoro-3-methoxyphenyl)pyrimidine-2,4(1H,3H)-dione | 3-((R)-2-Amino-2-phenyl-ethyl)-1-(2-fluoro-6-methanesulfonyl-benzyl)-5-(2-fluoro-3-methoxy-phenyl)-1H-pyrimidine-2,4-dione | CHEMBL364914 |
Type | Small organic molecule |
Emp. Form. | C27H25F2N3O5S |
Mol. Mass. | 541.566 |
SMILES | COc1cccc(c1F)-c1cn(Cc2c(F)cccc2S(C)(=O)=O)c(=O)n(C[C@H](N)c2ccccc2)c1=O |r| |
Structure |
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