Reaction Details |
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Target | Gonadotropin-releasing hormone receptor |
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Ligand | BDBM50162032 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_302845 (CHEMBL827890) |
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Ki | 13±n/a nM |
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Citation | Tucci, FC; Zhu, YF; Struthers, RS; Guo, Z; Gross, TD; Rowbottom, MW; Acevedo, O; Gao, Y; Saunders, J; Xie, Q; Reinhart, GJ; Liu, XJ; Ling, N; Bonneville, AK; Chen, T; Bozigian, H; Chen, C 3-[(2R)-Amino-2-phenylethyl]-1-(2,6-difluorobenzyl)-5-(2-fluoro-3-methoxyphenyl)- 6-methylpyrimidin-2,4-dione (NBI 42902) as a potent and orally active antagonist of the human gonadotropin-releasing hormone receptor. Design, synthesis, and in vitro and in vivo characterization. J Med Chem48:1169-78 (2005) [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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BDBM50162032 |
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n/a |
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Name | BDBM50162032 |
Synonyms: | 1-(2,6-Difluoro-benzyl)-5-(2,3-dihydro-benzo[1,4]dioxin-6-yl)-6-methyl-3-((R)-2-methylamino-2-phenyl-ethyl)-1H-pyrimidine-2,4-dione | CHEMBL425864 |
Type | Small organic molecule |
Emp. Form. | C29H27F2N3O4 |
Mol. Mass. | 519.5392 |
SMILES | CN[C@@H](Cn1c(=O)c(c(C)n(Cc2c(F)cccc2F)c1=O)-c1ccc2OCCOc2c1)c1ccccc1 |
Structure |
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