Reaction Details |
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Target | Gonadotropin-releasing hormone receptor |
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Ligand | BDBM50347982 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_756129 (CHEMBL1804385) |
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IC50 | 0.32±n/a nM |
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Citation | Miwa, K; Hitaka, T; Imada, T; Sasaki, S; Yoshimatsu, M; Kusaka, M; Tanaka, A; Nakata, D; Furuya, S; Endo, S; Hamamura, K; Kitazaki, T Discovery of 1-{4-[1-(2,6-difluorobenzyl)-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl]phenyl}-3-methoxyurea (TAK-385) as a potent, orally active, non-peptide antagonist of the human gonadotropin-releasing hormone receptor. J Med Chem54:4998-5012 (2011) [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_RAT | GnRH receptor | GnRH-R | Gnrhr |
Type: | PROTEIN |
Mol. Mass.: | 37767.60 |
Organism: | Rattus norvegicus |
Description: | ChEMBL_1335047 |
Residue: | 327 |
Sequence: | MANNASLEQDQNHCSAINNSIPLTQGKLPTLTLSGKIRVTVTFFLFLLSTAFNASFLVKL
QRWTQKRKKGKKLSRMKVLLKHLTLANLLETLIVMPLDGMWNITVQWYAGEFLCKVLSYL
KLFSMYAPAFMMVVISLDRSLAVTQPLAVQSKSKLERSMTSLAWILSIVFAGPQLYIFRM
IYLADGSGPAVFSQCVTHCSFPQWWHEAFYNFFTFSCLFIIPLLIMLICNAKIIFALTRV
LHQDPRKLQLNQSKNNIPRARLRTLKMTVAFGTSFVICWTPYYVLGIWYWFDPEMLNRVS
EPVNHFFFLFAFLNPCFDPLIYGYFSL
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BDBM50347982 |
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n/a |
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Name | BDBM50347982 |
Synonyms: | CHEMBL1800159 |
Type | Small organic molecule |
Emp. Form. | C29H27F2N7O5S |
Mol. Mass. | 623.63 |
SMILES | CONC(=O)Nc1ccc(cc1)-c1sc2n(Cc3c(F)cccc3F)c(=O)n(-c3ccc(OC)nn3)c(=O)c2c1CN(C)C |
Structure |
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