Reaction Details |
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Target | Gonadotropin-releasing hormone receptor |
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Ligand | BDBM50244135 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_554183 (CHEMBL963640) |
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IC50 | 14±n/a nM |
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Citation | Pelletier, JC; Chengalvala, M; Cottom, J; Feingold, I; Garrick, L; Green, D; Hauze, D; Huselton, C; Jetter, J; Kao, W; Kopf, GS; Lundquist, JT; Mann, C; Mehlmann, J; Rogers, J; Shanno, L; Wrobel, J 2-phenyl-4-piperazinylbenzimidazoles: orally active inhibitors of the gonadotropin releasing hormone (GnRH) receptor. Bioorg Med Chem16:6617-40 (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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BDBM50244135 |
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n/a |
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Name | BDBM50244135 |
Synonyms: | 4-{4-[2-(4-tert-Butyl-phenyl)-1H-benzoimidazol-4-yl]-piperazin-1-ylmethyl}-1,3-dihydro-benzoimidazole-2-thione | CHEMBL459659 |
Type | Small organic molecule |
Emp. Form. | C29H32N6S |
Mol. Mass. | 496.67 |
SMILES | CC(C)(C)c1ccc(cc1)-c1nc2c(cccc2[nH]1)N1CCN(Cc2cccc3[nH]c(=S)[nH]c23)CC1 |
Structure |
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