Reaction Details |
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Target | Gonadotropin-releasing hormone receptor |
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Ligand | BDBM50104565 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEBML_71456 |
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IC50 | 4.4±n/a nM |
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Citation | Ashton, WT; Sisco, RM; Kieczykowski, GR; Yang, YT; Yudkovitz, JB; Cui, J; Mount, GR; Ren, RN; Wu, TJ; Shen, X; Lyons, KA; Mao, AH; Carlin, JR; Karanam, BV; Vincent, SH; Cheng, K; Goulet, MT Orally bioavailable, indole-based nonpeptide GnRH receptor antagonists with high potency and functional activity. Bioorg Med Chem Lett11:2597-602 (2001) [PubMed] |
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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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BDBM50104565 |
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n/a |
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Name | BDBM50104565 |
Synonyms: | 2-{2-(3,5-Dimethyl-phenyl)-3-[(S)-1-methyl-2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indol-5-yl}-1-(4-ethanesulfonyl-piperazin-1-yl)-2-methyl-propan-1-one | CHEMBL312995 |
Type | Small organic molecule |
Emp. Form. | C38H51N5O3S |
Mol. Mass. | 657.908 |
SMILES | CCS(=O)(=O)N1CCN(CC1)C(=O)C(C)(C)c1ccc2[nH]c(c([C@H](C)CNCCCCc3ccncc3)c2c1)-c1cc(C)cc(C)c1 |
Structure |
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