Reaction Details |
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Target | Melanocortin receptor 4 |
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Ligand | BDBM50169440 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_310830 (CHEMBL833019) |
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EC50 | 238±n/a nM |
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Citation | Ye, Z; Guo, L; Barakat, KJ; Pollard, PG; Palucki, BL; Sebhat, IK; Bakshi, RK; Tang, R; Kalyani, RN; Vongs, A; Chen, AS; Chen, HY; Rosenblum, CI; MacNeil, T; Weinberg, DH; Peng, Q; Tamvakopoulos, C; Miller, RR; Stearns, RA; Cashen, DE; Martin, WJ; Metzger, JM; Strack, AM; MacIntyre, DE; Van der Ploeg, LH; Patchett, AA; Wyvratt, MJ; Nargund, RP Discovery and activity of (1R,4S,6R)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-2-methyl-2-azabicyclo[2.2.2]octane-6-carboxamide (3, RY764), a potent and selective melanocortin subtype-4 receptor agonist. Bioorg Med Chem Lett15:3501-5 (2005) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Melanocortin receptor 4 |
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Name: | Melanocortin receptor 4 |
Synonyms: | MC4-R | MC4R | MC4R_HUMAN | Melanocortin MC4 | Melanocortin receptor 4 (MC-4) | Melanocortin receptor 4 (MC4-R) | Melanocortin receptor 4 (MC4R) |
Type: | Enzyme |
Mol. Mass.: | 36949.50 |
Organism: | Homo sapiens (Human) |
Description: | P32245 |
Residue: | 332 |
Sequence: | MVNSTHRGMHTSLHLWNRSSYRLHSNASESLGKGYSDGGCYEQLFVSPEVFVTLGVISLL
ENILVIVAIAKNKNLHSPMYFFICSLAVADMLVSVSNGSETIVITLLNSTDTDAQSFTVN
IDNVIDSVICSSLLASICSLLSIAVDRYFTIFYALQYHNIMTVKRVGIIISCIWAACTVS
GILFIIYSDSSAVIICLITMFFTMLALMASLYVHMFLMARLHIKRIAVLPGTGAIRQGAN
MKGAITLTILIGVFVVCWAPFFLHLIFYISCPQNPYCVCFMSHFNLYLILIMCNSIIDPL
IYALRSQELRKTFKEIICCYPLGGLCDLSSRY
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BDBM50169440 |
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n/a |
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Name | BDBM50169440 |
Synonyms: | (1S,4R,6S)-2-Aza-bicyclo[2.2.2]octane-6-carboxylic acid [(R)-2-(4-tert-butylcarbamoyl-4-cyclohexyl-piperidin-1-yl)-1-(4-fluoro-benzyl)-2-oxo-ethyl]-amide | CHEMBL188966 |
Type | Small organic molecule |
Emp. Form. | C33H49FN4O3 |
Mol. Mass. | 568.7656 |
SMILES | CC(C)(C)NC(=O)C1(CCN(CC1)C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H]1C[C@H]2CC[C@@H]1NC2)C1CCCCC1 |
Structure |
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