Reaction Details |
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Target | Melanocortin receptor 4 |
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Ligand | BDBM50224177 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_450504 (CHEMBL900801) |
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IC50 | 280±n/a nM |
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Citation | Chen, C; Jiang, W; Tucci, F; Tran, JA; Fleck, BA; Hoare, SR; Joppa, M; Markison, S; Wen, J; Sai, Y; Johns, M; Madan, A; Chen, T; Chen, CW; Marinkovic, D; Arellano, M; Saunders, J; Foster, AC Discovery of 1-[2-[(1S)-(3-dimethylaminopropionyl)amino-2-methylpropyl]-4-methylphenyl]-4-[(2R)-methyl-3-(4-chlorophenyl)-propionyl]piperazine as an orally active antagonist of the melanocortin-4 receptor for the potential treatment of cachexia. J Med Chem50:5249-52 (2007) [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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BDBM50224177 |
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n/a |
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Name | BDBM50224177 |
Synonyms: | 1-{2-[(1S)-(aminopropionyl)amino-2-methylpropyl]-4-methylphenyl}-4-[(2R)-methyl-3-(4-chlorophenyl)propionyl]piperazine | 3-amino-N-((S)-1-(2-(4-((R)-3-(4-chlorophenyl)-2-methylpropanoyl)piperazin-1-yl)-5-methylphenyl)-2-methylpropyl)propanamide | CHEMBL240364 |
Type | Small organic molecule |
Emp. Form. | C28H39ClN4O2 |
Mol. Mass. | 499.088 |
SMILES | CC(C)[C@H](NC(=O)CCN)c1cc(C)ccc1N1CCN(CC1)C(=O)[C@H](C)Cc1ccc(Cl)cc1 |r| |
Structure |
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