Reaction Details |
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Target | Melanocortin receptor 4 |
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Ligand | BDBM50253737 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_538611 (CHEMBL1027401) |
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EC50 | 37±n/a nM |
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Citation | Tian, X; Switzer, AG; Derose, SA; Mishra, RK; Solinsky, MG; Mumin, RN; Ebetino, FH; Jayasinghe, LR; Webster, ME; Colson, AO; Crossdoersen, D; Pinney, BB; Farmer, JA; Dowty, ME; Obringer, CM; Cruze, CA; Burklow, ML; Suchanek, PM; Dong, L; Dirr, MK; Sheldon, RJ; Wos, JA Discovery of orally bioavailable 1,3,4-trisubstituted 2-oxopiperazine-based melanocortin-4 receptor agonists as potential antiobesity agents. J Med Chem51:6055-66 (2008) [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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BDBM50253737 |
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n/a |
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Name | BDBM50253737 |
Synonyms: | CHEMBL453300 | N-((R)-3-(4-Fluorophenyl)-1-((S)-4-((S)-1-(methylamino)-3-(naphthalen-2-yl)-1-oxopropan-2-yl)-3-oxo-2-propylpiperazin-1-yl)-1-oxopropan-2-yl)thiazole-4-carboxamide |
Type | Small organic molecule |
Emp. Form. | C34H36FN5O4S |
Mol. Mass. | 629.744 |
SMILES | CCC[C@@H]1N(CCN([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)C1=O)C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1cscn1 |r| |
Structure |
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