Reaction Details |
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Target | Melanocortin receptor 5 |
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Ligand | BDBM50157314 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_306506 (CHEMBL828111) |
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IC50 | 2400±n/a nM |
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Citation | Palucki, BL; Park, MK; Nargund, RP; Ye, Z; Sebhat, IK; Pollard, PG; Kalyani, RN; Tang, R; Macneil, T; Weinberg, DH; Vongs, A; Rosenblum, CI; Doss, GA; Miller, RR; Stearns, RA; Peng, Q; Tamvakopoulos, C; McGowan, E; Martin, WJ; Metzger, JM; Shepherd, CA; Strack, AM; Macintyre, DE; Van der Ploeg, LH; Patchett, AA Discovery of (2S)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-4-methyl-2-piperazinecarboxamide (MB243), a potent and selective melanocortin subtype-4 receptor agonist. Bioorg Med Chem Lett15:171-5 (2004) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Melanocortin receptor 5 |
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Name: | Melanocortin receptor 5 |
Synonyms: | MC-2 | MC5-R | MC5R | MC5R_HUMAN | Melanocortin MC5 | Melanocortin receptor (M4 and M5) | Melanocortin receptor 5 | Melanocortin receptor 5 (MC5R) |
Type: | Enzyme |
Mol. Mass.: | 36612.92 |
Organism: | Homo sapiens (Human) |
Description: | P33032 |
Residue: | 325 |
Sequence: | MNSSFHLHFLDLNLNATEGNLSGPNVKNKSSPCEDMGIAVEVFLTLGVISLLENILVIGA
IVKNKNLHSPMYFFVCSLAVADMLVSMSSAWETITIYLLNNKHLVIADAFVRHIDNVFDS
MICISVVASMCSLLAIAVDRYVTIFYALRYHHIMTARRSGAIIAGIWAFCTGCGIVFILY
SESTYVILCLISMFFAMLFLLVSLYIHMFLLARTHVKRIAALPGASSARQRTSMQGAVTV
TMLLGVFTVCWAPFFLHLTLMLSCPQNLYCSRFMSHFNMYLILIMCNSVMDPLIYAFRSQ
EMRKTFKEIICCRGFRIACSFPRRD
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BDBM50157314 |
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n/a |
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Name | BDBM50157314 |
Synonyms: | (S)-4-Methyl-piperazine-2-carboxylic acid [(R)-2-(4-tert-butylcarbamoyl-4-cyclohexyl-piperidin-1-yl)-1-(4-fluoro-benzyl)-2-oxo-ethyl]-amide | CHEMBL368876 |
Type | Small organic molecule |
Emp. Form. | C31H48FN5O3 |
Mol. Mass. | 557.7429 |
SMILES | CN1CCN[C@@H](C1)C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C |
Structure |
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