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Target
Melanocortin receptor 5
Ligand
BDBM50157321
Substrate
n/a
Meas. Tech.
ChEMBL_310467 (CHEMBL834411)
EC50
840±n/a nM
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 Lett 15:171-5 (2004) [PubMed]  Article 
Target
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:
MNSSFHLHFLDLNLNATEGNLSGPNVKNKSSPCEDMGIAVEVFLTLGVISLLENILVIGAIVKNKNLHSPMYFFVCSLAVADMLVSMSSAWETITIYLLNNKHLVIADAFVRHIDNVFDSMICISVVASMCSLLAIAVDRYVTIFYALRYHHIMTARRSGAIIAGIWAFCTGCGIVFILYSESTYVILCLISMFFAMLFLLVSLYIHMFLLARTHVKRIAALPGASSARQRTSMQGAVTVTMLLGVFTVCWAPFFLHLTLMLSCPQNLYCSRFMSHFNMYLILIMCNSVMDPLIYAFRSQEMRKTFKEIICCRGFRIACSFPRRD
  
Inhibitor
Name:
BDBM50157321
Synonyms:
(R)-4-Methyl-piperazine-2-carboxylic acid [(R)-2-(4-tert-butylcarbamoyl-4-cyclohexyl-piperidin-1-yl)-1-(4-fluoro-benzyl)-2-oxo-ethyl]-amide; dihydrochloride | CHEMBL2145453
Type:
Small organic molecule
Emp. Form.:
C36H52F7N5O7
Mol. Mass.:
799.8162
SMILES:
OC(=O)C(F)(F)F.OC(=O)C(F)(F)F.CCN1CCN[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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