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TargetMelanocortin receptor 3
LigandBDBM50224185
Substrate/Competitorn/a
Meas. Tech.ChEMBL_450506 (CHEMBL900803)
Ki 230±n/a nM
Citation Chen, CJiang, WTucci, FTran, JAFleck, BAHoare, SRJoppa, MMarkison, SWen, JSai, YJohns, MMadan, AChen, TChen, CWMarinkovic, DArellano, MSaunders, JFoster, 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
More Info.:Get all data from this article,  Assay Method
 
Melanocortin receptor 3
Name:Melanocortin receptor 3
Synonyms:MC3-R | MC3R | MC3R_HUMAN | Melanocortin MC3 | Melanocortin receptor (M3 and M4)
Type:Enzyme
Mol. Mass.:36044.86
Organism:Homo sapiens (Human)
Description:P41968
Residue:323
Sequence:
MNASCCLPSVQPTLPNGSEHLQAPFFSNQSSSAFCEQVFIKPEVFLSLGIVSLLENILVI
LAVVRNGNLHSPMYFFLCSLAVADMLVSVSNALETIMIAIVHSDYLTFEDQFIQHMDNIF
DSMICISLVASICNLLAIAVDRYVTIFYALRYHSIMTVRKALTLIVAIWVCCGVCGVVFI
VYSESKMVIVCLITMFFAMMLLMGTLYVHMFLFARLHVKRIAALPPADGVAPQQHSCMKG
AVTITILLGVFIFCWAPFFLHLVLIITCPTNPYCICYTAHFNTYLVLIMCNSVIDPLIYA
FRSLELRNTFREILCGCNGMNLG
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50224185
n/a
NameBDBM50224185
Synonyms:1-{2-[(1S)-(methylaminoacetamido)-2-methylpropyl]-4-methylphenyl}-4-[(2R)-methyl-3-(2-fluoro-4-chlorophenyl)propionyl]piperazine | CHEMBL240571 | N-((S)-1-(2-(4-((R)-3-(4-chloro-2-fluorophenyl)-2-methylpropanoyl)piperazin-1-yl)-5-methylphenyl)-2-methylpropyl)-2-(methylamino)acetamide
TypeSmall organic molecule
Emp. Form.C28H38ClFN4O2
Mol. Mass.517.078
SMILESCNCC(=O)N[C@@H](C(C)C)c1cc(C)ccc1N1CCN(CC1)C(=O)[C@H](C)Cc1ccc(Cl)cc1F |r|
Structure
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