Reaction Details Report a problem with these data
Target
Melanocyte-stimulating hormone receptor
Ligand
BDBM50253658
Substrate
n/a
Meas. Tech.
ChEMBL_538609 (CHEMBL1027399)
Ki
16832±n/a nM
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 Chem 51:6055-66 (2008) [PubMed] Article
More Info.:
Target
Name:
Melanocyte-stimulating hormone receptor
Synonyms:
MC1-R | MC1R | MSH-R | MSHR | MSHR_HUMAN | Melanocortin MC1 | Melanocortin receptor (M1 and M4) | Melanocortin receptor 1 (MC-1) | Melanocortin receptor 1 (MC1-R) | Melanocortin receptor 1 (MC1R)
Type:
Enzyme
Mol. Mass.:
34717.23
Organism:
Homo sapiens (Human)
Description:
Q01726
Residue:
317
Sequence:
MAVQGSQRRLLGSLNSTPTAIPQLGLAANQTGARCLEVSISDGLFLSLGLVSLVENALVVATIAKNRNLHSPMYCFICCLALSDLLVSGSNVLETAVILLLEAGALVARAAVLQQLDNVIDVITCSSMLSSLCFLGAIAVDRYISIFYALRYHSIVTLPRARRAVAAIWVASVVFSTLFIAYYDHVAVLLCLVVFFLAMLVLMAVLYVHMLARACQHAQGIARLHKRQRPVHQGFGLKGAVTLTILLGIFFLCWGPFFLHLTLIVLCPEHPTCGCIFKNFNLFLALIICNAIIDPLIYAFHSQELRRTLKEVLTCSW
Inhibitor
Name:
BDBM50253658
Synonyms:
2-[4-[2-Amino-3-(4-fluoro-phenyl)-propionyl]-3-(2-dimethylaminoethyl)-2-oxo-piperazin-1-yl]-N-methyl-3-naphthalen-2-yl-propionamide | CHEMBL468252
Type:
Small organic molecule
Emp. Form.:
C31H38FN5O3
Mol. Mass.:
547.6635
SMILES:
CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN([C@@H](CCN(C)C)C1=O)C(=O)[C@H](N)Cc1ccc(F)cc1 |r|