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Target
Melanocyte-stimulating hormone receptor
Ligand
BDBM50253748
Substrate
n/a
Meas. Tech.
ChEMBL_538609 (CHEMBL1027399)
EC50
69±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 
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:
BDBM50253748
Synonyms:
(2S)-N-((1R)-1-[(4-Fluorophenyl)methyl]-2-{(2S)-4-[(1S)-2-(methylamino)-1-(2-naphthalenylmethyl)-2-oxoethyl]-3-oxo-2-propyl-1-piperazinyl}-2-oxoethyl)-2-piperidinecarboxamide | CHEMBL448410
Type:
Small organic molecule
Emp. Form.:
C36H44FN5O4
Mol. Mass.:
629.7641
SMILES:
CCC[C@@H]1N(CCN([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)C1=O)C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H]1CCCCN1 |r|
Structure:
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