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Target
Melanocortin receptor 4
Ligand
BDBM50329959
Substrate
n/a
Meas. Tech.
ChEMBL_675992 (CHEMBL1272930)
IC50
0.43±n/a nM
Citation
 He, S; Ye, Z; Dobbelaar, PH; Bakshi, RK; Hong, Q; Dellureficio, JP; Sebhat, IK; Guo, L; Liu, J; Jian, T; Lai, Y; Franklin, CL; Reibarkh, M; Holmes, MA; Weinberg, DH; MacNeil, T; Tang, R; Tamvakopoulos, C; Peng, Q; Miller, RR; Stearns, RA; Chen, HY; Chen, AS; Strack, AM; Fong, TM; Wyvratt, MJ; Nargund, RP Discovery of highly potent and efficacious MC4R agonists with spiroindane N-Me-1,2,4-triazole privileged structures for the treatment of obesity. Bioorg Med Chem Lett 20:6524-32 (2010) [PubMed]  Article 
Target
Name:
Melanocortin receptor 4
Synonyms:
MC4-R | MC4R | MC4R_HUMAN | Melanocortin MC4 | Melanocortin receptor 4 (MC-4) | Melanocortin receptor 4 (MC4-R) | Melanocortin receptor 4 (MC4R)
Type:
Enzyme
Mol. Mass.:
36949.50
Organism:
Homo sapiens (Human)
Description:
P32245
Residue:
332
Sequence:
MVNSTHRGMHTSLHLWNRSSYRLHSNASESLGKGYSDGGCYEQLFVSPEVFVTLGVISLLENILVIVAIAKNKNLHSPMYFFICSLAVADMLVSVSNGSETIVITLLNSTDTDAQSFTVNIDNVIDSVICSSLLASICSLLSIAVDRYFTIFYALQYHNIMTVKRVGIIISCIWAACTVSGILFIIYSDSSAVIICLITMFFTMLALMASLYVHMFLMARLHIKRIAVLPGTGAIRQGANMKGAITLTILIGVFVVCWAPFFLHLIFYISCPQNPYCVCFMSHFNLYLILIMCNSIIDPLIYALRSQELRKTFKEIICCYPLGGLCDLSSRY
  
Inhibitor
Name:
BDBM50329959
Synonyms:
(6-chloro-5-methyl-3-(2-(1-methyl-1H-1,2,4-triazol-5-yl)propan-2-yl)-2,3-dihydrospiro[indene-1,4'-piperidine]-1'-yl)((1R,2R)-2-(2,4-difluorophenyl)-4-(methyl(tetrahydro-2H-pyran-4-yl)amino)cyclopentyl)methanone | CHEMBL1269576
Type:
Small organic molecule
Emp. Form.:
C38H48ClF2N5O2
Mol. Mass.:
680.27
SMILES:
CN(C1C[C@H]([C@@H](C1)c1ccc(F)cc1F)C(=O)N1CCC2(C[C@@H](c3cc(C)c(Cl)cc23)C(C)(C)c2ncnn2C)CC1)C1CCOCC1 |r|
Structure:
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