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Target
Melanocortin receptor 4
Ligand
BDBM50315683
Substrate
n/a
Meas. Tech.
ChEMBL_624014 (CHEMBL1108859)
EC50
365±n/a nM
Citation
 Lansdell, MI; Hepworth, D; Calabrese, A; Brown, AD; Blagg, J; Burring, DJ; Wilson, P; Fradet, D; Brown, TB; Quinton, F; Mistry, N; Tang, K; Mount, N; Stacey, P; Edmunds, N; Adams, C; Gaboardi, S; Neal-Morgan, S; Wayman, C; Cole, S; Phipps, J; Lewis, M; Verrier, H; Gillon, V; Feeder, N; Heatherington, A; Sultana, S; Haughie, S; Martin, SW; Sudworth, M; Tweedy, S Discovery of a selective small-molecule melanocortin-4 receptor agonist with efficacy in a pilot study of sexual dysfunction in humans. J Med Chem 53:3183-97 (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:
BDBM50315683
Synonyms:
((3S,4R)-4-(2,4-difluorophenyl)-1-methylpyrrolidin-3-yl)((3S,4R,5R)-4-(4-fluorophenyl)-4-hydroxy-3,5-dimethylpiperidin-1-yl)methanone | CHEMBL1093858
Type:
Small organic molecule
Emp. Form.:
C25H29F3N2O2
Mol. Mass.:
446.5052
SMILES:
C[C@H]1CN(C[C@@H](C)[C@]1(O)c1ccc(F)cc1)C(=O)[C@@H]1CN(C)C[C@H]1c1ccc(F)cc1F |r|
Structure:
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