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Target
Melanocyte-stimulating hormone receptor
Ligand
BDBM50315688
Substrate
n/a
Meas. Tech.
ChEMBL_624018 (CHEMBL1116904)
EC50
>5010±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:
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:
BDBM50315688
Synonyms:
((3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidin-3-yl)((3S,4R,5R)-4-(2,6-difluorophenyl)-4-hydroxy-3,5-dimethylpiperidin-1-yl)methanone | CHEMBL1092550
Type:
Small organic molecule
Emp. Form.:
C28H34F4N2O2
Mol. Mass.:
506.5754
SMILES:
C[C@H]1CN(C[C@@H](C)[C@]1(O)c1c(F)cccc1F)C(=O)[C@@H]1CN(C[C@H]1c1ccc(F)cc1F)C(C)(C)C |r|
Structure:
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