Reaction Details Report a problem with these data
Target
Melanocortin receptor 3
Ligand
BDBM50027432
Substrate
n/a
Meas. Tech.
ChEMBL_624017 (CHEMBL1116903)
EC50
5.4±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
More Info.:
Target
Name:
Melanocortin receptor 3
Synonyms:
MC3-R | MC3R | MC3R_HUMAN | Melanocortin MC3 | Melanocortin receptor (M3 and M4)
Type:
Enzyme
Mol. Mass.:
36044.86
Organism:
Homo sapiens (Human)
Description:
P41968
Residue:
323
Sequence:
MNASCCLPSVQPTLPNGSEHLQAPFFSNQSSSAFCEQVFIKPEVFLSLGIVSLLENILVILAVVRNGNLHSPMYFFLCSLAVADMLVSVSNALETIMIAIVHSDYLTFEDQFIQHMDNIFDSMICISLVASICNLLAIAVDRYVTIFYALRYHSIMTVRKALTLIVAIWVCCGVCGVVFIVYSESKMVIVCLITMFFAMMLLMGTLYVHMFLFARLHVKRIAALPPADGVAPQQHSCMKGAVTITILLGVFIFCWAPFFLHLVLIITCPTNPYCICYTAHFNTYLVLIMCNSVIDPLIYAFRSLELRNTFREILCGCNGMNLG
Inhibitor
Name:
BDBM50027432
Synonyms:
CHEMBL2372570
Type:
Small organic molecule
Emp. Form.:
C50H69N15O9
Mol. Mass.:
1024.178
SMILES:
CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC2=NC=NC2)NC1=O)C(N)=O |r,c:68,t:66|