Reaction Details Report a problem with these data
Target
Melanocortin receptor 4
Ligand
BDBM50252899
Substrate
n/a
Meas. Tech.
ChEMBL_1365574 (CHEMBL3297283)
EC50
0.280000±n/a nM
Citation
Haslach, EM; Huang, H; Dirain, M; Debevec, G; Geer, P; Santos, RG; Giulianotti, MA; Pinilla, C; Appel, JR; Doering, SR; Walters, MA; Houghten, RA; Haskell-Luevano, C Identification of tetrapeptides from a mixture based positional scanning library that can restore nM full agonist function of the L106P, I69T, I102S, A219V, C271Y, and C271R human melanocortin-4 polymorphic receptors (hMC4Rs). J Med Chem 57:4615-28 (2014) [PubMed] Article
More Info.:
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:
BDBM50252899
Synonyms:
Ac-His-DPhe(pCl)-Arg-Trp-NH2 | CHEMBL491870
Type:
Small organic molecule
Emp. Form.:
C34H42ClN11O5
Mol. Mass.:
720.221
SMILES:
CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O |r,wU:4.3,14.14,26.27,wD:37.38,(16.37,-31.04,;16.37,-32.58,;15.05,-33.35,;17.71,-33.36,;19.04,-32.59,;19.04,-31.04,;20.38,-30.27,;21.79,-30.9,;22.82,-29.76,;22.05,-28.42,;20.54,-28.74,;20.38,-33.36,;20.38,-34.9,;21.71,-32.59,;23.05,-33.36,;23.05,-34.89,;24.37,-35.67,;25.72,-34.9,;27.05,-35.67,;27.04,-37.21,;28.38,-37.99,;25.71,-37.98,;24.38,-37.21,;24.38,-32.59,;24.38,-31.05,;25.71,-33.35,;27.05,-32.59,;27.05,-31.05,;28.38,-30.28,;28.38,-28.74,;29.72,-27.97,;29.72,-26.44,;28.39,-25.67,;31.06,-25.66,;28.38,-33.36,;28.38,-34.91,;29.72,-32.59,;31.06,-33.36,;31.06,-34.91,;32.38,-35.68,;33.8,-35.05,;34.82,-36.2,;34.05,-37.53,;34.52,-39,;33.49,-40.15,;31.98,-39.82,;31.51,-38.36,;32.54,-37.21,;32.38,-32.6,;33.72,-33.37,;32.38,-31.06,)|