Reaction Details Report a problem with these data
Target
Glucagon receptor
Ligand
BDBM50334481
Substrate
n/a
Meas. Tech.
ChEMBL_857260 (CHEMBL2160605)
IC50
86±n/a nM
Citation
Xiong, Y; Guo, J; Candelore, MR; Liang, R; Miller, C; Dallas-Yang, Q; Jiang, G; McCann, PE; Qureshi, SA; Tong, X; Xu, SS; Shang, J; Vincent, SH; Tota, LM; Wright, MJ; Yang, X; Zhang, BB; Tata, JR; Parmee, ER Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-ß-alanine (MK-0893) for the treatment of type II diabetes. J Med Chem 55:6137-48 (2012) [PubMed] Article
More Info.:
Target
Name:
Glucagon receptor
Synonyms:
GCGR | GL-R | GLR_HUMAN | Glucagon Receptor (GCGR) | Glucagon receptor (GlucR)
Type:
Enzyme
Mol. Mass.:
54026.92
Organism:
Homo sapiens (Human)
Description:
P47871
Residue:
477
Sequence:
MPPCQPQRPLLLLLLLLACQPQVPSAQVMDFLFEKWKLYGDQCHHNLSLLPPPTELVCNRTFDKYSCWPDTPANTTANISCPWYLPWHHKVQHRFVFKRCGPDGQWVRGPRGQPWRDASQCQMDGEEIEVQKEVAKMYSSFQVMYTVGYSLSLGALLLALAILGGLSKLHCTRNAIHANLFASFVLKASSVLVIDGLLRTRYSQKIGDDLSVSTWLSDGAVAGCRVAAVFMQYGIVANYCWLLVEGLYLHNLLGLATLPERSFFSLYLGIGWGAPMLFVVPWAVVKCLFENVQCWTSNDNMGFWWILRFPVFLAILINFFIFVRIVQLLVAKLRARQMHHTDYKFRLAKSTLTLIPLLGVHEVVFAFVTDEHAQGTLRSAKLFFDLFLSSFQGLLVAVLYCFLNKEVQSELRRRWHRWRLGKVLWEERNTSNHRASSSPGHGPPSKELQFGRGGGSQDSSAETPLAGGLPRLAESPF
Inhibitor
Name:
BDBM50334481
Synonyms:
3-(4-((3-(3,5-dichlorophenyl)-5-(4-(trifluoromethoxy)phenyl)-1H-pyrazol-1-yl)methyl)benzamido)propanoic acid | CHEMBL1644183
Type:
Small organic molecule
Emp. Form.:
C27H20Cl2F3N3O4
Mol. Mass.:
578.367
SMILES:
OC(=O)CCNC(=O)c1ccc(Cn2nc(cc2-c2ccc(OC(F)(F)F)cc2)-c2cc(Cl)cc(Cl)c2)cc1