Reaction Details Report a problem with these data
Target
Glucagon receptor
Ligand
BDBM50334511
Substrate
n/a
Meas. Tech.
ChEMBL_701136 (CHEMBL1648234)
IC50
520±n/a nM
Citation
Shen, DM; Brady, EJ; Candelore, MR; Dallas-Yang, Q; Ding, VD; Feeney, WP; Jiang, G; McCann, ME; Mock, S; Qureshi, SA; Saperstein, R; Shen, X; Tong, X; Tota, LM; Wright, MJ; Yang, X; Zheng, S; Chapman, KT; Zhang, BB; Tata, JR; Parmee, ER Discovery of novel, potent, selective, and orally active human glucagon receptor antagonists containing a pyrazole core. Bioorg Med Chem Lett 21:76-81 (2010) [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:
BDBM50334511
Synonyms:
4-((5-(4-(1-(4-chlorophenyl)ethyl)phenyl)-3-(4-(trifluoromethoxy)phenyl)-1H-pyrazol-1-yl)methyl)-N-(2H-tetrazol-5-yl)benzamide | CHEMBL1644199
Type:
Small organic molecule
Emp. Form.:
C33H25ClF3N7O2
Mol. Mass.:
644.046
SMILES:
CC(c1ccc(Cl)cc1)c1ccc(cc1)-c1cc(nn1Cc1ccc(cc1)C(=O)Nc1nnn[nH]1)-c1ccc(OC(F)(F)F)cc1