Target
Glucagon receptor
Ligand
BDBM50244337
Substrate
n/a
Meas. Tech.
ChEMBL_491827 (CHEMBL945217)
IC50
23±n/a nM
Citation
 Kim, RMChang, JLins, ARBrady, ECandelore, MRDallas-Yang, QDing, VDragovic, JIliff, SJiang, GMock, SQureshi, SSaperstein, RSzalkowski, DTamvakopoulos, CTota, LWright, MYang, XTata, JRChapman, KZhang, BBParmee, ER Discovery of potent, orally active benzimidazole glucagon receptor antagonists. Bioorg Med Chem Lett 18:3701-5 (2008) [PubMed]  Article 
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:
BDBM50244337
Synonyms:
CHEMBL511964 | trans-4-(((4-tert-butylcyclohexyl)(5,6-dichloro-1-methyl-1H-benzo[d]imidazol-2-yl)amino)methyl)-N-(1H-tetrazol-5-yl)benzamide
Type:
Small organic molecule
Emp. Form.:
C27H32Cl2N8O
Mol. Mass.:
555.502
SMILES:
Cn1c(nc2cc(Cl)c(Cl)cc12)N(Cc1ccc(cc1)C(=O)Nc1nnn[nH]1)[C@H]1CC[C@@H](CC1)C(C)(C)C |r,wU:28.31,wD:31.38,(37.8,-49.39,;38.58,-48.06,;40,-47.47,;39.88,-45.93,;38.38,-45.58,;37.65,-44.23,;36.11,-44.19,;35.37,-42.84,;35.31,-45.51,;33.77,-45.47,;36.05,-46.85,;37.58,-46.89,;41.33,-48.24,;41.33,-49.78,;42.66,-50.56,;43.99,-49.79,;45.31,-50.57,;45.31,-52.11,;43.96,-52.87,;42.64,-52.09,;46.64,-52.89,;46.63,-54.43,;47.97,-52.13,;49.3,-52.91,;49.82,-54.36,;51.36,-54.32,;51.8,-52.84,;50.53,-51.97,;42.66,-47.48,;42.67,-45.94,;44.01,-45.19,;45.34,-45.97,;45.32,-47.51,;43.99,-48.26,;46.68,-45.21,;48,-44.43,;47.45,-46.54,;45.92,-43.87,)|
Structure:
Search PDB for entries with ligand similarity: