Target
Glucagon receptor
Ligand
BDBM50244080
Substrate
n/a
Meas. Tech.
ChEMBL_491827 (CHEMBL945217)
IC50
>1000±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:
BDBM50244080
Synonyms:
CHEMBL509900 | trans-4-((4-tert-butylcyclohexyl)(5-methyl-1H-benzo[d]imidazol-2-yl)amino)methyl)-N-(1H-tetrazol-5-yl)benzamide
Type:
Small organic molecule
Emp. Form.:
C27H34N8O
Mol. Mass.:
486.6119
SMILES:
Cc1ccc2nc([nH]c2c1)N(Cc1ccc(cc1)C(=O)Nc1nnn[nH]1)[C@H]1CC[C@@H](CC1)C(C)(C)C |r,wU:26.29,wD:29.36,(16.94,-17.66,;17.68,-19.01,;16.88,-20.33,;17.62,-21.67,;19.15,-21.71,;20.15,-22.88,;21.58,-22.29,;21.45,-20.75,;19.95,-20.4,;19.22,-19.05,;22.91,-23.07,;22.9,-24.61,;24.23,-25.38,;25.56,-24.62,;26.89,-25.39,;26.88,-26.93,;25.53,-27.7,;24.21,-26.92,;28.21,-27.71,;28.2,-29.25,;29.55,-26.95,;30.88,-27.73,;31.39,-29.18,;32.93,-29.14,;33.37,-27.67,;32.1,-26.79,;24.23,-22.3,;24.24,-20.77,;25.58,-20.01,;26.91,-20.79,;26.9,-22.33,;25.56,-23.09,;28.25,-20.03,;29.58,-19.25,;29.03,-21.36,;27.49,-18.7,)|
Structure:
Search PDB for entries with ligand similarity: