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Target
Glucagon receptor
Ligand
BDBM50244121
Substrate
n/a
Meas. Tech.
ChEMBL_491827 (CHEMBL945217)
IC50
71±n/a nM
Citation
 Kim, RM; Chang, J; Lins, AR; Brady, E; Candelore, MR; Dallas-Yang, Q; Ding, V; Dragovic, J; Iliff, S; Jiang, G; Mock, S; Qureshi, S; Saperstein, R; Szalkowski, D; Tamvakopoulos, C; Tota, L; Wright, M; Yang, X; Tata, JR; Chapman, K; Zhang, BB; Parmee, 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:
BDBM50244121
Synonyms:
CHEMBL517861 | trans-4-(((4-tert-butylcyclohexyl)(1,5-dimethyl-1H-benzo[d]imidazol-2-yl)amino)methyl)-N-(1H-tetrazol-5-yl)benzamide
Type:
Small organic molecule
Emp. Form.:
C28H36N8O
Mol. Mass.:
500.6384
SMILES:
Cc1ccc2n(C)c(nc2c1)N(Cc1ccc(cc1)C(=O)Nc1nnn[nH]1)[C@H]1CC[C@@H](CC1)C(C)(C)C |r,wU:27.30,wD:30.37,(-7.79,-31.95,;-7.05,-33.31,;-7.85,-34.63,;-7.12,-35.97,;-5.59,-36.01,;-4.58,-37.18,;-4.94,-38.68,;-3.16,-36.58,;-3.28,-35.05,;-4.78,-34.69,;-5.51,-33.35,;-1.83,-37.36,;-1.84,-38.9,;-.51,-39.68,;.82,-38.91,;2.15,-39.69,;2.15,-41.23,;.8,-41.99,;-.53,-41.21,;3.47,-42.01,;3.46,-43.55,;4.81,-41.25,;6.14,-42.03,;6.66,-43.48,;8.2,-43.44,;8.64,-41.96,;7.37,-41.09,;-.5,-36.6,;-.5,-35.06,;.85,-34.3,;2.18,-35.09,;2.16,-36.63,;.83,-37.38,;3.52,-34.33,;4.84,-33.55,;4.29,-35.66,;2.75,-32.99,)|
Structure:
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