Reaction Details Report a problem with these data
Target
Glucagon receptor
Ligand
BDBM50244162
Substrate
n/a
Meas. Tech.
ChEMBL_491827 (CHEMBL945217)
IC50
430±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:
BDBM50244162
Synonyms:
CHEMBL515202 | cis-4-(((4-tert-butylcyclohexyl)(1-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:
Cn1c(nc2ccccc12)N(Cc1ccc(cc1)C(=O)Nc1nnn[nH]1)[C@H]1CC[C@H](CC1)C(C)(C)C |r,wU:26.29,29.36,(-7.22,-33.1,;-6.45,-31.77,;-5.02,-31.18,;-5.15,-29.64,;-6.65,-29.29,;-7.38,-27.94,;-8.92,-27.9,;-9.72,-29.22,;-8.98,-30.56,;-7.45,-30.6,;-3.69,-31.96,;-3.7,-33.5,;-2.37,-34.27,;-1.04,-33.51,;.29,-34.28,;.28,-35.82,;-1.07,-36.59,;-2.39,-35.81,;1.61,-36.6,;1.6,-38.14,;2.95,-35.84,;4.28,-36.62,;4.79,-38.07,;6.33,-38.03,;6.77,-36.56,;5.51,-35.68,;-2.37,-31.19,;-2.36,-29.66,;-1.01,-28.9,;.31,-29.68,;.3,-31.22,;-1.04,-31.98,;1.65,-28.92,;2.98,-28.14,;2.43,-30.26,;.89,-27.59,)|
Structure:
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