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TargetGlucagon receptor
LigandBDBM50244122
Substrate/Competitorn/a
Meas. Tech.ChEMBL_491826 (CHEMBL945216)
IC50 4±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 Lett18:3701-5 (2008) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Glucagon receptor
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:
MPPCQPQRPLLLLLLLLACQPQVPSAQVMDFLFEKWKLYGDQCHHNLSLLPPPTELVCNR
TFDKYSCWPDTPANTTANISCPWYLPWHHKVQHRFVFKRCGPDGQWVRGPRGQPWRDASQ
CQMDGEEIEVQKEVAKMYSSFQVMYTVGYSLSLGALLLALAILGGLSKLHCTRNAIHANL
FASFVLKASSVLVIDGLLRTRYSQKIGDDLSVSTWLSDGAVAGCRVAAVFMQYGIVANYC
WLLVEGLYLHNLLGLATLPERSFFSLYLGIGWGAPMLFVVPWAVVKCLFENVQCWTSNDN
MGFWWILRFPVFLAILINFFIFVRIVQLLVAKLRARQMHHTDYKFRLAKSTLTLIPLLGV
HEVVFAFVTDEHAQGTLRSAKLFFDLFLSSFQGLLVAVLYCFLNKEVQSELRRRWHRWRL
GKVLWEERNTSNHRASSSPGHGPPSKELQFGRGGGSQDSSAETPLAGGLPRLAESPF
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50244122
n/a
NameBDBM50244122
Synonyms:CHEMBL459457 | trans-4-(((4-tert-butylcyclohexyl)(1-methyl-1H-benzo[d]imidazol-2-yl)amino)methyl)-N-(1H-tetrazol-5-yl)benzamide
TypeSmall organic molecule
Emp. Form.C27H34N8O
Mol. Mass.486.6119
SMILESCn1c(nc2ccccc12)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,(21.92,-38.87,;22.27,-37.38,;23.7,-36.78,;23.58,-35.25,;22.08,-34.89,;21.34,-33.54,;19.8,-33.5,;19,-34.82,;19.74,-36.17,;21.27,-36.2,;25.03,-37.56,;25.02,-39.1,;26.35,-39.88,;27.68,-39.11,;29.01,-39.89,;29,-41.43,;27.66,-42.19,;26.33,-41.41,;30.33,-42.21,;30.32,-43.75,;31.67,-41.45,;33,-42.22,;33.52,-43.67,;35.06,-43.64,;35.5,-42.16,;34.23,-41.29,;26.36,-36.8,;26.36,-35.26,;27.71,-34.5,;29.04,-35.28,;29.02,-36.82,;27.69,-37.58,;30.38,-34.53,;31.7,-33.74,;31.15,-35.86,;29.61,-33.19,)|
Structure
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