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TargetGlucagon receptor
LigandBDBM50334486
Substrate/Competitorn/a
Meas. Tech.ChEMBL_701136 (CHEMBL1648234)
IC50 3.2±n/a nM
Citation Shen, DMBrady, EJCandelore, MRDallas-Yang, QDing, VDFeeney, WPJiang, GMcCann, MEMock, SQureshi, SASaperstein, RShen, XTong, XTota, LMWright, MJYang, XZheng, SChapman, KTZhang, BBTata, JRParmee, ER Discovery of novel, potent, selective, and orally active human glucagon receptor antagonists containing a pyrazole core. Bioorg Med Chem Lett21:76-81 (2010) [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:
BDBM50334486
n/a
NameBDBM50334486
Synonyms:CHEMBL1643951 | trans-4-((1-(4-tert-butylcyclohexyl)-3-(4-(trifluoromethoxy)phenyl)ureido)methyl)-N-(2H-tetrazol-5-yl)benzamide
TypeSmall organic molecule
Emp. Form.C27H32F3N7O3
Mol. Mass.559.5833
SMILESCC(C)(C)[C@H]1CC[C@@H](CC1)N(Cc1ccc(cc1)C(=O)Nc1nnn[nH]1)C(=O)Nc1ccc(OC(F)(F)F)cc1 |r,wU:7.10,wD:4.3,(26.38,-4.09,;27.72,-3.32,;29.05,-4.09,;27.7,-4.85,;27.72,-1.78,;29.05,-1.01,;29.05,.54,;27.72,1.29,;26.38,.53,;26.38,-1.01,;27.71,2.83,;26.38,3.6,;25.05,2.82,;25.05,1.27,;23.71,.5,;22.38,1.27,;22.38,2.82,;23.71,3.59,;21.05,.5,;21.04,-1.04,;19.71,1.27,;18.38,.5,;16.98,1.14,;15.95,-.01,;16.72,-1.34,;18.23,-1.02,;29.04,3.61,;29.04,5.15,;30.38,2.84,;31.71,3.62,;33.04,2.85,;34.37,3.62,;34.37,5.16,;35.7,5.94,;37.03,5.18,;38.36,5.96,;37.04,3.64,;38.36,4.41,;33.02,5.93,;31.7,5.15,)|
Structure
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