Target Validation Information
Target ID T60182
Target Name Glucagon receptor
Target Type
Successful
Drug Potency against Target [des-His1,Tyr5,Glu9,D-Tyr10]glucagon-NH2 Drug Info IC50 = 74 nM [534147]
[des-His1,Tyr5,Glu9,D-Phe10]glucagon-NH2 Drug Info IC50 = 34.5 nM [534147]
Des-His1[Glu9]glucagon-NH2 Drug Info IC50 = 18 nM [527432]
BI-32169 Drug Info IC50 = 440 nM [527224]
[des-His1,Tyr5,Glu9]glucagon-NH2 Drug Info IC50 = 2.3 nM [534147]
[des-His1,Tyr5,Glu9,D-Ala10]glucagon-NH2 Drug Info IC50 = 510 nM [534147]
References
Ref 534147J Med Chem. 1996 Jun 21;39(13):2449-55.Topographical amino acid substitution in position 10 of glucagon leads to antagonists/partial agonists with greater binding differences.
Ref 534147J Med Chem. 1996 Jun 21;39(13):2449-55.Topographical amino acid substitution in position 10 of glucagon leads to antagonists/partial agonists with greater binding differences.
Ref 527432Bioorg Med Chem Lett. 2005 Mar 1;15(5):1401-5.Discovery and investigation of a novel class of thiophene-derived antagonists of the human glucagon receptor.
Ref 527224J Nat Prod. 2004 Sep;67(9):1528-31.BI-32169, a bicyclic 19-peptide with strong glucagon receptor antagonist activity from Streptomyces sp.
Ref 534147J Med Chem. 1996 Jun 21;39(13):2449-55.Topographical amino acid substitution in position 10 of glucagon leads to antagonists/partial agonists with greater binding differences.
Ref 534147J Med Chem. 1996 Jun 21;39(13):2449-55.Topographical amino acid substitution in position 10 of glucagon leads to antagonists/partial agonists with greater binding differences.

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