Target Validation Information
TTD ID	T60182
Target Name	Glucagon receptor (GCGR)
Type of Target	Successful
Drug Potency against Target	BI-32169	Drug Info	IC50 = 440 nM	[1]
	Des-His1[Glu9]glucagon-NH2	Drug Info	IC50 = 18 nM	[2]
	[des-His1,Tyr5,Glu9,D-Ala10]glucagon-NH2	Drug Info	IC50 = 510 nM	[3]
	[des-His1,Tyr5,Glu9,D-Phe10]glucagon-NH2	Drug Info	IC50 = 34.5 nM	[3]
	[des-His1,Tyr5,Glu9,D-Tyr10]glucagon-NH2	Drug Info	IC50 = 74 nM	[3]
	[des-His1,Tyr5,Glu9]glucagon-NH2	Drug Info	IC50 = 2.3 nM	[3]
References
REF 1	BI-32169, a bicyclic 19-peptide with strong glucagon receptor antagonist activity from Streptomyces sp. J Nat Prod. 2004 Sep;67(9):1528-31.
REF 2	Discovery and investigation of a novel class of thiophene-derived antagonists of the human glucagon receptor. Bioorg Med Chem Lett. 2005 Mar 1;15(5):1401-5.
REF 3	Topographical amino acid substitution in position 10 of glucagon leads to antagonists/partial agonists with greater binding differences. J Med Chem. 1996 Jun 21;39(13):2449-55.

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