Target Validation Information
TTD ID	T36075
Target Name	Glucagon-like peptide 1 receptor (GLP1R)
Type of Target	Successful
Drug Potency against Target	C[Asp22-Lys26][Gly8]GLP-1(7-37)-NH2	Drug Info	IC50 = 64 nM	[1]
	C[Cpa19-Lys26][Gly8]GLP-1(7-37)-NH2	Drug Info	IC50 = 2000 nM	[1]
	C[Glu18-Lys22][Gly8]GLP-1(7-37)-NH2	Drug Info	IC50 = 3.6 nM	[1]
	C[Glu19-Lys23][Gly8]GLP-1(7-37)-NH2	Drug Info	IC50 = 17 nM	[1]
	C[Glu21-Lys25][Gly8]GLP-1(7-37)-NH2	Drug Info	IC50 = 60 nM	[1]
	C[Glu21-Lys26][Gly8]GLP-1(7-37)-NH2	Drug Info	IC50 = 210 nM	[1]
	C[Glu22-Orn26][Gly8]GLP-1(7-37)-NH2	Drug Info	IC50 = 6.4 nM	[1]
	C[Glu23-Lys27][Gly8]GLP-1(7-37)-NH2	Drug Info	IC50 = 1.9 nM	[1]
	C[Glu24-Lys28][Gly8]GLP-1(7-37)-NH2	Drug Info	IC50 = 290 nM	[1]
	C[Glu26-Lys30][Gly8]GLP-1(7-37)-NH2	Drug Info	IC50 = 16 nM	[1]
	C[hGlu22-Lys26][Gly8]GLP-1(7-37)-NH2	Drug Info	IC50 = 6.2 nM	[1]
	GLP-1	Drug Info	IC50 = 1.9 nM	[2]
	Glu20-Lys24][Gly8][GLP-1(7-37)-NH2	Drug Info	IC50 = 26 nM	[1]
	HAEGTFTSDVSSYLEGQAAKEFIAWLVKGRG-NH2	Drug Info	IC50 = 1.7 nM	[1]
	HAEGTFTSDVSSYLEGQAAKEIFAWLVKGR	Drug Info	IC50 = 2.6 nM	[3]
	[Gly8, aib22]GLP-1(7-37)-NH2	Drug Info	IC50 = 2.9 nM	[1]
	[Gly8,Glu22]GLP-1(7,37)-NH2	Drug Info	IC50 = 1.1 nM	[1]
	[Gly8]GLP-1(7-37)-NH2	Drug Info	IC50 = 2.8 nM	[1]
References
REF 1	Design and synthesis of conformationally constrained glucagon-like peptide-1 derivatives with increased plasma stability and prolonged in vivo acti... J Med Chem. 2008 May 8;51(9):2758-65.
REF 2	Influence of selective fluorination on the biological activity and proteolytic stability of glucagon-like peptide-1. J Med Chem. 2008 Nov 27;51(22):7303-7.
REF 3	Search for alpha-helical propensity in the receptor-bound conformation of glucagon-like peptide-1. Bioorg Med Chem. 2008 Dec 1;16(23):10106-12.

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