Target Validation Information
Target ID T36075
Target Name Glucagon-like peptide 1 receptor
Target Type
Successful
Drug Potency against Target C[hGlu22-Lys26][Gly8]GLP-1(7-37)-NH2 Drug Info IC50 = 6.2 nM [529424]
C[Glu22-Orn26][Gly8]GLP-1(7-37)-NH2 Drug Info IC50 = 6.4 nM [529424]
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGRG-NH2 Drug Info IC50 = 1.7 nM [529424]
C[Glu21-Lys26][Gly8]GLP-1(7-37)-NH2 Drug Info IC50 = 210 nM [529424]
[Gly8]GLP-1(7-37)-NH2 Drug Info IC50 = 2.8 nM [529424]
C[Glu26-Lys30][Gly8]GLP-1(7-37)-NH2 Drug Info IC50 = 16 nM [529424]
C[Glu23-Lys27][Gly8]GLP-1(7-37)-NH2 Drug Info IC50 = 1.9 nM [529424]
C[Glu18-Lys22][Gly8]GLP-1(7-37)-NH2 Drug Info IC50 = 3.6 nM [529424]
C[Glu19-Lys23][Gly8]GLP-1(7-37)-NH2 Drug Info IC50 = 17 nM [529424]
C[Glu24-Lys28][Gly8]GLP-1(7-37)-NH2 Drug Info IC50 = 290 nM [529424]
C[Asp22-Lys26][Gly8]GLP-1(7-37)-NH2 Drug Info IC50 = 64 nM [529424]
[Gly8,Glu22]GLP-1(7,37)-NH2 Drug Info IC50 = 1.1 nM [529424]
Glu20-Lys24][Gly8][GLP-1(7-37)-NH2 Drug Info IC50 = 26 nM [529424]
C[Cpa19-Lys26][Gly8]GLP-1(7-37)-NH2 Drug Info IC50 = 2000 nM [529424]
[Gly8, aib22]GLP-1(7-37)-NH2 Drug Info IC50 = 2.9 nM [529424]
C[Glu21-Lys25][Gly8]GLP-1(7-37)-NH2 Drug Info IC50 = 60 nM [529424]
HAEGTFTSDVSSYLEGQAAKEIFAWLVKGR Drug Info IC50 = 2.6 nM [529772]
NH2-HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR-CONH2 Drug Info IC50 = 1.9 nM [529763]
References
Ref 529424J Med Chem. 2008 May 8;51(9):2758-65. Epub 2008 Apr 15.Design and synthesis of conformationally constrained glucagon-like peptide-1 derivatives with increased plasma stability and prolonged in vivo activity.
Ref 529424J Med Chem. 2008 May 8;51(9):2758-65. Epub 2008 Apr 15.Design and synthesis of conformationally constrained glucagon-like peptide-1 derivatives with increased plasma stability and prolonged in vivo activity.
Ref 529424J Med Chem. 2008 May 8;51(9):2758-65. Epub 2008 Apr 15.Design and synthesis of conformationally constrained glucagon-like peptide-1 derivatives with increased plasma stability and prolonged in vivo activity.
Ref 529424J Med Chem. 2008 May 8;51(9):2758-65. Epub 2008 Apr 15.Design and synthesis of conformationally constrained glucagon-like peptide-1 derivatives with increased plasma stability and prolonged in vivo activity.
Ref 529424J Med Chem. 2008 May 8;51(9):2758-65. Epub 2008 Apr 15.Design and synthesis of conformationally constrained glucagon-like peptide-1 derivatives with increased plasma stability and prolonged in vivo activity.
Ref 529424J Med Chem. 2008 May 8;51(9):2758-65. Epub 2008 Apr 15.Design and synthesis of conformationally constrained glucagon-like peptide-1 derivatives with increased plasma stability and prolonged in vivo activity.
Ref 529424J Med Chem. 2008 May 8;51(9):2758-65. Epub 2008 Apr 15.Design and synthesis of conformationally constrained glucagon-like peptide-1 derivatives with increased plasma stability and prolonged in vivo activity.
Ref 529424J Med Chem. 2008 May 8;51(9):2758-65. Epub 2008 Apr 15.Design and synthesis of conformationally constrained glucagon-like peptide-1 derivatives with increased plasma stability and prolonged in vivo activity.
Ref 529424J Med Chem. 2008 May 8;51(9):2758-65. Epub 2008 Apr 15.Design and synthesis of conformationally constrained glucagon-like peptide-1 derivatives with increased plasma stability and prolonged in vivo activity.
Ref 529424J Med Chem. 2008 May 8;51(9):2758-65. Epub 2008 Apr 15.Design and synthesis of conformationally constrained glucagon-like peptide-1 derivatives with increased plasma stability and prolonged in vivo activity.
Ref 529424J Med Chem. 2008 May 8;51(9):2758-65. Epub 2008 Apr 15.Design and synthesis of conformationally constrained glucagon-like peptide-1 derivatives with increased plasma stability and prolonged in vivo activity.
Ref 529424J Med Chem. 2008 May 8;51(9):2758-65. Epub 2008 Apr 15.Design and synthesis of conformationally constrained glucagon-like peptide-1 derivatives with increased plasma stability and prolonged in vivo activity.
Ref 529424J Med Chem. 2008 May 8;51(9):2758-65. Epub 2008 Apr 15.Design and synthesis of conformationally constrained glucagon-like peptide-1 derivatives with increased plasma stability and prolonged in vivo activity.
Ref 529424J Med Chem. 2008 May 8;51(9):2758-65. Epub 2008 Apr 15.Design and synthesis of conformationally constrained glucagon-like peptide-1 derivatives with increased plasma stability and prolonged in vivo activity.
Ref 529424J Med Chem. 2008 May 8;51(9):2758-65. Epub 2008 Apr 15.Design and synthesis of conformationally constrained glucagon-like peptide-1 derivatives with increased plasma stability and prolonged in vivo activity.
Ref 529424J Med Chem. 2008 May 8;51(9):2758-65. Epub 2008 Apr 15.Design and synthesis of conformationally constrained glucagon-like peptide-1 derivatives with increased plasma stability and prolonged in vivo activity.
Ref 529772Bioorg Med Chem. 2008 Dec 1;16(23):10106-12. Epub 2008 Oct 5.Search for alpha-helical propensity in the receptor-bound conformation of glucagon-like peptide-1.
Ref 529763J Med Chem. 2008 Nov 27;51(22):7303-7.Influence of selective fluorination on the biological activity and proteolytic stability of glucagon-like peptide-1.

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