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 529424 | J 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 529424 | J 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 529424 | J 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 529424 | J 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 529424 | J 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 529424 | J 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 529424 | J 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 529424 | J 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 529424 | J 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 529424 | J 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 529424 | J 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 529424 | J 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 529424 | J 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 529424 | J 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 529424 | J 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 529424 | J 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 529772 | Bioorg 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 529763 | J 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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