teneligliptin [Ligand Id: 9906] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2147777 (MP-513, Teneligliptin)
  • dipeptidyl peptidase 4/Dipeptidyl peptidase IV in Human [ChEMBL: CHEMBL284] [GtoPdb: 1612] [UniProtKB: P27487]
  • dipeptidyl peptidase 4/Dipeptidyl peptidase IV in Rat [ChEMBL: CHEMBL4653] [GtoPdb: 1612] [UniProtKB: P14740]
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  • dipeptidyl peptidase 9/Dipeptidyl peptidase IX in Human [ChEMBL: CHEMBL4793] [GtoPdb: 2357] [UniProtKB: Q86TI2]
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  • dipeptidyl peptidase 8/Dipeptidyl peptidase VIII in Human [ChEMBL: CHEMBL4657] [GtoPdb: 2356] [UniProtKB: Q6V1X1]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
dipeptidyl peptidase 4/Dipeptidyl peptidase IV in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL284] [GtoPdb: 1612] [UniProtKB: P27487]
ChEMBL Binding affinity to human recombinant DPP4 (39 to 766 residues) at 5 uM by isothermal titration calorimetry B 7.92 pKd 11.9 nM Kd J Med Chem (2016) 59: 7466-7477 [PMID:27438064]
ChEMBL Binding affinity to human recombinant DPP4 (39 to 766 residues) by surface plasmon resonance analysis B 9.39 pKd 0.41 nM Kd J Med Chem (2016) 59: 7466-7477 [PMID:27438064]
GtoPdb - - 9.43 pIC50 0.37 nM IC50 Bioorg Med Chem (2012) 20: 5705-19 [PMID:22959556]
ChEMBL Inhibition of DPP4 in human plasma using GLY-Pro-MCA as substrate after 60 mins by fluorescence assay B 9.43 pIC50 0.37 nM IC50 Bioorg Med Chem (2012) 20: 5705-5719 [PMID:22959556]
dipeptidyl peptidase 4/Dipeptidyl peptidase IV in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4653] [GtoPdb: 1612] [UniProtKB: P14740]
ChEMBL Inhibition of DPP4 in rat plasma using GLY-Pro-MCA as substrate after 60 mins by fluorescence assay B 9.54 pIC50 0.29 nM IC50 Bioorg Med Chem (2012) 20: 5705-5719 [PMID:22959556]
dipeptidyl peptidase 9/Dipeptidyl peptidase IX in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4793] [GtoPdb: 2357] [UniProtKB: Q86TI2]
ChEMBL Inhibition of human DPP9 using GLY-Pro-MCA as substrate after 30 mins by cell-based fluorescence assay B 6.27 pIC50 540 nM IC50 Bioorg Med Chem (2012) 20: 5705-5719 [PMID:22959556]
GtoPdb - - 6.27 pIC50 540 nM IC50 Bioorg Med Chem (2012) 20: 5705-19 [PMID:22959556]
dipeptidyl peptidase 8/Dipeptidyl peptidase VIII in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4657] [GtoPdb: 2356] [UniProtKB: Q6V1X1]
ChEMBL Inhibition of human DPP8 using GLY-Pro-MCA as substrate after 30 mins by cell-based fluorescence assay B 6.59 pIC50 260 nM IC50 Bioorg Med Chem (2012) 20: 5705-5719 [PMID:22959556]
GtoPdb - - 6.59 pIC50 260 nM IC50 Bioorg Med Chem (2012) 20: 5705-19 [PMID:22959556]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]