saxagliptin [Ligand Id: 6316] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL385517 (BMS-477118, BMS-477118-11, Saxagliptin)
  • Dipeptidyl-peptidase 7/Dipeptidyl peptidase II in Human [ChEMBL: CHEMBL3976] [GtoPdb: 1605] [UniProtKB: Q9UHL4]
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  • dipeptidyl peptidase 4/Dipeptidyl peptidase IV in Human [ChEMBL: CHEMBL284] [GtoPdb: 1612] [UniProtKB: P27487]
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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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  • fibroblast activation protein alpha/Fibroblast activation protein alpha in Human [ChEMBL: CHEMBL4683] [GtoPdb: 2365] [UniProtKB: Q12884]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Dipeptidyl-peptidase 7/Dipeptidyl peptidase II in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3976] [GtoPdb: 1605] [UniProtKB: Q9UHL4]
ChEMBL Inhibition of human DPP2 using Lys-Ala-AMC as substrate by fluorimetric analysis B 4.52 pIC50 >30000 nM IC50 Bioorg Med Chem (2012) 20: 5864-5883 [PMID:22938786]
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 7.8 pKd 15.9 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 9.52 pKd 0.3 nM Kd J Med Chem (2016) 59: 7466-7477 [PMID:27438064]
GtoPdb - - 9.2 pKi 0.6 nM Ki Curr Drug Targets (2009) 10: 71-87 [PMID:19149538]
ChEMBL In vitro inhibition constant against human Dipeptidyl peptidase IV B 9.22 pKi 0.6 nM Ki J Med Chem (2005) 48: 5025-5037 [PMID:16033281]
ChEMBL Inhibition of human DPP4 expressed in Caco-2 cells B 9.22 pKi 0.6 nM Ki J Med Chem (2006) 49: 6416-6420 [PMID:17034148]
ChEMBL Inhibition of human DPP4 B 9.22 pKi 0.6 nM Ki Bioorg Med Chem Lett (2007) 17: 6476-6480 [PMID:17937986]
ChEMBL Inhibition of human DPP4 B 9.22 pKi 0.6 nM Ki Bioorg Med Chem (2009) 17: 1783-1802 [PMID:19217790]
ChEMBL Inhibition of DPP4 B 9.22 pKi 0.6 nM Ki Eur J Med Chem (2009) 44: 3318-3322 [PMID:19375196]
ChEMBL Inhibition of DPP4 in human Caco2 cells using H-Ala-Pro-7-amido-4-trifluoromethylcoumarin as substrate after 1 hr by fluorescence assay B 7.3 pIC50 50 nM IC50 Bioorg Med Chem (2013) 21: 2795-2825 [PMID:23623674]
ChEMBL Inhibition of DPP4 (unknown origin) B 7.3 pIC50 50 nM IC50 J Med Chem (2014) 57: 2197-2212 [PMID:24099035]
ChEMBL Inhibition of human recombinant DPP-4 using H-Gly-Pro-AMC as substrate after 10 mins by fluorescence assay B 7.52 pIC50 30.3 nM IC50 Bioorg Med Chem (2014) 22: 1383-1393 [PMID:24457090]
ChEMBL Inhibition of DPP4 B 8.47 pIC50 3.4 nM IC50 Bioorg Med Chem Lett (2010) 20: 3596-3600 [PMID:20483603]
ChEMBL Inhibition of DPP4 in human plasma using Gly-Pro-AMC as substrate by fluorimetric analysis B 8.47 pIC50 3.37 nM IC50 Bioorg Med Chem (2012) 20: 5864-5883 [PMID:22938786]
ChEMBL Inhibition of human recombinant DPP4 by fluorescence assay B 8.52 pIC50 3 nM IC50 Bioorg Med Chem Lett (2009) 19: 4437-4440 [PMID:19482472]
ChEMBL Inhibition of DPP4 B 9.22 pIC50 0.6 nM IC50 J Med Chem (2011) 54: 5737-5746 [PMID:21711053]
dipeptidyl peptidase 9/Dipeptidyl peptidase IX in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4793] [GtoPdb: 2357] [UniProtKB: Q86TI2]
ChEMBL Inhibition of DPP9 B 7.15 pKi 71 nM Ki J Med Chem (2006) 49: 6416-6420 [PMID:17034148]
ChEMBL Inhibition of DPP9 B 6.98 pIC50 104 nM IC50 Bioorg Med Chem (2012) 20: 5864-5883 [PMID:22938786]
ChEMBL Inhibition of DPP9 B 7 pIC50 100 nM IC50 Bioorg Med Chem Lett (2010) 20: 3596-3600 [PMID:20483603]
dipeptidyl peptidase 8/Dipeptidyl peptidase VIII in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4657] [GtoPdb: 2356] [UniProtKB: Q6V1X1]
ChEMBL Inhibition of DPP8 B 6.89 pKi 130 nM Ki J Med Chem (2006) 49: 6416-6420 [PMID:17034148]
ChEMBL Inhibition of DPP8 B 6.61 pIC50 244 nM IC50 Bioorg Med Chem (2012) 20: 5864-5883 [PMID:22938786]
ChEMBL Inhibition of DPP8 B 6.62 pIC50 240 nM IC50 Bioorg Med Chem Lett (2010) 20: 3596-3600 [PMID:20483603]
fibroblast activation protein alpha/Fibroblast activation protein alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4683] [GtoPdb: 2365] [UniProtKB: Q12884]
ChEMBL Inhibition of FAP (unknown origin) B 6 pIC50 >1000 nM IC50 Bioorg Med Chem Lett (2020) 30: 127253-127253 [PMID:32527554]

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]