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

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ChEMBL ligand: CHEMBL385517 (BMS-477118, SBMS-477118)
  • 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 (unknown origin) B 7.3 pIC50 50 nM IC50 J Med Chem (2014) 57: 2197-2212 [PMID:24099035]
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 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 human DPP4 using Gly-Pro-AMC as substrate incubated for 30 mins by continuous fluorescent assay B 8.82 pIC50 1.5 nM IC50 Bioorg Med Chem Lett (2022) 76: 129018-129018 [PMID:36209967]
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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]