talabostat [Ligand Id: 9892] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL67279 (PT-100, Talabostat, Valinyl-L-Boroproline)
  • 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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  • prolyl endopeptidase/Prolyl endopeptidase in Human [ChEMBL: CHEMBL3202] [GtoPdb: 2395] [UniProtKB: P48147]
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  • fibroblast activation protein alpha/Seprase in Mouse [ChEMBL: CHEMBL5769] [GtoPdb: 2365] [UniProtKB: P97321]
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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 Inhibitory activity of compound against Dipeptidylpeptidase II (DPP II) B 3.9 pKi 125000 nM Ki J. Med. Chem. (2003) 46: 5005-5014 [PMID:14584950]
ChEMBL Inhibition of Dipeptidyl Peptidase II (Quiescent cell proline peptidase) B 6.9 pKi 125 nM Ki Bioorg. Med. Chem. Lett. (2002) 12: 2825-2828 [PMID:12270155]
ChEMBL Inhibition of quiescent cell proline dipeptidase (QPP) B 6.9 pKi 125 nM Ki J. Med. Chem. (2004) 47: 4135-4141 [PMID:15293982]
ChEMBL Inhibition of DPP2 in human seminal plasma using Lys-Ala-p-nitroanilide as substrate incubated for 15 mins prior to substrate addition B 7.07 pIC50 86 nM IC50 ACS Med. Chem. Lett. (2013) 4: 491-496 [PMID:24900696]
ChEMBL Binding affinity to DPP2 (unknown origin) B 7.07 pIC50 86 nM IC50 MedChemComm (2014) 5: 1700-1707
ChEMBL Inhibition of DPP2 (unknown origin) using AMC substrate by fluorometric assay B 7.07 pIC50 86 nM IC50 Bioorg Med Chem Lett (2021) 37: 127846-127846 [PMID:33571650]
ChEMBL Inhibition of human seminal plasma DPP2 assessed as pNA release from Lys-Ala-p-nitroanilide substrate pre-incubated with enzyme for 15 min prior to substrate addition by fluorescence technique B 7.07 pIC50 86 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 3412-3417 [PMID:22525314]
ChEMBL Inhibition of DPP2 purified from human seminal plasma using Lys-Ala-p-nitroanilide as substrate by spectrophotometry B 7.07 pIC50 86 nM IC50 J. Med. Chem. (2014) 57: 3053-3074 [PMID:24617858]
ChEMBL Inhibition of human DPP2 B 7.52 pIC50 30 nM IC50 Bioorg. Med. Chem. Lett. (2007) 17: 507-510 [PMID:17055271]
ChEMBL Compound was tested in vitro for inhibition of Dipeptidylpeptidase II B 7.82 pIC50 15 nM IC50 J. Med. Chem. (1996) 39: 2087-2094 [PMID:8642568]
dipeptidyl peptidase 4/Dipeptidyl peptidase IV in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL284] [GtoPdb: 1612] [UniProtKB: P27487]
ChEMBL Inhibitory activity of compound against Dipeptidylpeptidase IV (DPP IV) B 5.7 pKi 2000 nM Ki J. Med. Chem. (2003) 46: 5005-5014 [PMID:14584950]
ChEMBL Inhibition of Dipeptidyl Peptidase IV B 8.7 pKi 2 nM Ki Bioorg. Med. Chem. Lett. (2002) 12: 2825-2828 [PMID:12270155]
ChEMBL Binding affinity for dipeptidylpeptidase IV B 8.7 pKi 2 nM Ki J. Med. Chem. (2004) 47: 4135-4141 [PMID:15293982]
GtoPdb - - 9.74 pKi 0.18 nM Ki J Med Chem (2008) 51: 6005-13 [PMID:18783201]
ChEMBL Inhibition of human placental DPP4 B 9.74 pKi 0.18 nM Ki J. Med. Chem. (2007) 50: 2391-2398 [PMID:17458948]
ChEMBL Inhibition of human placental DPP4 B 9.74 pKi 0.18 nM Ki J. Med. Chem. (2008) 51: 6005-6013 [PMID:18783201]
ChEMBL Inhibition of human placental DPP4 at pH 8 B 5.92 pIC50 1200 nM IC50 J. Med. Chem. (2007) 50: 2391-2398 [PMID:17458948]
ChEMBL Inhibition Assay: The inhibitor solution is prepared by dissolving 3-5 mg of inhibitor in pH 2 solution (0.01 N HCl), such that the concentration of the solution is equal to 1 mg/10 mL. A 10 μL sample of this solution is then added to 990 μL of pH 8 buffer (0.1 M HEPES, 0.14 M NaCl), and the solution is allowed to stand at room temperature overnight.The enzyme solution is prepared by diluting 20 μL of DPIV (concentration 2.5 nM) into 40 mL of pH 8 buffer.The substrate solution is prepared by dissolving 2.0 mg of L-alanyl-L-proline-para-nitroanilide into 20 mL of pH 8 buffer.250 μL of enzyme solution is added to well #B1 to #H1, #A2 to #H2, and #A3 to #H3 of a 96 well plate, while well #A1 receives 250 μL of pH 8 buffer instead of enzyme solution. 904 of pH 8 buffer is then added to column 5 (from well #A5 to #H5). B 5.92 pIC50 1200 nM IC50 US-8933056-B2. Soft protease inhibitors and pro-soft forms thereof (2015)
ChEMBL Inhibition of DDP4 at pH 7.4 preincubated for 10 mins B 6.33 pIC50 470 nM IC50 J. Med. Chem. (2011) 54: 2022-2028 [PMID:21388136]
ChEMBL In vitro for inhibition of Dipeptidylpeptidase IV. B 7.59 pIC50 26 nM IC50 J. Med. Chem. (1996) 39: 2087-2094 [PMID:8642568]
ChEMBL Inhibition of DPP4 (unknown origin) using AMC substrate by fluorometric assay B 7.66 pIC50 22 nM IC50 Bioorg Med Chem Lett (2021) 37: 127846-127846 [PMID:33571650]
ChEMBL Inhibition of human seminal plasma DPP4 assessed as pNA release from Gly-Pro-p-nitroanilide substrate pre-incubated with enzyme for 15 min prior to substrate addition by fluorescence technique B 7.66 pIC50 22 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 3412-3417 [PMID:22525314]
ChEMBL Inhibition of DPP4 in human seminal plasma using Gly-Pro-p-nitroanilide as substrate incubated for 15 mins prior to substrate addition B 7.66 pIC50 22 nM IC50 ACS Med. Chem. Lett. (2013) 4: 491-496 [PMID:24900696]
ChEMBL Inhibition of DPP4 purified from human seminal plasma using Gly-Pro-p-nitroanilide as substrate by spectrophotometry B 7.66 pIC50 22 nM IC50 J. Med. Chem. (2014) 57: 3053-3074 [PMID:24617858]
ChEMBL Binding affinity to DPP4 (unknown origin) B 7.66 pIC50 22 nM IC50 MedChemComm (2014) 5: 1700-1707
ChEMBL Inhibition of DPP4 (unknown origin) B 7.66 pIC50 22 nM IC50 J Med Chem (2019) 62: 7874-7884 [PMID:31393718]
ChEMBL Inhibition Assay: The inhibitor solution is prepared by dissolving 3-5 mg of inhibitor in pH 2 solution (0.01 N HCl), such that the concentration of the solution is equal to 1 mg/10 mL. A 10 μL sample of this solution is then added to 990 μL of pH 8 buffer (0.1 M HEPES, 0.14 M NaCl), and the solution is allowed to stand at room temperature overnight.The enzyme solution is prepared by diluting 20 μL of DPIV (concentration 2.5 nM) into 40 mL of pH 8 buffer.The substrate solution is prepared by dissolving 2.0 mg of L-alanyl-L-proline-para-nitroanilide into 20 mL of pH 8 buffer.250 μL of enzyme solution is added to well #B1 to #H1, #A2 to #H2, and #A3 to #H3 of a 96 well plate, while well #A1 receives 250 μL of pH 8 buffer instead of enzyme solution. 904 of pH 8 buffer is then added to column 5 (from well #A5 to #H5). B 8.77 pIC50 1.7 nM IC50 US-8933056-B2. Soft protease inhibitors and pro-soft forms thereof (2015)
ChEMBL Inhibition of human placental DPP4 at pH 2 B 8.8 pIC50 1.6 nM IC50 J. Med. Chem. (2007) 50: 2391-2398 [PMID:17458948]
ChEMBL Inhibition of DDP4 at pH 2 preincubated for 10 mins B 8.82 pIC50 1.5 nM IC50 J. Med. Chem. (2011) 54: 2022-2028 [PMID:21388136]
ChEMBL Inhibition of human DPP4 using H-Gly-Pro-AMC as substrate preincubated for 10 mins prior to substrate addition by fluorescence assay B 9.05 pIC50 0.9 nM IC50 J. Med. Chem. (2013) 56: 3467-3477 [PMID:23594271]
ChEMBL Inhibition of human DPP4 B 10 pIC50 0.1 nM IC50 Bioorg. Med. Chem. Lett. (2007) 17: 507-510 [PMID:17055271]
dipeptidyl peptidase 9/Dipeptidyl peptidase IX in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4793] [GtoPdb: 2357] [UniProtKB: Q86TI2]
ChEMBL Inhibition of human recombinant DPP9 expressed in HEK293T cells B 9.12 pKi 0.76 nM Ki J. Med. Chem. (2008) 51: 6005-6013 [PMID:18783201]
GtoPdb - - 9.12 pKi 0.76 nM Ki J Med Chem (2008) 51: 6005-13 [PMID:18783201]
ChEMBL Inhibition of human recombinant DPP9 expressed in intact HEK293T cells after 2 hrs B 5.17 pIC50 6800 nM IC50 J. Med. Chem. (2008) 51: 6005-6013 [PMID:18783201]
ChEMBL Inhibition of human DPP9 using H-Gly-Pro-AMC as substrate preincubated for 10 mins prior to substrate addition by fluorescence assay B 8.66 pIC50 2.2 nM IC50 J. Med. Chem. (2013) 56: 3467-3477 [PMID:23594271]
ChEMBL Inhibition of human DPP9 B 8.7 pIC50 2 nM IC50 Bioorg. Med. Chem. Lett. (2007) 17: 507-510 [PMID:17055271]
dipeptidyl peptidase 8/Dipeptidyl peptidase VIII in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4657] [GtoPdb: 2356] [UniProtKB: Q6V1X1]
GtoPdb - - 8.82 pKi 1.5 nM Ki J Med Chem (2008) 51: 6005-13 [PMID:18783201]
ChEMBL Inhibition of human recombinant DPP8 expressed in HEK293T cells B 8.82 pKi 1.5 nM Ki J. Med. Chem. (2008) 51: 6005-6013 [PMID:18783201]
ChEMBL Inhibition of human DPP8 B 7.77 pIC50 17 nM IC50 Bioorg. Med. Chem. Lett. (2007) 17: 507-510 [PMID:17055271]
ChEMBL Inhibition of human DPP8 using H-Gly-Pro-AMC as substrate preincubated for 10 mins prior to substrate addition by fluorescence assay B 8.26 pIC50 5.5 nM IC50 J. Med. Chem. (2013) 56: 3467-3477 [PMID:23594271]
fibroblast activation protein alpha/Fibroblast activation protein alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4683] [GtoPdb: 2365] [UniProtKB: Q12884]
ChEMBL Inhibition of FAP in human U87MG cells using Suc-Gly-Pro-AMC as substrate by fluorescence based assay B 6.65 pIC50 224 nM IC50 Bioorg Med Chem Lett (2020) 30: 127253-127253 [PMID:32527554]
ChEMBL Binding affinity to FAP (unknown origin) B 7.15 pIC50 70 nM IC50 MedChemComm (2014) 5: 1700-1707
ChEMBL Inhibition of FAP (unknown origin) using AMC substrate by fluorometric assay B 7.15 pIC50 70 nM IC50 Bioorg Med Chem Lett (2021) 37: 127846-127846 [PMID:33571650]
ChEMBL Inhibition of FAP (unknown origin) B 7.18 pIC50 66 nM IC50 J Med Chem (2019) 62: 7874-7884 [PMID:31393718]
ChEMBL Inhibition of human FAP B 7.62 pIC50 24 nM IC50 Bioorg. Med. Chem. Lett. (2007) 17: 507-510 [PMID:17055271]
ChEMBL Inhibition of human FAP using Z-Gly-Pro-AMC as substrate preincubated for 10 mins prior to substrate addition by fluorescence assay B 7.92 pIC50 12 nM IC50 J. Med. Chem. (2013) 56: 3467-3477 [PMID:23594271]
prolyl endopeptidase/Prolyl endopeptidase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3202] [GtoPdb: 2395] [UniProtKB: P48147]
ChEMBL Compound was tested in vitro for inhibition of Prolyl endopeptidase B 4.64 pIC50 23000 nM IC50 J. Med. Chem. (1996) 39: 2087-2094 [PMID:8642568]
ChEMBL Inhibition of prolyl oligopeptidase B 5.1 pIC50 7960 nM IC50 Bioorg. Med. Chem. Lett. (2007) 17: 507-510 [PMID:17055271]
ChEMBL Inhibition of human recombinant PREP expressed in Escherichia coli using Z-Gly-Pro-p-nitroanilide as substrate incubated for 15 mins prior to substrate addition B 6.01 pIC50 980 nM IC50 ACS Med. Chem. Lett. (2013) 4: 491-496 [PMID:24900696]
ChEMBL Inhibition of recombinant human PREP purified from Escherichia coli using Z-Gly-Pro-p-nitroanilide as substrate by spectrophotometry B 6.01 pIC50 980 nM IC50 J. Med. Chem. (2014) 57: 3053-3074 [PMID:24617858]
ChEMBL Binding affinity to PREP (unknown origin) B 6.01 pIC50 980 nM IC50 MedChemComm (2014) 5: 1700-1707
ChEMBL Inhibition of POP (unknown origin) B 6.01 pIC50 980 nM IC50 J Med Chem (2019) 62: 7874-7884 [PMID:31393718]
ChEMBL Inhibition of PREP (unknown origin) using AMC substrate by fluorometric assay B 6.01 pIC50 980 nM IC50 Bioorg Med Chem Lett (2021) 37: 127846-127846 [PMID:33571650]
ChEMBL Inhibition of human recombinant PREP expressed in Escherichia coli assessed as pNA release from Z-Gly-Pro-p-nitroanilide pre-incubated with enzyme for 15 mins prior to substrate addition by fluorescence technique B 6.01 pIC50 980 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 3412-3417 [PMID:22525314]
ChEMBL Inhibition of human PREP using Z-Gly-Pro-AMC as substrate preincubated for 10 mins prior to substrate addition by fluorescence assay B 7.14 pIC50 73 nM IC50 J. Med. Chem. (2013) 56: 3467-3477 [PMID:23594271]
fibroblast activation protein alpha/Seprase in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5769] [GtoPdb: 2365] [UniProtKB: P97321]
ChEMBL Inhibition of mouse recombinant FAP expressed in HEK293 cells using Ala-Pro-p-nitroanilide as substrate incubated for 15 mins prior to substrate addition B 7.15 pIC50 70 nM IC50 ACS Med. Chem. Lett. (2013) 4: 491-496 [PMID:24900696]
ChEMBL Inhibition of mouse recombinant FAP expressed in HEK293 cells assessed as pNA release from Ala-Pro-p-nitroanilide pre-incubated with enzyme for 15 mins prior to substrate addition by fluorescence technique B 7.18 pIC50 66 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 3412-3417 [PMID:22525314]
ChEMBL Inhibition of recombinant mouse FAP purified from HEK293 cell supernatant using Ala-Pro-p-nitroanilide as substrate by spectrophotometry B 7.18 pIC50 66 nM IC50 J. Med. Chem. (2014) 57: 3053-3074 [PMID:24617858]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]