ChEMBL ligand: CHEMBL67279 (PT-100, Talabostat, Valinyl-L-Boroproline)
Dipeptidyl-peptidase 7/Dipeptidyl peptidase II in Human [ChEMBL: CHEMBL3976] [GtoPdb: 1605] [UniProtKB: Q9UHL4] There should be some charts here, you may need to enable JavaScript!
dipeptidyl peptidase 4/Dipeptidyl peptidase IV in Human [ChEMBL: CHEMBL284] [GtoPdb: 1612] [UniProtKB: P27487] There should be some charts here, you may need to enable JavaScript!
dipeptidyl peptidase 9/Dipeptidyl peptidase IX in Human [ChEMBL: CHEMBL4793] [GtoPdb: 2357] [UniProtKB: Q86TI2] There should be some charts here, you may need to enable JavaScript!
dipeptidyl peptidase 8/Dipeptidyl peptidase VIII in Human [ChEMBL: CHEMBL4657] [GtoPdb: 2356] [UniProtKB: Q6V1X1] There should be some charts here, you may need to enable JavaScript!
fibroblast activation protein alpha/Fibroblast activation protein alpha in Human [ChEMBL: CHEMBL4683] [GtoPdb: 2365] [UniProtKB: Q12884] There should be some charts here, you may need to enable JavaScript!
prolyl endopeptidase/Prolyl endopeptidase in Human [ChEMBL: CHEMBL3202] [GtoPdb: 2395] [UniProtKB: P48147] There should be some charts here, you may need to enable JavaScript!
fibroblast activation protein alpha/Seprase in Mouse [ChEMBL: CHEMBL5769] [GtoPdb: 2365] [UniProtKB: P97321] There should be some charts here, you may need to enable JavaScript!

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	Binding affinity to DPP-4 (unknown origin) assessed as inhibition constant	B	9.74	pKi	0.18	nM	Ki	Bioorg Med Chem (2022) 63: 116748-116748 [PMID:35453036]
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)	B	7.66	pIC50	22	nM	IC50	Eur J Med Chem (2022) 240: 114543-114543 [PMID:35797897]
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 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 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 (unknown origin)	B	7.18	pKi	66	nM	Ki	Eur J Med Chem (2022) 240: 114543-114543 [PMID:35797897]
ChEMBL	Binding affinity to FAP (unknown origin) assessed as inhibition constant	B	8.3	pKi	5	nM	Ki	Bioorg Med Chem (2022) 63: 116748-116748 [PMID:35453036]
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 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]