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	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 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]