Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
ChEMBL ligand: CHEMBL67279 (PT-100, Talabostat, Valinyl-L-Boroproline) |
---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
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]