vildagliptin [Ligand Id: 6310] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL142703 (Galvus, LAF 237, LAF-237, LAF237, NVP-LAF 237, NVP-LAF237, Vildagliptin, Vildagliptina, Vildagliptine, Vitagliptin, Xiliarx) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Dipeptidyl peptidase 9 in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4295538] [UniProtKB: E1BI31] | ||||||||
| ChEMBL | Inhibition of bovine DPP9 | B | 6.17 | pIC50 | 680 | nM | IC50 | Eur J Med Chem (2017) 139: 482-491 [PMID:28826083] |
| Dipeptidyl-peptidase 7/Dipeptidyl peptidase II in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3976] [GtoPdb: 1605] [UniProtKB: Q9UHL4] | ||||||||
| ChEMBL | Inhibition of DPP7 (unknown origin) expressed in baculovirus expression system using Nle-Pro-AMC as substrate by continuous fluorometric assay | B | 4 | pIC50 | >100000 | nM | IC50 | Eur J Med Chem (2014) 86: 242-256 [PMID:25164763] |
| ChEMBL | Inhibition of DPP2 (unknown origin) | B | 4 | pIC50 | >100000 | nM | IC50 | Medchemcomm (2014) 5: 1700-1707 |
| ChEMBL | Inhibitory concentration against DPP-II [Quiescent cell proline dipeptidase] or DPP-VII | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 3271-3275 [PMID:15927466] |
| ChEMBL | Inhibitory activity against DPP2 | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2006) 49: 373-380 [PMID:16392822] |
| ChEMBL | Inhibitory concentration against dipeptidylpeptidase 2 | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 687-691 [PMID:15664838] |
| ChEMBL | Inhibitory activity against quiescent cell prolyl peptidase (QPP). | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 43-46 [PMID:14684294] |
| ChEMBL | Inhibition of DPP2 | B | 4.3 | pIC50 | >50000 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 3596-3600 [PMID:20483603] |
| ChEMBL | Inhibition of human recombinant His-tagged DPP2 expressed in insect cells | B | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (2010) 53: 6572-6583 [PMID:20718420] |
| ChEMBL | Inhibition of human DPP2 | B | 4.7 | pIC50 | >20000 | nM | IC50 | Bioorg Med Chem (2009) 17: 2388-2399 [PMID:19261480] |
| ChEMBL | Inhibition of DPP2 | B | 4.7 | pIC50 | >20000 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 1908-1912 [PMID:19269819] |
| ChEMBL | Inhibition of DPP2 (unknown origin) | B | 5.3 | pIC50 | >5000 | nM | IC50 | J Med Chem (2023) 66: 12717-12738 [PMID:37721854] |
| Dipeptidyl peptidase IV in Porphyromonas gingivalis (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4295559] [UniProtKB: O31048] | ||||||||
| ChEMBL | Inhibition of Porphyromonas gingivalis N-terminal His-tagged DPP4 expressed in Escherichia coli using Gly-Pro-p-nitroanilide as substrate preincubated for 15 mins | B | 7.77 | pKi | 17 | nM | Ki | Eur J Med Chem (2017) 139: 482-491 [PMID:28826083] |
| ChEMBL | Inhibition of Porphyromonas gingivalis N-terminal His-tagged DPP4 expressed in Escherichia coli using Gly-Pro-p-nitroanilide as substrate | B | 5.89 | pIC50 | 1300 | nM | IC50 | Eur J Med Chem (2017) 139: 482-491 [PMID:28826083] |
| 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 | 7.97 | pKd | 10.7 | 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 | 8.62 | pKd | 2.4 | nM | Kd | J Med Chem (2016) 59: 7466-7477 [PMID:27438064] |
| ChEMBL | Inhibition of DPP4 | B | 4.77 | pKi | 17000 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 4154-4158 [PMID:18556199] |
| GtoPdb | - | - | 7.8 | pKi | 17 | nM | Ki | Curr Drug Targets (2009) 10: 71-87 [PMID:19149538] |
| ChEMBL | Binding affinity to human DPP-4 using gly-pro-pNA as substrate assessed as inhibition constant | B | 7.89 | pKi | 13 | nM | Ki | J Med Chem (2023) 66: 11593-11631 [PMID:37647598] |
| ChEMBL | Inhibition of human DPP4 expressed in Caco-2 cells | B | 8.4 | pKi | 4 | nM | Ki | J Med Chem (2006) 49: 6416-6420 [PMID:17034148] |
| ChEMBL | Inhibition of DPP4 in human plasma using Gly-Pro-AMC as substrate by fluorimetric analysis | B | 8.52 | pKi | 3 | nM | Ki | Bioorg Med Chem (2012) 20: 5864-5883 [PMID:22938786] |
| ChEMBL | Inhibition of human recombinant DPP-4 using Gly-Pro-7-amido-4-methylcoumarin as substrate | B | 4.62 | pIC50 | 24000 | nM | IC50 | J Med Chem (2023) 66: 11593-11631 [PMID:37647598] |
| ChEMBL | Inhibition of DPP4 (unknown origin) | B | 5.46 | pIC50 | 3500 | nM | IC50 | Bioorg Med Chem (2020) 28: 115263-115263 [PMID:32008883] |
| ChEMBL | Inhibition of DPP4 (unknown origin) | B | 6.92 | pIC50 | 120 | nM | IC50 | Eur J Med Chem (2022) 240: 114543-114543 [PMID:35797897] |
| ChEMBL | Inhibition of DPP4 | B | 6.92 | pIC50 | 120 | nM | IC50 | J Med Chem (2011) 54: 5737-5746 [PMID:21711053] |
| ChEMBL | Inhibition of DPP4 | B | 6.92 | pIC50 | 120 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 4154-4158 [PMID:18556199] |
| 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 | 6.92 | pIC50 | 120 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 3412-3417 [PMID:22525314] |
| ChEMBL | Inhibition of human DPP4 | B | 6.92 | pIC50 | 120 | nM | IC50 | Eur J Med Chem (2017) 139: 482-491 [PMID:28826083] |
| ChEMBL | Inhibition of human recombinant DPP4 (39 to 766 residues) using Ala-Pro-AFC as substrate incubated for 1 hr by fluorescence assay | B | 7.02 | pIC50 | 95 | nM | IC50 | J Med Chem (2016) 59: 7466-7477 [PMID:27438064] |
| ChEMBL | Inhibition of human recombinant DPP4 expressed in baculovirus expression system using Ala-Pro-AMC as substrate by continuous fluorometric assay | B | 7.15 | pIC50 | 70 | nM | IC50 | Eur J Med Chem (2014) 86: 242-256 [PMID:25164763] |
| ChEMBL | Inhibition of DPP4 (unknown origin) | B | 7.15 | pIC50 | 70 | nM | IC50 | Eur J Med Chem (2018) 157: 527-561 [PMID:30119011] |
| 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 | 7.21 | pIC50 | 62 | nM | IC50 | Bioorg Med Chem (2013) 21: 2795-2825 [PMID:23623674] |
| ChEMBL | Inhibition of human recombinant DPP-4 expressed in human Caco-2 cells using H-Ala-Pro-7-amido-4-trifluoromethylcoumarin as substrate measured after 1 hrs by fluorescence based assay | B | 7.21 | pIC50 | 62 | nM | IC50 | J Med Chem (2023) 66: 11593-11631 [PMID:37647598] |
| ChEMBL | Inhibition of human recombinant His-tagged DPP4 expressed in insect cells | B | 7.25 | pIC50 | 56 | nM | IC50 | J Med Chem (2010) 53: 6572-6583 [PMID:20718420] |
| ChEMBL | Inhibition of DPP4 | B | 7.25 | pIC50 | 56 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 1908-1912 [PMID:19269819] |
| ChEMBL | Inhibitory concentration against dipeptidylpeptidase IV | B | 7.29 | pIC50 | 51 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 687-691 [PMID:15664838] |
| ChEMBL | Inhibitory concentration against Dipeptidylpeptidase IV [DPP-IV] | B | 7.29 | pIC50 | 51 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 3271-3275 [PMID:15927466] |
| ChEMBL | Inhibitory activity against DPP4 | B | 7.29 | pIC50 | 51 | nM | IC50 | J Med Chem (2006) 49: 373-380 [PMID:16392822] |
| ChEMBL | Inhibition of human DPP4 | B | 7.29 | pIC50 | 51 | nM | IC50 | Bioorg Med Chem (2009) 17: 2388-2399 [PMID:19261480] |
| ChEMBL | Inhibition of DPP4 | B | 7.29 | pIC50 | 51 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 3596-3600 [PMID:20483603] |
| ChEMBL | Inhibition of human DPP4 using Gly-Pro-AMC as substrate incubated for 30 mins by continuous fluorescent assay | B | 7.47 | pIC50 | 34 | nM | IC50 | Bioorg Med Chem Lett (2022) 76: 129018-129018 [PMID:36209967] |
| ChEMBL | Inhibition of human recombinant DPP-4 (1 to 530 residues) using Gly-Pro-AMC as substrate preincubated for 30 mins followed by substrate addition measured after 5 mins by CF assay | B | 7.47 | pIC50 | 34 | nM | IC50 | J Med Chem (2023) 66: 11593-11631 [PMID:37647598] |
| ChEMBL | Inhibition of DPP4 | B | 7.47 | pIC50 | 34 | nM | IC50 | Bioorg Med Chem (2009) 17: 1783-1802 [PMID:19217790] |
| ChEMBL | Inhibitory activity against dipeptidylpeptidase IV. | B | 7.47 | pIC50 | 34 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 43-46 [PMID:14684294] |
| ChEMBL | Inhibition of human DPP4 | B | 7.64 | pIC50 | 23 | nM | IC50 | Medchemcomm (2014) 5: 1700-1707 |
| ChEMBL | Inhibition of 6xHis-tagged recombinant human DPP4 expressed in baculovirus expression system assessed as hydrolysis of Ala-Pro-aminomethylcoumarin by fluorometric assay | B | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem (2013) 21: 7418-7429 [PMID:24153396] |
| ChEMBL | Inhibition of DPP4 in presence of 50% human serum | B | 7.77 | pIC50 | 17 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 3596-3600 [PMID:20483603] |
| ChEMBL | Inhibition of human DPP4 by fluorimetry | B | 7.78 | pIC50 | 16.6 | nM | IC50 | Eur J Med Chem (2009) 44: 3318-3322 [PMID:19375196] |
| ChEMBL | Inhibition of DPP4 in presence of 50% rat serum | B | 7.8 | pIC50 | 16 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 3596-3600 [PMID:20483603] |
| ChEMBL | Inhibition of DPP4 in human serum assessed as decrease in p-nitroaniline formation using Gly-Pro-p-nitroanilide as substrate preincubated for 5 mins followed by incubation with substrate for 15 mins by microplate reader analysis | B | 7.82 | pIC50 | 15 | nM | IC50 | Eur J Med Chem (2020) 185: 111808-111808 [PMID:31683103] |
| GtoPdb | - | - | 8 | pIC50 | 10 | nM | IC50 | ChemMedChem (2022) 17: e202200097 [PMID:35760756] |
| ChEMBL | Inhibition of DPP4 (unknown origin) | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (2023) 66: 12717-12738 [PMID:37721854] |
| ChEMBL | Inhibition of DPP4 (unknown origin) | B | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 731-736 [PMID:24439847] |
| ChEMBL | Inhibition of DPP4 | B | 8.05 | pIC50 | 9 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 3565-3568 [PMID:20488702] |
| ChEMBL | Inhibitory concentration against dipeptidylpeptidase IV | B | 8.46 | pIC50 | 3.5 | nM | IC50 | J Med Chem (2004) 47: 4135-4141 [PMID:15293982] |
| ChEMBL | Inhibition of DPP-4 in human Caco-2 cells using H-Ala-Pro-pNA as substrate preincubated for 30 mins followed by substrate addition measured after 10 mins by fluorescence based assay | B | 8.46 | pIC50 | 3.5 | nM | IC50 | J Med Chem (2023) 66: 11593-11631 [PMID:37647598] |
| ChEMBL | Inhibition of DPP4 | B | 8.46 | pIC50 | 3.5 | nM | IC50 | Eur J Med Chem (2009) 44: 3318-3322 [PMID:19375196] |
| ChEMBL | Inhibition of DPP4 (unknown origin) | B | 8.46 | pIC50 | 3.5 | nM | IC50 | J Med Chem (2014) 57: 2197-2212 [PMID:24099035] |
| ChEMBL | Inhibition of human DPP4 expressed in baculovirus expression system using Gly-Pro-AMC substrate incubated or 30 mins by fluorescence based assay | B | 8.49 | pIC50 | 3.2 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 3516-3521 [PMID:22503246] |
| ChEMBL | Inhibition of human purified His-tagged DPP-4 assessed as cleavage of substrate using Gly-Pro-AMC chromogenic substrate after 60 mins by fluorescence spectrophotometry | B | 8.52 | pIC50 | 3 | nM | IC50 | Bioorg Med Chem (2013) 21: 5679-5687 [PMID:23938053] |
| 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 DPP4 in human plasma assessed as formation of 7-amino-4-methylcoumarin from glycyl-L-proline 4-methylcoumaryl-7-amide by fluorescence assay | B | 9.24 | pIC50 | 0.58 | nM | IC50 | Bioorg Med Chem (2011) 19: 5490-5499 [PMID:21865048] |
| dipeptidyl peptidase 4/Dipeptidyl peptidase IV in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3883] [GtoPdb: 1612] [UniProtKB: P28843] | ||||||||
| ChEMBL | Inhibition of mouse DPP-4 using Gly-Pro-AMC as substrate measured after 5 mins by CF assay | B | 7.59 | pIC50 | 26 | nM | IC50 | J Med Chem (2023) 66: 11593-11631 [PMID:37647598] |
| dipeptidyl peptidase 9/Dipeptidyl peptidase IX in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4793] [GtoPdb: 2357] [UniProtKB: Q86TI2] | ||||||||
| ChEMBL | Inhibition of DPP9 | B | 7.02 | pKi | 95 | nM | Ki | Bioorg Med Chem (2012) 20: 5864-5883 [PMID:22938786] |
| ChEMBL | Binding affinity to DPP-9 (unknown origin) assessed as inhibition constant | B | 7.02 | pKi | 95 | nM | Ki | J Med Chem (2023) 66: 11593-11631 [PMID:37647598] |
| ChEMBL | Inhibition of C-terminal hexa his-tagged human recombinant DPP-9 (1 to 863 residues) expressed in Pichia pastoris using H-Gly-Pro-AMC as substrate assessed as inhibition constant measured after 3 hrs by fluorescence based assay | B | 7.02 | pKi | 95 | nM | Ki | J Med Chem (2023) 66: 11593-11631 [PMID:37647598] |
| ChEMBL | Inhibition of DPP9 | B | 7.17 | pKi | 68 | nM | Ki | J Med Chem (2006) 49: 6416-6420 [PMID:17034148] |
| ChEMBL | Inhibition of DPP9 | B | 5.92 | pIC50 | 1200 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 3596-3600 [PMID:20483603] |
| ChEMBL | Inhibition of human recombinant His-tagged DPP9 expressed in insect cells | B | 5.92 | pIC50 | 1200 | nM | IC50 | J Med Chem (2010) 53: 6572-6583 [PMID:20718420] |
| ChEMBL | Inhibition of DPP9 | B | 6.17 | pIC50 | 680 | nM | IC50 | J Med Chem (2011) 54: 5737-5746 [PMID:21711053] |
| ChEMBL | Inhibition of DPP9 | B | 6.17 | pIC50 | 680 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 4154-4158 [PMID:18556199] |
| ChEMBL | Inhibition of DPP9 (unknown origin) | B | 6.64 | pIC50 | 230 | nM | IC50 | J Med Chem (2023) 66: 12717-12738 [PMID:37721854] |
| ChEMBL | Inhibition of DPP9 | B | 6.64 | pIC50 | 230 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 3565-3568 [PMID:20488702] |
| GtoPdb | - | - | 6.64 | pIC50 | 230 | nM | IC50 | ChemMedChem (2022) 17: e202200097 [PMID:35760756] |
| ChEMBL | Inhibition of 6xHis-tagged recombinant DPP9 (unknown origin) expressed in baculovirus expression system assessed as hydrolysis of Ala-Pro-aminomethylcoumarin preincubated for 20 mins followed by Gly-PropNA3 Tos addition measured after 90 mins by fluorometric assay | B | 6.7 | pIC50 | 200 | nM | IC50 | Bioorg Med Chem (2013) 21: 7418-7429 [PMID:24153396] |
| ChEMBL | Inhibition of DPP9 (unknown origin) expressed in baculovirus expression system using Ala-Pro-AMC as substrate by continuous fluorometric assay | B | 6.7 | pIC50 | 200 | nM | IC50 | Eur J Med Chem (2014) 86: 242-256 [PMID:25164763] |
| ChEMBL | Inhibition of DPP9 (unknown origin) | B | 7.1 | pIC50 | 80 | nM | IC50 | Medchemcomm (2014) 5: 1700-1707 |
| ChEMBL | Inhibition of human purified His-tagged DPP-9 assessed as cleavage of substrate using Gly-Pro-AMC chromogenic substrate after 60 mins by fluorescence spectrophotometry | B | 7.18 | pIC50 | 66 | nM | IC50 | Bioorg Med Chem (2013) 21: 5679-5687 [PMID:23938053] |
| ChEMBL | Inhibition of human recombinant DPP9 using Gly-Pro-AMC as substrate preincubated for 15 mins followed by substrate addition and measured for 20 mins by fluorescence based microplate reader assay | B | 9.92 | pIC50 | 0.12 | nM | IC50 | Eur J Med Chem (2021) 225: 113765-113765 [PMID:34399391] |
| dipeptidyl peptidase 8/Dipeptidyl peptidase VIII in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4657] [GtoPdb: 2356] [UniProtKB: Q6V1X1] | ||||||||
| ChEMBL | Inhibition of DPP8 | B | 5.87 | pKi | 1342 | nM | Ki | J Med Chem (2006) 49: 6416-6420 [PMID:17034148] |
| ChEMBL | Inhibition of DPP8 | B | 6.09 | pKi | 810 | nM | Ki | Bioorg Med Chem (2012) 20: 5864-5883 [PMID:22938786] |
| ChEMBL | Binding affinity to DPP-8 (unknown origin) assessed as inhibition constant | B | 6.09 | pKi | 810 | nM | Ki | J Med Chem (2023) 66: 11593-11631 [PMID:37647598] |
| ChEMBL | Inhibition of C-terminal V5 epitope hexa his-tagged human recombinant DPP-8 (1 to 882 residues) expressed in Sf9 cells using H-Gly-Pro-AMC as substrate assessed as inhibition constant measured after 3 hrs by fluorescence based assay | B | 6.09 | pKi | 810 | nM | Ki | J Med Chem (2023) 66: 11593-11631 [PMID:37647598] |
| ChEMBL | Inhibitory concentration against dipeptidylpeptidase 8 | B | 4.85 | pIC50 | 14219 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 687-691 [PMID:15664838] |
| ChEMBL | Inhibitory activity against DPP8 | B | 4.85 | pIC50 | 14219 | nM | IC50 | J Med Chem (2006) 49: 373-380 [PMID:16392822] |
| ChEMBL | Inhibitory concentration against Dipeptidylpeptidase 8 | B | 4.85 | pIC50 | 14219 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 3271-3275 [PMID:15927466] |
| ChEMBL | Inhibition of DPP8 | B | 4.85 | pIC50 | 14200 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 3596-3600 [PMID:20483603] |
| ChEMBL | Inhibition of human recombinant His-tagged DPP8 expressed in insect cells | B | 4.85 | pIC50 | 14000 | nM | IC50 | J Med Chem (2010) 53: 6572-6583 [PMID:20718420] |
| ChEMBL | Inhibition of DPP8 | B | 4.85 | pIC50 | 14000 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 1908-1912 [PMID:19269819] |
| ChEMBL | Inhibition of human DPP8 | B | 4.85 | pIC50 | 14000 | nM | IC50 | Bioorg Med Chem (2009) 17: 2388-2399 [PMID:19261480] |
| ChEMBL | Inhibition of DPP8 (unknown origin) | B | 5.05 | pIC50 | 9000 | nM | IC50 | Eur J Med Chem (2017) 139: 482-491 [PMID:28826083] |
| ChEMBL | Inhibition of DPP8 | B | 5.05 | pIC50 | 9000 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 4154-4158 [PMID:18556199] |
| ChEMBL | Inhibition of DPP8 | B | 5.05 | pIC50 | 9000 | nM | IC50 | J Med Chem (2011) 54: 5737-5746 [PMID:21711053] |
| ChEMBL | Inhibition of DPP8 | B | 5.42 | pIC50 | 3820 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 3565-3568 [PMID:20488702] |
| ChEMBL | Inhibition of DPP8 (unknown origin) | B | 5.66 | pIC50 | 2200 | nM | IC50 | J Med Chem (2023) 66: 12717-12738 [PMID:37721854] |
| GtoPdb | - | - | 5.66 | pIC50 | 2200 | nM | IC50 | ChemMedChem (2022) 17: e202200097 [PMID:35760756] |
| ChEMBL | Inhibition of DPP8 (unknown origin) expressed in baculovirus expression system using Ala-Pro-AMC as substrate by continuous fluorometric assay | B | 5.71 | pIC50 | 1960 | nM | IC50 | Eur J Med Chem (2014) 86: 242-256 [PMID:25164763] |
| ChEMBL | Inhibition of 6xHis-tagged recombinant DPP8 (unknown origin) expressed in baculovirus expression system assessed as hydrolysis of Ala-Pro-aminomethylcoumarin preincubated for 20 mins followed by Gly-PropNA3 Tos addition measured after 90 mins by fluorometric assay | B | 5.71 | pIC50 | 1960 | nM | IC50 | Bioorg Med Chem (2013) 21: 7418-7429 [PMID:24153396] |
| ChEMBL | Inhibition of DPP8 (unknown origin) | B | 5.85 | pIC50 | 1400 | nM | IC50 | Medchemcomm (2014) 5: 1700-1707 |
| ChEMBL | Inhibition of human purified His-tagged DPP-8 assessed as cleavage of substrate using Gly-Pro-AMC chromogenic substrate after 60 mins by fluorescence spectrophotometry | B | 5.96 | pIC50 | 1100 | nM | IC50 | Bioorg Med Chem (2013) 21: 5679-5687 [PMID:23938053] |
| ChEMBL | Inhibition of human recombinant DPP8 using Gly-Pro-AMC as substrate preincubated for 15 mins followed by substrate addition and measured for 20 mins by fluorescence based microplate reader assay | B | 8.73 | pIC50 | 1.85 | nM | IC50 | Eur J Med Chem (2021) 225: 113765-113765 [PMID:34399391] |
| fibroblast activation protein alpha/Fibroblast activation protein alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4683] [GtoPdb: 2365] [UniProtKB: Q12884] | ||||||||
| ChEMBL | Inhibition of FAP | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 3596-3600 [PMID:20483603] |
| ChEMBL | Inhibition of human recombinant FAP expressed in Hi5 insect cells | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2010) 53: 6572-6583 [PMID:20718420] |
| ChEMBL | Inhibition of FAP in human U87MG cells using Suc-Gly-Pro-AMC as substrate by fluorescence based assay | B | 4.1 | pIC50 | 79760 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127253-127253 [PMID:32527554] |
| ChEMBL | Inhibition of human recombinant FAPalpha expressed in baculovirus expression system using Ala-Pro-7-amido-4-trifluoromethylcoumarin as substrate by fluorescence based assay | B | 4.14 | pIC50 | 73000 | nM | IC50 | J Med Chem (2023) 66: 11593-11631 [PMID:37647598] |
| ChEMBL | Inhibition of FAP (unknown origin) | B | 4.14 | pIC50 | 73000 | nM | IC50 | Medchemcomm (2014) 5: 1700-1707 |
| ChEMBL | Inhibition of FAP (unknown origin) | B | 4.28 | pIC50 | 52000 | nM | IC50 | Eur J Med Chem (2022) 240: 114543-114543 [PMID:35797897] |
| ChEMBL | Inhibition of human FAP | B | 4.7 | pIC50 | >20000 | nM | IC50 | Bioorg Med Chem (2009) 17: 2388-2399 [PMID:19261480] |
| ChEMBL | Inhibition of FAP (unknown origin) expressed in baculovirus expression system using Nle-Pro-AMC as substrate by continuous fluorometric assay | B | 5.43 | pIC50 | 3720 | nM | IC50 | Eur J Med Chem (2014) 86: 242-256 [PMID:25164763] |
| ChEMBL | Inhibition of 6xHis-tagged recombinant FAP (unknown origin) expressed in baculovirus expression system assessed as hydrolysis of Nle-Pro-aminomethylcoumarin after 20 mins by fluorometric assay | B | 5.43 | pIC50 | 3720 | nM | IC50 | Bioorg Med Chem (2013) 21: 7418-7429 [PMID:24153396] |
| Glomulin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5465342] [UniProtKB: Q92990] | ||||||||
| ChEMBL | Inhibition of FAP (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2023) 66: 12717-12738 [PMID:37721854] |
| prolyl endopeptidase/Prolyl endopeptidase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3202] [GtoPdb: 2395] [UniProtKB: P48147] | ||||||||
| 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 | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 3412-3417 [PMID:22525314] |
| ChEMBL | Inhibition of PREP (unknown origin) | B | 4.3 | pIC50 | >50000 | nM | IC50 | Medchemcomm (2014) 5: 1700-1707 |
| ChEMBL | Inhibition of PREP (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2023) 66: 12717-12738 [PMID:37721854] |
| 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 assessed as pNA release from Ala-Pro-p-nitroanilide pre-incubated with enzyme for 15 mins prior to substrate addition by fluorescence technique | B | 4.28 | pIC50 | 52000 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 3412-3417 [PMID:22525314] |
| TRPV4 in Human [GtoPdb: 510] [UniProtKB: Q9HBA0] | ||||||||
| GtoPdb | - | - | 3 | pEC50 | 1000000 | nM | EC50 | Hypertension (2020) 75: 150-162 [PMID:31735085] |
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]
