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, Vitagliptin) |
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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 | 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 | Inhibitory concentration against dipeptidylpeptidase 2 | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 687-691 [PMID:15664838] |
| 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 | 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 | 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 DPP2 | B | 4.7 | pIC50 | >20000 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 1908-1912 [PMID:19269819] |
| ChEMBL | Inhibition of human DPP2 | B | 4.7 | pIC50 | >20000 | nM | IC50 | Bioorg Med Chem (2009) 17: 2388-2399 [PMID:19261480] |
| 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 | 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 DPP4 (unknown origin) | B | 5.46 | pIC50 | 3500 | nM | IC50 | Bioorg Med Chem (2020) 28: 115263-115263 [PMID:32008883] |
| ChEMBL | Inhibition of DPP4 | B | 6.92 | pIC50 | 120 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 4154-4158 [PMID:18556199] |
| ChEMBL | Inhibition of DPP4 | B | 6.92 | pIC50 | 120 | nM | IC50 | J Med Chem (2011) 54: 5737-5746 [PMID:21711053] |
| 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 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 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 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 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 | Inhibition of human DPP4 | B | 7.29 | pIC50 | 51 | nM | IC50 | Bioorg Med Chem (2009) 17: 2388-2399 [PMID:19261480] |
| 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 | Inhibition of DPP4 | B | 7.29 | pIC50 | 51 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 3596-3600 [PMID:20483603] |
| ChEMBL | Inhibitory activity against DPP4 | B | 7.29 | pIC50 | 51 | nM | IC50 | J Med Chem (2006) 49: 373-380 [PMID:16392822] |
| 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 | 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 | 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 | 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 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 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 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 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 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 | 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 | Bioorg Med Chem Lett (2008) 18: 4154-4158 [PMID:18556199] |
| 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 | 6.64 | 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 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 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) | 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 | 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 | 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 (unknown origin) | B | 5.05 | pIC50 | 9000 | nM | IC50 | Eur J Med Chem (2017) 139: 482-491 [PMID:28826083] |
| ChEMBL | Inhibition of DPP8 | B | 5.42 | pIC50 | 3820 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 3565-3568 [PMID:20488702] |
| GtoPdb | - | - | 5.66 | pIC50 | 2200 | nM | IC50 | ChemMedChem (2022) 17: e202200097 [PMID:35760756] |
| 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) 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 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 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 | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 3596-3600 [PMID:20483603] |
| 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 FAP (unknown origin) | B | 4.14 | pIC50 | 73000 | nM | IC50 | Medchemcomm (2014) 5: 1700-1707 |
| ChEMBL | Inhibition of human FAP | B | 4.7 | pIC50 | >20000 | nM | IC50 | Bioorg Med Chem (2009) 17: 2388-2399 [PMID:19261480] |
| 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] |
| 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] |
| 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 |
| 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 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]
