alogliptin [Ligand Id: 6319] activity data from GtoPdb and ChEMBL
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: CHEMBL376359 (Alogliptin, Vipidia) |
|---|
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 | Inhibition of human DPP2 using Lys-Ala-AMC as substrate by fluorimetric analysis | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem (2012) 20: 5864-5883 [PMID:22938786] |
| ChEMBL | Inhibition of DPP2 (unknown origin) | B | 4 | pIC50 | >100000 | nM | IC50 | Medchemcomm (2014) 5: 1700-1707 |
| ChEMBL | Inhibition of QPP (unknown origin) preincubated for 30 mins followed by Nle-Pro-AMC addition measured for 50 mins by continuous fluorescence assay | B | 4 | pIC50 | >100000 | nM | IC50 | ACS Med Chem Lett (2016) 7: 498-501 [PMID:27190600] |
| 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 | 7.55 | pKd | 28.5 | 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 in human Caco2 cells using H-Ala-Pro-7-amido-4-trifluoromethylcoumarin as substrate after 1 hr by fluorescence assay | B | 7.62 | pIC50 | 24 | nM | IC50 | Bioorg Med Chem (2013) 21: 2795-2825 [PMID:23623674] |
| ChEMBL | Inhibition of human recombinant DPP-4 at 10 uM using Gly-Pro-Aminomethylcoumarin as substrate by Spectra max fluorometer analysis relative to control | B | 7.64 | pIC50 | 23 | nM | IC50 | Bioorg Med Chem (2021) 46: 116354-116354 [PMID:34428715] |
| ChEMBL | Inhibition of human DPP4 by fluorimetry | B | 8 | pIC50 | <10 | nM | IC50 | Eur J Med Chem (2009) 44: 3318-3322 [PMID:19375196] |
| ChEMBL | Inhibition of human DPP4 preincubated for 30 mins followed by Gly-Pro-AMC addition measured for 50 mins by continuous fluorescence assay | B | 8.12 | pIC50 | 7.6 | nM | IC50 | ACS Med Chem Lett (2016) 7: 498-501 [PMID:27190600] |
| ChEMBL | Inhibition of human DPP4 using Gly-Pro-AMC as substrate incubated for 30 mins by continuous fluorescent assay | B | 8.12 | pIC50 | 7.5 | nM | IC50 | Bioorg Med Chem Lett (2022) 76: 129018-129018 [PMID:36209967] |
| ChEMBL | Inhibition of human DPP4 | B | 8.15 | pIC50 | 7 | nM | IC50 | J Med Chem (2011) 54: 510-524 [PMID:21186796] |
| ChEMBL | Inhibition of human recombinant DPP4 pre-incubated with compound for 15 mins before substrate addition by luminescence assay | B | 8.15 | pIC50 | 7 | nM | IC50 | ACS Med Chem Lett (2014) 5: 921-926 [PMID:25147615] |
| ChEMBL | Inhibition of human recombinant DPP4 (39 to 766 residues) using Ala-Pro-AFC as substrate incubated for 1 hr by fluorescence assay | B | 8.15 | pIC50 | 7 | nM | IC50 | J Med Chem (2016) 59: 7466-7477 [PMID:27438064] |
| ChEMBL | Inhibition of DPP4 (unknown origin) | B | 8.15 | pIC50 | 7 | nM | IC50 | Eur J Med Chem (2020) 207: 112801-112801 [PMID:32927231] |
| ChEMBL | Inhibition of human DPP4 | B | 8.16 | pIC50 | 6.9 | nM | IC50 | Medchemcomm (2014) 5: 1700-1707 |
| ChEMBL | Inhibition of human recombinant DPP-4 using (H-Gly-Pro-AMC as substrate | B | 8.16 | pIC50 | 6.85 | nM | IC50 | Bioorg Med Chem (2021) 46: 116354-116354 [PMID:34428715] |
| ChEMBL | Inhibition of human recombinant DPP4 using Gly-Pro-7-amido-4-methyl-coumarin as substrate incubated for 15 mins by fluorescence assay | B | 8.28 | pIC50 | 5.3 | nM | IC50 | J Med Chem (2017) 60: 6480-6515 [PMID:28421763] |
| ChEMBL | Inhibition of recombinant human DPP4 expressed in baculovirus infected Sf9 insect cells using Gly-Pro-AMC as substrate preincubated for 15 mins followed by substrate addition measured at 60 secs interval for 20 mins by fluorometic method | B | 8.35 | pIC50 | 4.46 | nM | IC50 | Eur J Med Chem (2019) 180: 509-523 [PMID:31336309] |
| ChEMBL | Inhibition of DPP-4 (unknown origin) | B | 8.4 | pIC50 | 4 | nM | IC50 | Bioorg Med Chem (2021) 46: 116354-116354 [PMID:34428715] |
| ChEMBL | Inhibition of human DPP4 using A-P-7-amido-4-trifluoromethylcoumarin as substrate pretreated for 10 mins followed by substrate addition measured after 10 mins | B | 8.4 | pIC50 | 4 | nM | IC50 | Bioorg Med Chem (2018) 26: 903-912 [PMID:29373269] |
| ChEMBL | Inhibition of DPP4 in human Caco-2 cells using AP-AFC as substrate preincubated with enzyme for 10 mins followed by substrate addition and measured after 10 mins by fluorescence based analysis | B | 8.4 | pIC50 | 4 | nM | IC50 | Eur J Med Chem (2020) 208: 112850-112850 [PMID:32987315] |
| ChEMBL | Inhibition of DPP4 in human plasma using Gly-Pro-AMC as substrate by fluorimetric analysis | B | 8.4 | pIC50 | 4 | nM | IC50 | Bioorg Med Chem (2012) 20: 5864-5883 [PMID:22938786] |
| ChEMBL | Inhibition of DPP4 after 20 mins by fluorescence assay | B | 8.47 | pIC50 | 3.4 | nM | IC50 | Eur J Med Chem (2011) 46: 71-76 [PMID:21106276] |
| ChEMBL | Inhibition of human DPP4 after 10 mins | B | 8.47 | pIC50 | 3.4 | nM | IC50 | Eur J Med Chem (2012) 52: 205-212 [PMID:22475866] |
| GtoPdb | - | - | 8.5 | pIC50 | 3.4 | nM | IC50 | Eur J Med Chem (2012) 52: 205-12 [PMID:22475866] |
| ChEMBL | Inhibition of human recombinant DPP4 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 | 8.51 | pIC50 | 3.1 | nM | IC50 | Eur J Med Chem (2021) 225: 113765-113765 [PMID:34399391] |
| ChEMBL | Inhibition of recombinant human DPP4 expressed in baculovirus infected Sf9 insect cells using Gly-Pro-AMC as substrate measured at 60 secs interval for 20 mins by fluorescence assay | B | 8.57 | pIC50 | 2.7 | nM | IC50 | Bioorg Med Chem (2019) 27: 644-654 [PMID:30642693] |
| ChEMBL | Inhibition of human recombinant DPP-4 | B | 8.57 | pIC50 | 2.7 | nM | IC50 | Bioorg Med Chem (2021) 46: 116354-116354 [PMID:34428715] |
| ChEMBL | Inhibition of human recombinant DPP-4 | B | 8.59 | pIC50 | 2.6 | nM | IC50 | Bioorg Med Chem (2021) 46: 116354-116354 [PMID:34428715] |
| ChEMBL | Inhibition of DPP-4 (unknown origin) | B | 8.59 | pIC50 | 2.56 | nM | IC50 | Bioorg Med Chem (2021) 46: 116354-116354 [PMID:34428715] |
| ChEMBL | Inhibition of human DPP-4 using Gly-pro-AMC as substrate preincubated for 10 mins followed by substrate addition measured after 10 mins | B | 8.82 | pIC50 | 1.5 | nM | IC50 | Eur J Med Chem (2013) 68: 312-320 [PMID:23994324] |
| 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 | pIC50 | 1 | 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 (unknown origin) preincubated for 20 mins followed by Gly-Pro-AMC addition measured for 50 mins by continuous fluorescence assay | B | 4 | pIC50 | >100000 | nM | IC50 | ACS Med Chem Lett (2016) 7: 498-501 [PMID:27190600] |
| ChEMBL | Inhibition of DPP9 | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem (2012) 20: 5864-5883 [PMID:22938786] |
| ChEMBL | Inhibition of human recombinant DPP9 pre-incubated with compound for 15 mins before substrate addition by luminescence assay | B | 4 | pIC50 | >100000 | nM | IC50 | ACS Med Chem Lett (2014) 5: 921-926 [PMID:25147615] |
| ChEMBL | Inhibition of DPP9 (unknown origin) | B | 4 | pIC50 | >100000 | nM | IC50 | Medchemcomm (2014) 5: 1700-1707 |
| ChEMBL | Inhibition of DPP9 (unknown origin) | B | 4.3 | pIC50 | >50000 | nM | IC50 | Eur J Med Chem (2020) 208: 112850-112850 [PMID:32987315] |
| ChEMBL | Inhibition of DPP9 after 20 mins by fluorescence assay | B | 4.6 | pIC50 | >25000 | nM | IC50 | Eur J Med Chem (2011) 46: 71-76 [PMID:21106276] |
| ChEMBL | Inhibition of DPP9 | B | 4.6 | pIC50 | >25000 | nM | IC50 | Eur J Med Chem (2012) 52: 205-212 [PMID:22475866] |
| 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 | 7 | pIC50 | >100 | 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 recombinant DPP8 (unknown origin) preincubated for 20 mins followed by Ala-Pro-AFC addition measured for 40 mins by continuous fluorescence assay | B | 4 | pIC50 | >100000 | nM | IC50 | ACS Med Chem Lett (2016) 7: 498-501 [PMID:27190600] |
| ChEMBL | Inhibition of human DPP8 | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2011) 54: 510-524 [PMID:21186796] |
| ChEMBL | Inhibition of DPP8 | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem (2012) 20: 5864-5883 [PMID:22938786] |
| ChEMBL | Inhibition of human recombinant DPP8 pre-incubated with compound for 15 mins before substrate addition by luminescence assay | B | 4 | pIC50 | >100000 | nM | IC50 | ACS Med Chem Lett (2014) 5: 921-926 [PMID:25147615] |
| ChEMBL | Inhibition of DPP8 (unknown origin) | B | 4 | pIC50 | >100000 | nM | IC50 | Medchemcomm (2014) 5: 1700-1707 |
| ChEMBL | Inhibition of DPP8 (unknown origin) | B | 4.3 | pIC50 | >50000 | nM | IC50 | Eur J Med Chem (2020) 208: 112850-112850 [PMID:32987315] |
| ChEMBL | Inhibition of DPP8 after 20 mins by fluorescence assay | B | 4.6 | pIC50 | >25000 | nM | IC50 | Eur J Med Chem (2011) 46: 71-76 [PMID:21106276] |
| ChEMBL | Inhibition of DPP8 | B | 4.6 | pIC50 | >25000 | nM | IC50 | Eur J Med Chem (2012) 52: 205-212 [PMID:22475866] |
| 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 | 7 | pIC50 | >100 | 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 FAPalpha | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem (2012) 20: 5864-5883 [PMID:22938786] |
| ChEMBL | Inhibition of FAP (unknown origin) | B | 4 | pIC50 | >100000 | nM | IC50 | Medchemcomm (2014) 5: 1700-1707 |
| ChEMBL | Inhibition of FAP (unknown origin) preincubated for 20 mins followed by Nle-Pro-AMC addition measured for 40 mins by continuous fluorescence assay | B | 4 | pIC50 | >100000 | nM | IC50 | ACS Med Chem Lett (2016) 7: 498-501 [PMID:27190600] |
| prolyl endopeptidase/Prolyl endopeptidase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3202] [GtoPdb: 2395] [UniProtKB: P48147] | ||||||||
| ChEMBL | Inhibition of PREP (unknown origin) | B | 4 | pIC50 | >100000 | nM | IC50 | Medchemcomm (2014) 5: 1700-1707 |
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]
