alogliptin [Ligand Id: 6319] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL376359 (Alogliptin, Vipidia) |
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| 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 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 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 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 DPP4 | B | 8.16 | pIC50 | 6.9 | nM | IC50 | Medchemcomm (2014) 5: 1700-1707 |
| 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 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 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 human DPP4 after 10 mins | B | 8.47 | pIC50 | 3.4 | nM | IC50 | Eur J Med Chem (2012) 52: 205-212 [PMID:22475866] |
| 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] |
| 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 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 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]
