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: CHEMBL385517 (BMS-477118, BMS-477118-11, Saxagliptin) |
---|
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 | 4.52 | pIC50 | >30000 | nM | IC50 | Bioorg Med Chem (2012) 20: 5864-5883 [PMID:22938786] |
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 | 7.8 | pKd | 15.9 | 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 | 9.52 | pKd | 0.3 | nM | Kd | J Med Chem (2016) 59: 7466-7477 [PMID:27438064] |
GtoPdb | - | - | 9.2 | pKi | 0.6 | nM | Ki | Curr Drug Targets (2009) 10: 71-87 [PMID:19149538] |
ChEMBL | In vitro inhibition constant against human Dipeptidyl peptidase IV | B | 9.22 | pKi | 0.6 | nM | Ki | J Med Chem (2005) 48: 5025-5037 [PMID:16033281] |
ChEMBL | Inhibition of human DPP4 expressed in Caco-2 cells | B | 9.22 | pKi | 0.6 | nM | Ki | J Med Chem (2006) 49: 6416-6420 [PMID:17034148] |
ChEMBL | Inhibition of human DPP4 | B | 9.22 | pKi | 0.6 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 6476-6480 [PMID:17937986] |
ChEMBL | Inhibition of human DPP4 | B | 9.22 | pKi | 0.6 | nM | Ki | Bioorg Med Chem (2009) 17: 1783-1802 [PMID:19217790] |
ChEMBL | Inhibition of DPP4 | B | 9.22 | pKi | 0.6 | nM | Ki | Eur J Med Chem (2009) 44: 3318-3322 [PMID:19375196] |
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 | 7.3 | pIC50 | 50 | nM | IC50 | Bioorg Med Chem (2013) 21: 2795-2825 [PMID:23623674] |
ChEMBL | Inhibition of DPP4 (unknown origin) | B | 7.3 | pIC50 | 50 | nM | IC50 | J Med Chem (2014) 57: 2197-2212 [PMID:24099035] |
ChEMBL | Inhibition of human recombinant DPP-4 using H-Gly-Pro-AMC as substrate after 10 mins by fluorescence assay | B | 7.52 | pIC50 | 30.3 | nM | IC50 | Bioorg Med Chem (2014) 22: 1383-1393 [PMID:24457090] |
ChEMBL | Inhibition of DPP4 | B | 8.47 | pIC50 | 3.4 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 3596-3600 [PMID:20483603] |
ChEMBL | Inhibition of DPP4 in human plasma using Gly-Pro-AMC as substrate by fluorimetric analysis | B | 8.47 | pIC50 | 3.37 | nM | IC50 | Bioorg Med Chem (2012) 20: 5864-5883 [PMID:22938786] |
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 | B | 9.22 | pIC50 | 0.6 | nM | IC50 | J Med Chem (2011) 54: 5737-5746 [PMID:21711053] |
dipeptidyl peptidase 9/Dipeptidyl peptidase IX in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4793] [GtoPdb: 2357] [UniProtKB: Q86TI2] | ||||||||
ChEMBL | Inhibition of DPP9 | B | 7.15 | pKi | 71 | nM | Ki | J Med Chem (2006) 49: 6416-6420 [PMID:17034148] |
ChEMBL | Inhibition of DPP9 | B | 6.98 | pIC50 | 104 | nM | IC50 | Bioorg Med Chem (2012) 20: 5864-5883 [PMID:22938786] |
ChEMBL | Inhibition of DPP9 | B | 7 | pIC50 | 100 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 3596-3600 [PMID:20483603] |
dipeptidyl peptidase 8/Dipeptidyl peptidase VIII in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4657] [GtoPdb: 2356] [UniProtKB: Q6V1X1] | ||||||||
ChEMBL | Inhibition of DPP8 | B | 6.89 | pKi | 130 | nM | Ki | J Med Chem (2006) 49: 6416-6420 [PMID:17034148] |
ChEMBL | Inhibition of DPP8 | B | 6.61 | pIC50 | 244 | nM | IC50 | Bioorg Med Chem (2012) 20: 5864-5883 [PMID:22938786] |
ChEMBL | Inhibition of DPP8 | B | 6.62 | pIC50 | 240 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 3596-3600 [PMID:20483603] |
fibroblast activation protein alpha/Fibroblast activation protein alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4683] [GtoPdb: 2365] [UniProtKB: Q12884] | ||||||||
ChEMBL | Inhibition of FAP (unknown origin) | B | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127253-127253 [PMID:32527554] |
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]