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ChEMBL ligand: CHEMBL385517 (BMS-477118, SBMS-477118) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 (unknown origin) | B | 7.3 | pIC50 | 50 | nM | IC50 | J Med Chem (2014) 57: 2197-2212 [PMID:24099035] |
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 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 human DPP4 using Gly-Pro-AMC as substrate incubated for 30 mins by continuous fluorescent assay | B | 8.82 | pIC50 | 1.5 | nM | IC50 | Bioorg Med Chem Lett (2022) 76: 129018-129018 [PMID:36209967] |
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 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]