compound 9 [PMID: 20718420] [Ligand Id: 9893] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1243373
  • Dipeptidyl-peptidase 7/Dipeptidyl peptidase II in Human [ChEMBL: CHEMBL3976] [GtoPdb: 1605] [UniProtKB: Q9UHL4]
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  • dipeptidyl peptidase 4/Dipeptidyl peptidase IV in Human [ChEMBL: CHEMBL284] [GtoPdb: 1612] [UniProtKB: P27487]
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  • dipeptidyl peptidase 9/Dipeptidyl peptidase IX in Human [ChEMBL: CHEMBL4793] [GtoPdb: 2357] [UniProtKB: Q86TI2]
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  • dipeptidyl peptidase 8/Dipeptidyl peptidase VIII in Human [ChEMBL: CHEMBL4657] [GtoPdb: 2356] [UniProtKB: Q6V1X1]
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  • fibroblast activation protein alpha/Fibroblast activation protein alpha in Human [ChEMBL: CHEMBL4683] [GtoPdb: 2365] [UniProtKB: Q12884]
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  • prolyl endopeptidase/Prolyl endopeptidase in Human [ChEMBL: CHEMBL3202] [GtoPdb: 2395] [UniProtKB: P48147]
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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 recombinant His-tagged DPP2 expressed in insect cells B 4 pIC50 >100000 nM IC50 J Med Chem (2010) 53: 6572-6583 [PMID:20718420]
dipeptidyl peptidase 4/Dipeptidyl peptidase IV in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL284] [GtoPdb: 1612] [UniProtKB: P27487]
ChEMBL Inhibition of human DPP4 using H-Gly-Pro-AMC as substrate preincubated for 10 mins prior to substrate addition by fluorescence assay B 4 pIC50 >100000 nM IC50 J Med Chem (2013) 56: 3467-3477 [PMID:23594271]
ChEMBL Inhibition of human recombinant His-tagged DPP4 expressed in insect cells B 4.7 pIC50 >20000 nM IC50 J Med Chem (2010) 53: 6572-6583 [PMID:20718420]
GtoPdb - - 4.7 pIC50 >20000 nM IC50 J Med Chem (2010) 53: 6572-83 [PMID:20718420]
dipeptidyl peptidase 9/Dipeptidyl peptidase IX in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4793] [GtoPdb: 2357] [UniProtKB: Q86TI2]
ChEMBL Inhibition of human recombinant His-tagged DPP9 expressed in insect cells B 5.57 pIC50 2700 nM IC50 J Med Chem (2010) 53: 6572-6583 [PMID:20718420]
GtoPdb - - 5.57 pIC50 2700 nM IC50 J Med Chem (2010) 53: 6572-83 [PMID:20718420]
ChEMBL Inhibition of human DPP9 using H-Gly-Pro-AMC as substrate preincubated for 10 mins prior to substrate addition by fluorescence assay B 6.38 pIC50 420 nM IC50 J Med Chem (2013) 56: 3467-3477 [PMID:23594271]
dipeptidyl peptidase 8/Dipeptidyl peptidase VIII in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4657] [GtoPdb: 2356] [UniProtKB: Q6V1X1]
GtoPdb - - 5.43 pIC50 3700 nM IC50 J Med Chem (2010) 53: 6572-83 [PMID:20718420]
ChEMBL Inhibition of human recombinant His-tagged DPP8 expressed in insect cells B 5.43 pIC50 3700 nM IC50 J Med Chem (2010) 53: 6572-6583 [PMID:20718420]
ChEMBL Inhibition of human DPP8 using H-Gly-Pro-AMC as substrate preincubated for 10 mins prior to substrate addition by fluorescence assay B 5.92 pIC50 1200 nM IC50 J Med Chem (2013) 56: 3467-3477 [PMID:23594271]
fibroblast activation protein alpha/Fibroblast activation protein alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4683] [GtoPdb: 2365] [UniProtKB: Q12884]
ChEMBL Competitive inhibition of human recombinant FAP expressed in Hi5 insect cells by Lineweaver-Burke plot analysis B 8.1 pKi 7.9 nM Ki J Med Chem (2010) 53: 6572-6583 [PMID:20718420]
GtoPdb - - 7.72 pIC50 19 nM IC50 J Med Chem (2010) 53: 6572-83 [PMID:20718420]
ChEMBL Inhibition of human recombinant FAP expressed in Hi5 insect cells B 7.72 pIC50 19 nM IC50 J Med Chem (2010) 53: 6572-6583 [PMID:20718420]
ChEMBL Inhibition of human FAP using Z-Gly-Pro-AMC as substrate preincubated for 10 mins prior to substrate addition by fluorescence assay B 8.64 pIC50 2.3 nM IC50 J Med Chem (2013) 56: 3467-3477 [PMID:23594271]
prolyl endopeptidase/Prolyl endopeptidase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3202] [GtoPdb: 2395] [UniProtKB: P48147]
ChEMBL Inhibition of human PREP using Z-Gly-Pro-AMC as substrate preincubated for 10 mins prior to substrate addition by fluorescence assay B 8.74 pIC50 1.8 nM IC50 J Med Chem (2013) 56: 3467-3477 [PMID:23594271]

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]