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 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]