ARI-3099 [Ligand Id: 8563] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2333026
  • 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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  • fibroblast activation protein alpha in Human [GtoPdb: 2365] [UniProtKB: Q12884]
  • fibroblast activation protein alpha/Seprase in Mouse [ChEMBL: CHEMBL5769] [GtoPdb: 2365] [UniProtKB: P97321]
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  • acylaminoacyl-peptide hydrolase in Human [GtoPdb: 2328] [UniProtKB: P13798]
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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 DPP2 purified from human seminal plasma using Lys-Ala-p-nitroanilide as substrate by spectrophotometry B 4 pIC50 >100000 nM IC50 J. Med. Chem. (2014) 57: 3053-3074 [PMID:24617858]
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 DPP4 purified from human seminal plasma using Gly-Pro-p-nitroanilide as substrate by spectrophotometry B 4 pIC50 >100000 nM IC50 J. Med. Chem. (2014) 57: 3053-3074 [PMID:24617858]
dipeptidyl peptidase 9/Dipeptidyl peptidase IX in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4793] [GtoPdb: 2357] [UniProtKB: Q86TI2]
ChEMBL Inhibition of human DPP9 using H-Gly-Pro-AMC as substrate preincubated for 10 mins prior to substrate addition by fluorescence assay B 5.47 pIC50 3400 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]
ChEMBL Inhibition of human DPP8 using H-Gly-Pro-AMC as substrate preincubated for 10 mins prior to substrate addition by fluorescence assay B 5.25 pIC50 5600 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 FAP using Suc-GP-AMC as substrate by Lineweaver-Burk plot analysis B 8.05 pKi 9 nM Ki J. Med. Chem. (2013) 56: 3467-3477 [PMID:23594271]
GtoPdb - - 7.44 pIC50 36 nM IC50 J Med Chem (2013) 56: 3467-77 [PMID:23594271]
ChEMBL Inhibition of human FAP using Z-Gly-Pro-AMC as substrate preincubated for 10 mins prior to substrate addition by fluorescence assay B 7.44 pIC50 36 nM IC50 J. Med. Chem. (2013) 56: 3467-3477 [PMID:23594271]
ChEMBL Inhibition of FAP (unknown origin) B 7.44 pIC50 >36 nM IC50 J Med Chem (2019) 62: 7874-7884 [PMID:31393718]
prolyl endopeptidase/Prolyl endopeptidase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3202] [GtoPdb: 2395] [UniProtKB: P48147]
ChEMBL Competitive inhibition of human PREP using Suc-GP-AMC as substrate by Lineweaver-Burk plot analysis B 5.51 pKi 3100 nM Ki J. Med. Chem. (2013) 56: 3467-3477 [PMID:23594271]
ChEMBL Inhibition of human PREP using Z-Gly-Pro-AMC as substrate preincubated for 10 mins prior to substrate addition by fluorescence assay B 4.89 pIC50 13000 nM IC50 J. Med. Chem. (2013) 56: 3467-3477 [PMID:23594271]
ChEMBL Inhibition of POP (unknown origin) B 5 pIC50 >10000 nM IC50 J Med Chem (2019) 62: 7874-7884 [PMID:31393718]
ChEMBL Inhibition of recombinant human PREP purified from Escherichia coli using Z-Gly-Pro-p-nitroanilide as substrate by spectrophotometry B 6 pIC50 990 nM IC50 J. Med. Chem. (2014) 57: 3053-3074 [PMID:24617858]
fibroblast activation protein alpha in Human [GtoPdb: 2365] [UniProtKB: Q12884]
GtoPdb - - 7.44 pIC50 36 nM IC50 J Med Chem (2013) 56: 3467-77 [PMID:23594271]
fibroblast activation protein alpha/Seprase in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5769] [GtoPdb: 2365] [UniProtKB: P97321]
ChEMBL Inhibition of recombinant mouse FAP purified from HEK293 cell supernatant using Ala-Pro-p-nitroanilide as substrate by spectrophotometry B 7.6 pIC50 25 nM IC50 J. Med. Chem. (2014) 57: 3053-3074 [PMID:24617858]
acylaminoacyl-peptide hydrolase in Human [GtoPdb: 2328] [UniProtKB: P13798]
GtoPdb Substrate (Ac-Ala-AMC) assay. - 6.98 pIC50 104 nM IC50 Nat Chem Biol (2014) 10: 656-63 [PMID:24997602]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]