ARI-3099 [Ligand Id: 8563] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2333026 |
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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] |
| ChEMBL | Inhibition of DPP2 (unknown origin) using AMC substrate by fluorometric assay | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2021) 37: 127846-127846 [PMID:33571650] |
| 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] |
| ChEMBL | Inhibition of DPP4 (unknown origin) using AMC substrate by fluorometric assay | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2021) 37: 127846-127846 [PMID:33571650] |
| dipeptidyl peptidase 9/Dipeptidyl peptidase IX in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4793] [GtoPdb: 2357] [UniProtKB: Q86TI2] | ||||||||
| ChEMBL | Inhibition of DPP9 (unknown origin) using AMC substrate by fluorometric assay | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2021) 37: 127846-127846 [PMID:33571650] |
| 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] |
| ChEMBL | Inhibition of FAP (unknown origin) using AMC substrate by fluorometric assay | B | 7.6 | pIC50 | 25 | nM | IC50 | Bioorg Med Chem Lett (2021) 37: 127846-127846 [PMID:33571650] |
| 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] |
| ChEMBL | Inhibition of PREP (unknown origin) using AMC substrate by fluorometric assay | B | 6 | pIC50 | 990 | nM | IC50 | Bioorg Med Chem Lett (2021) 37: 127846-127846 [PMID:33571650] |
| 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 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]
