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) | B | 7.44 | pIC50 | 36 | nM | IC50 | Eur J Med Chem (2022) 240: 114543-114543 [PMID:35797897] |
| 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 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]
