aloxistatin [Ligand Id: 10714] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL63440 (Aloxistatin, Aloxistatina, Aloxistatine, Loxistatin, NSC-694281) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| calpain 1/Calpain 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3891] [GtoPdb: 2336] [UniProtKB: P07384] | ||||||||
| ChEMBL | Inhibition of human erythrocytes mu-calpain using Pep1 as substrate incubated for 30 mins under shaking condition in presence of CaCl2 by fluorescence assay | B | 4.21 | pIC50 | 62260 | nM | IC50 | Eur J Med Chem (2016) 121: 433-444 [PMID:27318120] |
| ChEMBL | The ability of compound to inhibit calpain in a preparation of lysed platelets was measured with a caseinolytic assay(assay 1) | B | 5.4 | pIC50 | 4000 | nM | IC50 | J Med Chem (1992) 35: 2048-2054 [PMID:1597856] |
| ChEMBL | The calpain inhibitory activity(I 50) was measured as ability to enter the platelet to inhibit calpain after cell lysis(assay 2) | B | 5.4 | pIC50 | 4000 | nM | IC50 | J Med Chem (1992) 35: 2048-2054 [PMID:1597856] |
| cathepsin B/Cathepsin B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4072] [GtoPdb: 2343] [UniProtKB: P07858] | ||||||||
| ChEMBL | Inhibition of cathepsin B (unknown origin) using RR-AMC as substrate preincubated for 30 mins followed by substrate addition and further incubated for 30 mins under shaking condition by fluorescence assay | B | 4.84 | pIC50 | 14390 | nM | IC50 | Eur J Med Chem (2016) 121: 433-444 [PMID:27318120] |
| cathepsin G/Cathepsin G in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4071] [GtoPdb: 2348] [UniProtKB: P08311] | ||||||||
| ChEMBL | Blockade of cathepsin G processing in human U937 cells by densitometry | B | 5.96 | pIC50 | 1100 | nM | IC50 | J Biol Chem (2007) 282: 20836-20846 [PMID:17535802] |
| GtoPdb | - | - | 5.96 | pIC50 | 1100 | nM | IC50 | J Biol Chem (2007) 282: 20836-46 [PMID:17535802] |
| cathepsin G/Cathepsin G in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5622] [GtoPdb: 2348] [UniProtKB: P28293] | ||||||||
| ChEMBL | Inhibition of cathepsin G activation in beta-estradiol differentiated mouse EcoM-G cells after 24 hrs | B | 5 | pIC50 | >10000 | nM | IC50 | J Biol Chem (2007) 282: 20836-20846 [PMID:17535802] |
| cathepsin L/Cathepsin L in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3837] [GtoPdb: 2351] [UniProtKB: P07711] | ||||||||
| ChEMBL | Inhibition of cathepsin L (unknown origin) using Z-FR-AMC as substrate preincubated for 30 mins followed by substrate addition and further incubated for 30 mins under shaking condition by fluorescence assay | B | 5.62 | pIC50 | 2410 | nM | IC50 | Eur J Med Chem (2016) 121: 433-444 [PMID:27318120] |
| proteinase 3/Myeloblastin in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5384] [GtoPdb: 2401] [UniProtKB: Q61096] | ||||||||
| ChEMBL | Inhibition of proteinase-3 activation in beta-estradiol differentiated mouse EcoM-G cells after 24 hrs | B | 5 | pIC50 | >10000 | nM | IC50 | J Biol Chem (2007) 282: 20836-20846 [PMID:17535802] |
| elastase, neutrophil expressed/Neutrophil elastase in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5156] [GtoPdb: 2358] [UniProtKB: Q3UP87] | ||||||||
| ChEMBL | Inhibition of neutrophil elastase activation in beta-estradiol differentiated mouse EcoM-G cells after 24 hrs | B | 5 | pIC50 | >10000 | nM | IC50 | J Biol Chem (2007) 282: 20836-20846 [PMID:17535802] |
| Papain in Carica papaya (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4779] [UniProtKB: P00784] | ||||||||
| ChEMBL | Kinetic constant Apparent binding constant (Ki`) for the inhibition of papain conducted in 0.1 M phosphate, pH 6.8, at 30 degree C | B | 4.28 | pKi | 52000 | nM | Ki | J Med Chem (1996) 39: 3357-3366 [PMID:8765519] |
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]
