aloxistatin [Ligand Id: 10714] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL63440 (Aloxistatin, 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 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]
