LHVS [Ligand Id: 9298] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL222649
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  • cathepsin C/Dipeptidyl peptidase I in Human [ChEMBL: CHEMBL2252] [GtoPdb: 2344] [UniProtKB: P53634]
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  • elastase, neutrophil expressed/Neutrophil elastase in Mouse [ChEMBL: CHEMBL5156] [GtoPdb: 2358] [UniProtKB: Q3UP87]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
cathepsin B/Cathepsin B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4072] [GtoPdb: 2343] [UniProtKB: P07858]
ChEMBL Inhibition of human cathepsin B B 5.35 pIC50 4504 nM IC50 Bioorg. Med. Chem. Lett. (2007) 17: 4929-4933 [PMID:17590332]
ChEMBL Inhibition of human recombinant cathepsin B after 10 mins B 5.87 pIC50 1360 nM IC50 J. Biol. Chem. (2007) 282: 20836-20846 [PMID:17535802]
GtoPdb - - 5.87 pIC50 1360 nM IC50 J Biol Chem (2007) 282: 20836-46 [PMID:17535802]
ChEMBL Inhibition of human cathepsin-B B 8.52 pIC50 3 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 3140-3144 [PMID:23639544]
cathepsin B/Cathepsin B in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5187] [GtoPdb: 2343] [UniProtKB: P10605]
ChEMBL Inhibition of mouse recombinant cathepsin B B 5.89 pIC50 1277 nM IC50 Bioorg. Med. Chem. Lett. (2007) 17: 4929-4933 [PMID:17590332]
cathepsin B/Cathepsin B in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2602] [GtoPdb: 2343] [UniProtKB: P00787]
ChEMBL Inhibition of rat liver lysosomal cathepsin B B 6.13 pIC50 735 nM IC50 Bioorg. Med. Chem. Lett. (2007) 17: 4929-4933 [PMID:17590332]
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 4.4 pIC50 39800 nM IC50 J. Biol. Chem. (2007) 282: 20836-20846 [PMID:17535802]
cathepsin K/Cathepsin K in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL268] [GtoPdb: 2350] [UniProtKB: P43235]
ChEMBL Inhibition of human cathepsin K B 8.21 pIC50 6.2 nM IC50 Bioorg. Med. Chem. Lett. (2007) 17: 4929-4933 [PMID:17590332]
ChEMBL Inhibition of human cathepsin-K B 8.4 pIC50 4 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 3140-3144 [PMID:23639544]
cathepsin K/Cathepsin K in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075277] [GtoPdb: 2350] [UniProtKB: P55097]
ChEMBL Inhibition of mouse recombinant cathepsin K B 6.41 pIC50 388 nM IC50 Bioorg. Med. Chem. Lett. (2007) 17: 4929-4933 [PMID:17590332]
Cathepsin L in Toxoplasma gondii (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4295862] [UniProtKB: Q6DMN0]
ChEMBL Inhibition of Toxoplasma gondii cathepsin L using Z-L-R-AMC as substrate preincubated for 5 mins followed by substrate addition measured over 5 mins by spectrophotometric method B 8.7 pIC50 2 nM IC50 Bioorg Med Chem Lett (2018) 28: 1972-1980 [PMID:29650289]
cathepsin L/Cathepsin L in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3837] [GtoPdb: 2351] [UniProtKB: P07711]
GtoPdb - - 8.15 pIC50 7 nM IC50 J Biol Chem (2007) 282: 20836-46 [PMID:17535802]
ChEMBL Inhibition of human recombinant cathepsin L after 10 mins B 8.15 pIC50 7 nM IC50 J. Biol. Chem. (2007) 282: 20836-20846 [PMID:17535802]
ChEMBL Inhibition of human cathepsin L B 8.24 pIC50 5.7 nM IC50 Bioorg. Med. Chem. Lett. (2007) 17: 4929-4933 [PMID:17590332]
ChEMBL Inhibition of human cathepsin L using Z-L-R-AMC as substrate preincubated for 5 mins followed by substrate addition measured over 5 mins by spectrophotometric method B 8.52 pIC50 3 nM IC50 Bioorg Med Chem Lett (2018) 28: 1972-1980 [PMID:29650289]
cathepsin V/Cathepsin L in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2305] [GtoPdb: 2352] [UniProtKB: P07154]
ChEMBL Inhibition of rat liver lysosomal cathepsin L B 8.39 pIC50 4.1 nM IC50 Bioorg. Med. Chem. Lett. (2007) 17: 4929-4933 [PMID:17590332]
cathepsin L in Human [GtoPdb: 2351] [UniProtKB: P07711]
GtoPdb - - 8.15 pIC50 7 nM IC50 J Biol Chem (2007) 282: 20836-46 [PMID:17535802]
cathepsin L/Cathepsin L1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5291] [GtoPdb: 2351] [UniProtKB: P06797]
ChEMBL Inhibition of mouse recombinant cathepsin L B 8.15 pIC50 7.1 nM IC50 Bioorg. Med. Chem. Lett. (2007) 17: 4929-4933 [PMID:17590332]
cathepsin S/Cathepsin S in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2954] [GtoPdb: 2353] [UniProtKB: P25774]
ChEMBL Inhibition of human cathepsin-S B 8.72 pIC50 1.9 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 3140-3144 [PMID:23639544]
ChEMBL Inhibition of human cathepsin S B 8.92 pIC50 1.2 nM IC50 Bioorg. Med. Chem. Lett. (2007) 17: 4929-4933 [PMID:17590332]
GtoPdb - - 9 pIC50 1 nM IC50 J Biol Chem (2007) 282: 20836-46 [PMID:17535802]
ChEMBL Inhibition of human recombinant cathepsin S after 10 mins B 9 pIC50 1 nM IC50 J. Biol. Chem. (2007) 282: 20836-20846 [PMID:17535802]
cathepsin S/Cathepsin S in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4098] [GtoPdb: 2353] [UniProtKB: O70370]
ChEMBL Inhibition of mouse recombinant cathepsin S B 9.3 pIC50 0.5 nM IC50 Bioorg. Med. Chem. Lett. (2007) 17: 4929-4933 [PMID:17590332]
cathepsin S/Cathepsin S in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075217] [GtoPdb: 2353] [UniProtKB: Q02765]
ChEMBL Inhibition of rat spleen cathepsin S B 8.77 pIC50 1.7 nM IC50 Bioorg. Med. Chem. Lett. (2007) 17: 4929-4933 [PMID:17590332]
cathepsin C/Dipeptidyl peptidase I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2252] [GtoPdb: 2344] [UniProtKB: P53634]
ChEMBL Inhibition of human recombinant cathepsin C after 10 mins B 5 pIC50 >10000 nM IC50 J. Biol. Chem. (2007) 282: 20836-20846 [PMID:17535802]
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 4.67 pIC50 21200 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 4.59 pIC50 25500 nM IC50 J. Biol. Chem. (2007) 282: 20836-20846 [PMID:17535802]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]