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ChEMBL ligand: CHEMBL371064 (AAE-581, AAE581, Balicatib) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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cathepsin B/Cathepsin B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4072] [GtoPdb: 2343] [UniProtKB: P07858] | ||||||||
ChEMBL | Inhibition of human cathepsin B using Z-Arg-Arg-pNA chromogenic substrate fluorogenic substrate incubated for 30 mins | B | 5.42 | pKi | 3800 | nM | Ki | ACS Med Chem Lett (2014) 5: 1076-1081 [PMID:25313316] |
ChEMBL | Inhibitory constant against human cathepsin B using Boc-Leu-Lys-Arg-AMC substrate | B | 5.54 | pKi | 2900 | nM | Ki | J Med Chem (2005) 48: 7520-7534 [PMID:16302794] |
ChEMBL | Inhibitory activity against human cathepsin B | B | 5.32 | pIC50 | 4800 | nM | IC50 | J Med Chem (2005) 48: 7535-7543 [PMID:16302795] |
ChEMBL | Inhibition of human recombinant CatB assessed as suppression of enzyme-mediated Z-Arg-Arg-AMC cleavage by QFRET assay | B | 5.32 | pIC50 | 4750 | nM | IC50 | J Med Chem (2012) 55: 6363-6374 [PMID:22742641] |
ChEMBL | Inhibitory activity against human cathepsin B expressed in HepG2 cells | B | 7.21 | pIC50 | 61 | nM | IC50 | J Med Chem (2005) 48: 7535-7543 [PMID:16302795] |
ChEMBL | Inhibition of cathepsin B in human HepG2 cells | B | 7.21 | pIC50 | 61 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 923-928 [PMID:18226527] |
cathepsin D/Cathepsin D in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2581] [GtoPdb: 2345] [UniProtKB: P07339] | ||||||||
ChEMBL | Inhibition of human cathepsin K using Z-Leu-Arg-AMC fluorogenic substrate incubated for 60 mins | B | 8.89 | pKi | 1.29 | nM | Ki | ACS Med Chem Lett (2014) 5: 1076-1081 [PMID:25313316] |
cathepsin K/Cathepsin K in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL268] [GtoPdb: 2350] [UniProtKB: P43235] | ||||||||
ChEMBL | Inhibition of human cathepsin-K using Z-Gly-Pro-Arg-AMC as substrate preincubated for 30 mins measured after 10 mins by fluorescence assay | B | 8.85 | pKi | 1.4 | nM | Ki | J Med Chem (2015) 58: 6928-6937 [PMID:26280490] |
ChEMBL | Inhibition of human recombinant CatK assessed as suppression of enzyme-mediated Z-Phe-Arg-AMC cleavage incubated for 1 hrs by QFRET assay | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2012) 55: 6363-6374 [PMID:22742641] |
ChEMBL | Inhibition of cathepsin-k | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2012) 55: 8827-8837 [PMID:22984809] |
GtoPdb | - | - | 8.85 | pIC50 | 1.4 | nM | IC50 | J Med Chem (2010) 53: 4332-53 [PMID:20218623] |
ChEMBL | Inhibitory activity against humanized rabbit cathepsin K | B | 8.85 | pIC50 | 1.4 | nM | IC50 | J Med Chem (2005) 48: 7535-7543 [PMID:16302795] |
ChEMBL | Inhibition of cathepsin K | B | 8.85 | pIC50 | 1.4 | nM | IC50 | J Med Chem (2010) 53: 4332-4353 [PMID:20218623] |
ChEMBL | Inhibition of human cathepsin K | B | 9.22 | pIC50 | 0.6 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 923-928 [PMID:18226527] |
Cathepsin K in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3349] [UniProtKB: P43236] | ||||||||
ChEMBL | Inhibitory constant against rabbit cathepsin K using Z-Phe-Arg-AMC substrate | B | 8.85 | pKi | 1.4 | nM | Ki | J Med Chem (2005) 48: 7520-7534 [PMID:16302794] |
ChEMBL | Inhibitory activity against rabbit cathepsin K | B | 8.57 | pIC50 | 2.7 | nM | IC50 | J Med Chem (2005) 48: 7535-7543 [PMID:16302795] |
ChEMBL | Inhibition of rabbit cathepsin K | B | 8.57 | pIC50 | 2.7 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 923-928 [PMID:18226527] |
cathepsin L/Cathepsin L in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3837] [GtoPdb: 2351] [UniProtKB: P07711] | ||||||||
ChEMBL | Inhibitory constant against human cathepsin L using Z-Phe-Arg-AMC substrate | B | 4.74 | pKi | 18000 | nM | Ki | J Med Chem (2005) 48: 7520-7534 [PMID:16302794] |
ChEMBL | Inhibition of human cathepsin L using Z-Phe-Arg-pNA chromogenic substrate fluorogenic substrate incubated for 30 mins | B | 5.49 | pKi | 3260 | nM | Ki | ACS Med Chem Lett (2014) 5: 1076-1081 [PMID:25313316] |
ChEMBL | Inhibition of human cathepsin-L using Z-Phe-Arg-AMC as substrate preincubated for 30 mins measured after 10 mins by fluorescence assay | B | 6.3 | pKi | 503 | nM | Ki | J Med Chem (2015) 58: 6928-6937 [PMID:26280490] |
ChEMBL | Inhibitory activity against human cathepsin L | B | 6.3 | pIC50 | 503 | nM | IC50 | J Med Chem (2005) 48: 7535-7543 [PMID:16302795] |
ChEMBL | Inhibitory activity against human cathepsin L expressed in HepG2 cells | B | 7.32 | pIC50 | 48 | nM | IC50 | J Med Chem (2005) 48: 7535-7543 [PMID:16302795] |
ChEMBL | Inhibition of cathepsin L in human HepG2 cells | B | 7.32 | pIC50 | 48 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 923-928 [PMID:18226527] |
cathepsin S/Cathepsin S in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2954] [GtoPdb: 2353] [UniProtKB: P25774] | ||||||||
ChEMBL | Inhibition of human cathepsin-S using Z-Phe-Val-Arg-AMC as substrate preincubated for 30 mins measured after 10 mins by fluorescence assay | B | 4.19 | pKi | 65000 | nM | Ki | J Med Chem (2015) 58: 6928-6937 [PMID:26280490] |
ChEMBL | Inhibition of human cathepsin S using Z-Phe-Arg-AMC fluorogenic substrate fluorogenic substrate incubated for 60 mins | B | 4.52 | pKi | 30100 | nM | Ki | ACS Med Chem Lett (2014) 5: 1076-1081 [PMID:25313316] |
ChEMBL | Inhibitory constant against human cathepsin S using Z-Val-Val-Arg-AMC substrate | B | 4.55 | pKi | 28000 | nM | Ki | J Med Chem (2005) 48: 7520-7534 [PMID:16302794] |
ChEMBL | Inhibitory activity against human cathepsin S | B | 4.19 | pIC50 | 65000 | nM | IC50 | J Med Chem (2005) 48: 7535-7543 [PMID:16302795] |
ChEMBL | Inhibitory activity against human cathepsin S expressed in ramos cells | B | 5.54 | pIC50 | 2900 | nM | IC50 | J Med Chem (2005) 48: 7535-7543 [PMID:16302795] |
ChEMBL | Inhibition of cathepsin S in human ramos cells | B | 5.54 | pIC50 | 2900 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 923-928 [PMID:18226527] |
cathepsin S/Cathepsin S in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4098] [GtoPdb: 2353] [UniProtKB: O70370] | ||||||||
ChEMBL | Inhibitory activity against mouse cathepsin S | B | 5.2 | pIC50 | 6350 | nM | IC50 | J Med Chem (2005) 48: 7535-7543 [PMID:16302795] |
ChEMBL | Inhibitory activity against mouse cathepsin S in mouse splenocytes | B | 6.32 | pIC50 | 480 | nM | IC50 | J Med Chem (2005) 48: 7535-7543 [PMID:16302795] |
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]