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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 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]