relacatib [Ligand Id: 7862] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL203665 (Relacatib, SB-462795)
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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 7.89 pKi 13 nM Ki J Med Chem (2006) 49: 1597-1612 [PMID:16509577]
ChEMBL Inhibition of cathepsin B in human HepG2 cells B 7.85 pIC50 14 nM IC50 Bioorg Med Chem Lett (2008) 18: 923-928 [PMID:18226527]
cathepsin K/Cathepsin K in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL268] [GtoPdb: 2350] [UniProtKB: P43235]
GtoPdb - - 9.39 pKi 0.41 nM Ki J Med Chem (2010) 53: 4332-53 [PMID:20218623]
ChEMBL Inhibition of human cathepsin K B 10.39 pKi 0.04 nM Ki J Med Chem (2006) 49: 1597-1612 [PMID:16509577]
ChEMBL Inhibition of cathepsin K B 10.39 pKi 0.04 nM Ki J Med Chem (2010) 53: 4332-4353 [PMID:20218623]
ChEMBL Inhibition of humanized rabbit cathepsin K B 9.3 pIC50 0.5 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 Inhibition of rabbit cathepsin K B 9.3 pIC50 0.5 nM IC50 Bioorg Med Chem Lett (2008) 18: 923-928 [PMID:18226527]
cathepsin K/Cathepsin K in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3034] [GtoPdb: 2350] [UniProtKB: O35186]
ChEMBL Inhibition of rat cathepsin K B 8.1 pKi 8 nM Ki J Med Chem (2006) 49: 1597-1612 [PMID:16509577]
cathepsin L/Cathepsin L in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3837] [GtoPdb: 2351] [UniProtKB: P07711]
ChEMBL Inhibition of human cathepsin L B 10.17 pKi 0.07 nM Ki J Med Chem (2006) 49: 1597-1612 [PMID:16509577]
ChEMBL Inhibition of cathepsin L in human HepG2 cells B 8.7 pIC50 2 nM IC50 Bioorg Med Chem Lett (2008) 18: 923-928 [PMID:18226527]
cathepsin V/Cathepsin L2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3272] [GtoPdb: 2352] [UniProtKB: O60911]
ChEMBL Inhibition of human cathepsin V B 10.2 pKi 0.06 nM Ki J Med Chem (2006) 49: 1597-1612 [PMID:16509577]
cathepsin S/Cathepsin S in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2954] [GtoPdb: 2353] [UniProtKB: P25774]
ChEMBL Inhibition of human cathepsin S B 8.8 pKi 1.6 nM Ki J Med Chem (2006) 49: 1597-1612 [PMID:16509577]
ChEMBL Inhibition of cathepsin S in human ramos cells B 8.1 pIC50 8 nM IC50 Bioorg Med Chem Lett (2008) 18: 923-928 [PMID:18226527]

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]