odanacatib [Ligand Id: 6478] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL481611 (MK0822, MK-0822, Odanacatib)
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  • cathepsin C/Dipeptidyl peptidase I in Human [ChEMBL: CHEMBL2252] [GtoPdb: 2344] [UniProtKB: P53634]
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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 cathepsin B in human HepG2 cells B 5.98 pIC50 1050 nM IC50 Bioorg Med Chem Lett (2008) 18: 923-928 [PMID:18226527]
ChEMBL Inhibition of cathepsin B B 5.99 pIC50 1034 nM IC50 Bioorg Med Chem Lett (2008) 18: 923-928 [PMID:18226527]
cathepsin F/Cathepsin F in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2517] [GtoPdb: 2347] [UniProtKB: Q9UBX1]
ChEMBL Inhibition of cathepsin F B 6.1 pIC50 795 nM IC50 Bioorg Med Chem Lett (2008) 18: 923-928 [PMID:18226527]
cathepsin H/Cathepsin H in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2225] [GtoPdb: 2349] [UniProtKB: P09668]
ChEMBL Inhibition of cathepsin H B 8 pIC50 >10 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]
ChEMBL Inhibition of human cathepsin K B 9.74 pKi 0.18 nM Ki Eur J Med Chem (2018) 144: 201-210 [PMID:29272750]
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 9 pIC50 <1 nM IC50 J Med Chem (2012) 55: 6363-6374 [PMID:22742641]
ChEMBL Inhibition of cathepsin-k B 9 pIC50 <1 nM IC50 J Med Chem (2012) 55: 8827-8837 [PMID:22984809]
ChEMBL Inhibition of humanized rabbit cathepsin K B 9.7 pIC50 0.2 nM IC50 Bioorg Med Chem Lett (2009) 19: 675-679 [PMID:19117756]
ChEMBL Inhibition of humanized rabbit cathepsin K B 9.7 pIC50 0.2 nM IC50 Bioorg Med Chem Lett (2010) 20: 887-892 [PMID:20061146]
ChEMBL Inhibition of humanized rabbit cathepsin K B 9.7 pIC50 0.2 nM IC50 Bioorg Med Chem Lett (2008) 18: 923-928 [PMID:18226527]
ChEMBL Inhibition of humanized rabbit cathepsin K B 9.7 pIC50 0.2 nM IC50 Bioorg Med Chem Lett (2011) 21: 920-923 [PMID:21232956]
ChEMBL Inhibition of cathepsin K B 9.7 pIC50 0.2 nM IC50 J Med Chem (2010) 53: 4332-4353 [PMID:20218623]
ChEMBL Inhibition of human cathepsin K B 9.7 pIC50 0.2 nM IC50 Bioorg Med Chem Lett (2008) 18: 923-928 [PMID:18226527]
GtoPdb - - 9.7 pIC50 0.2 nM IC50 Bioorg Med Chem Lett (2008) 18: 923-8 [PMID:18226527]
Cathepsin K in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3349] [UniProtKB: P43236]
ChEMBL Inhibition of rabbit cathepsin K B 9 pIC50 1 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 Inhibition of Cathepsin L (unknown origin) using Z-Phe-Arg-7-amido-4-methylcoumarin as substrate preincubated for 2 mins followed by susbtrate addition by fluorescence based analysis B 5.9 pKi 1258.93 nM Ki Bioorg Med Chem (2019) 27: 115083-115083 [PMID:31561938]
ChEMBL Inhibition of cathepsin L in human HepG2 cells B 5.31 pIC50 4843 nM IC50 Bioorg Med Chem Lett (2008) 18: 923-928 [PMID:18226527]
ChEMBL Inhibition of cathepsin L B 5.52 pIC50 2995 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 cathepsin V B 6.12 pIC50 762 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 recombinant CatS assessed as suppression of enzyme-mediated Z-Val-Val-Arg-AMC cleavage by QFRET assay B 6.74 pIC50 183 nM IC50 J Med Chem (2012) 55: 6363-6374 [PMID:22742641]
GtoPdb - - 7.22 pIC50 60 nM IC50 Bioorg Med Chem Lett (2008) 18: 923-8 [PMID:18226527]
ChEMBL Inhibition of cathepsin S B 7.22 pIC50 60 nM IC50 Bioorg Med Chem Lett (2008) 18: 923-928 [PMID:18226527]
ChEMBL Inhibition of cathepsin S in human ramos cells B 7.35 pIC50 45 nM IC50 Bioorg Med Chem Lett (2008) 18: 923-928 [PMID:18226527]
cathepsin Z/Cathepsin Z in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4160] [GtoPdb: 2354] [UniProtKB: Q9UBR2]
GtoPdb - - 8 pIC50 10 nM IC50 Bioorg Med Chem Lett (2008) 18: 923-8 [PMID:18226527]
ChEMBL Inhibition of cathepsin Z B 8 pIC50 >10 nM IC50 Bioorg Med Chem Lett (2008) 18: 923-928 [PMID:18226527]
Cruzipain in Trypanosoma cruzi (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3563] [UniProtKB: P25779]
ChEMBL Inhibition of Trypanosoma cruzi cruzain using Z-Phe-Arg-7-amido-4-methylcoumarin as substrate preincubated for 2 mins followed by susbtrate addition by fluorescence based analysis B 6.9 pKi 125.89 nM Ki Bioorg Med Chem (2019) 27: 115083-115083 [PMID:31561938]
cathepsin C/Dipeptidyl peptidase I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2252] [GtoPdb: 2344] [UniProtKB: P53634]
ChEMBL Inhibition of cathepsin C B 8 pIC50 >10 nM IC50 Bioorg Med Chem Lett (2008) 18: 923-928 [PMID:18226527]

ChEMBL data shown on this page come from version 32:

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]