Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
ChEMBL ligand: CHEMBL481611 (MK-0822, MK0822, Odanacatib) |
---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
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 (unknown origin) assessed as inhibition of AFC release using sequence RR labelled with AFC as substrate by fluorescence based analysis | B | 5.7 | pIC50 | <2000 | nM | IC50 | Bioorg Med Chem (2022) 74: 117053-117053 [PMID:36270112] |
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 Cathepsin K (unknown origin) assessed as inhibition of AFC release using sequence LR labelled with AFC as substrate by fluorescence based analysis | B | 8.77 | pIC50 | 1.7 | nM | IC50 | Bioorg Med Chem (2022) 74: 117053-117053 [PMID:36270112] |
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 (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] |
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] |
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 Cathepsin S (unknown origin) assessed as inhibition of AFC release using sequence VVR labelled with AFC as substrate by fluorescence based analysis | B | 6.3 | pIC50 | <500 | nM | IC50 | Bioorg Med Chem (2022) 74: 117053-117053 [PMID:36270112] |
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 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]