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Assay Detail

CHEMBL1292094

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of human cathepsin B by fluorescence assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cathepsin B (CHEMBL4072)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Trifluoromethylphenyl as P2 for ketoamide-based cathepsin S inhibitors.
Cai J, Robinson J, Belshaw S, Everett K, Fradera X, van Zeeland M, van Berkom L, van Rijnsbergen P, Popplestone L, Baugh M, Dempster M, Bruin J, Hamilton W, Kinghorn E, Westwood P, Kerr J, Rankovic Z, Arbuckle W, Bennett DJ, Jones PS, Long C, Martin I, Uitdehaag JC, Meulemans T.
Bioorg Med Chem Lett (2010) 20 : 6890 -6894
PubMed 21030256 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.18 5.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1289645 1 5.49
CHEMBL1289305 1 5.24
CHEMBL1289644 1 4.82
CHEMBL1289856 1 -
CHEMBL1289857 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1289645 IC50 = 3236.0 nM 5.49
CHEMBL1289305 IC50 = 5754.0 nM 5.24
CHEMBL1289644 IC50 = 15136.0 nM 4.82
CHEMBL1289856 IC50 > 10000.0 nM -
CHEMBL1289857 IC50 > 10000.0 nM -