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Assay Detail

CHEMBL2073363

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

Binding
Inhibition of dog recombinant cathepsin K using Z-Phe-Arg-AMC as substrate preincubated for 30 mins measured after 1 hr by quenched fluorescent resonance energy transfer assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Canis lupus familiaris
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cathepsin K (CHEMBL2069160)
Type SINGLE PROTEIN
Organism Canis familiaris

Publication

Isosteric replacements for benzothiazoles and optimisation to potent Cathepsin K inhibitors free from hERG channel inhibition.
Dossetter AG, Bowyer J, Cook CR, Crawford JJ, Finlayson JE, Heron NM, Heyes C, Highton AJ, Hudson JA, Jestel A, Krapp S, MacFaul PA, McGuire TM, Morley AD, Morris JJ, Page KM, Ribeiro LR, Sawney H, Steinbacher S, Smith C.
Bioorg Med Chem Lett (2012) 22 : 5563 -5568
PubMed 22858142 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.75 7.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2070937 1 7.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2070937 IC50 = 18.0 nM 7.75