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Assay Detail

CHEMBL2168712

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

Binding
Inhibition of dog recombinant CatK assessed as suppression of enzyme-mediated Z-Phe-Arg-AMC cleavage by QFRET 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

(1R,2R)-N-(1-cyanocyclopropyl)-2-(6-methoxy-1,3,4,5-tetrahydropyrido[4,3-b]indole-2-carbonyl)cyclohexanecarboxamide (AZD4996): a potent and highly selective cathepsin K inhibitor for the treatment of osteoarthritis.
Dossetter AG, Beeley H, Bowyer J, Cook CR, Crawford JJ, Finlayson JE, Heron NM, Heyes C, Highton AJ, Hudson JA, Jestel A, Kenny PW, Krapp S, Martin S, MacFaul PA, McGuire TM, Gutierrez PM, Morley AD, Morris JJ, Page KM, Ribeiro LR, Sawney H, Steinbacher S, Smith C, Vickers M.
J Med Chem (2012) 55 : 6363 -6374
PubMed 22742641 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 9.10 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2163587 1 9.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2163587 IC50 = 0.8 nM 9.10