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Assay Detail

CHEMBL2175127

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Binding
Inhibition of cathepsin-k
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Cathepsin K (CHEMBL268)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Pharmacokinetic benefits of 3,4-dimethoxy substitution of a phenyl ring and design of isosteres yielding orally available cathepsin K inhibitors.
Crawford JJ, Kenny PW, Bowyer J, Cook CR, Finlayson JE, Heyes C, Highton AJ, Hudson JA, Jestel A, Krapp S, Martin S, Macfaul PA, McDermott BP, McGuire TM, Morley AD, Morris JJ, Page KM, Ribeiro LR, Sawney H, Steinbacher S, Smith C, Dossetter AG.
J Med Chem (2012) 55 : 8827 -8837
PubMed 22984809 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.88 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL371064 BALICATIB 2.0 1 8.30
CHEMBL2070936 1 7.82
CHEMBL2071097 1 7.52
CHEMBL2163587 1 -
CHEMBL481611 ODANACATIB 3.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL371064 BALICATIB IC50 = 5.0 nM 8.30
CHEMBL2070936 IC50 = 15.0 nM 7.82
CHEMBL2071097 IC50 = 30.0 nM 7.52
CHEMBL2163587 IC50 < 1.0 nM -
CHEMBL481611 ODANACATIB IC50 < 1.0 nM -