Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL3606685

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

Binding
Inhibition of human cathepsin-K using Z-Gly-Pro-Arg-AMC as substrate preincubated for 30 mins measured after 10 mins by fluorescence assay
8
Total Activities
8
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 K (CHEMBL268)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of N-(Functionalized benzoyl)-homocycloleucyl-glycinonitriles as Potent Cathepsin K Inhibitors.
Borišek J, Vizovišek M, Sosnowski P, Turk B, Turk D, Mohar B, Novič M.
J Med Chem (2015) 58 : 6928 -6937
PubMed 26280490 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 7.67 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL371064 BALICATIB 2.0 1 8.85
CHEMBL3605410 1 8.00
CHEMBL3605409 1 7.80
CHEMBL3605413 1 7.66
CHEMBL3605414 1 7.26
CHEMBL3605408 1 7.16
CHEMBL3605412 1 6.94
CHEMBL3605411 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL371064 BALICATIB Ki = 1.4 nM 8.85
CHEMBL3605410 Ki = 10.0 nM 8.00
CHEMBL3605409 Ki = 16.0 nM 7.80
CHEMBL3605413 Ki = 22.0 nM 7.66
CHEMBL3605414 Ki = 55.0 nM 7.26
CHEMBL3605408 Ki = 70.0 nM 7.16
CHEMBL3605412 Ki = 114.0 nM 6.94
CHEMBL3605411 Ki > 500.0 nM -