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Assay Detail

CHEMBL949945

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

Binding
Inhibition of human recombinant cathepsin K
20
Total Activities
20
Compounds Tested
2
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

Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality.
Maryanoff BE, Costanzo MJ.
Bioorg Med Chem (2008) 16 : 1562 -1595
PubMed 18053726 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 7.47 9.02
IC50 6 6.06 8.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL209293 1 9.02
CHEMBL209215 1 8.77
CHEMBL116402 1 8.57
CHEMBL379622 1 8.48
CHEMBL405602 1 8.10
CHEMBL257692 1 8.07
CHEMBL270792 1 8.02
CHEMBL210198 1 7.66
CHEMBL211050 1 7.54
CHEMBL446718 1 7.40
CHEMBL208566 1 7.27
CHEMBL361816 1 6.64
CHEMBL272374 1 6.30
CHEMBL411498 1 5.52
CHEMBL361975 1 5.51
CHEMBL360745 1 5.40
CHEMBL181105 1 5.15
CHEMBL360237 1 5.09
CHEMBL272375 1 5.02
CHEMBL271004 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL209293 Ki = 0.95 nM 9.02
CHEMBL209215 Ki = 1.7 nM 8.77
CHEMBL116402 IC50 = 2.7 nM 8.57
CHEMBL379622 Ki = 3.3 nM 8.48
CHEMBL405602 Ki = 7.9 nM 8.10
CHEMBL257692 Ki = 8.5 nM 8.07
CHEMBL270792 Ki = 9.5 nM 8.02
CHEMBL210198 Ki = 22.0 nM 7.66
CHEMBL211050 Ki = 29.0 nM 7.54
CHEMBL446718 Ki = 40.0 nM 7.40
CHEMBL208566 Ki = 54.0 nM 7.27
CHEMBL361816 IC50 = 230.0 nM 6.64
CHEMBL272374 Ki = 500.0 nM 6.30
CHEMBL411498 Ki = 3000.0 nM 5.52
CHEMBL361975 IC50 = 3100.0 nM 5.51
CHEMBL360745 IC50 = 4000.0 nM 5.40
CHEMBL181105 IC50 = 7100.0 nM 5.15
CHEMBL360237 IC50 = 8100.0 nM 5.09
CHEMBL272375 Ki = 9600.0 nM 5.02
CHEMBL271004 Ki < 0.25 nM -