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Assay Detail

CHEMBL827830

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

Binding
Inhibition of 10 uM Cbz-Phe-Arg-AMC binding to human cathepsin K by fluorescence assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Cathepsin K (CHEMBL268)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Ketoheterocycle-based inhibitors of cathepsin K: a novel entry into the synthesis of peptidic ketoheterocycles.
Tavares FX, Deaton DN, Miller AB, Miller LR, Wright LL.
Bioorg Med Chem Lett (2005) 15 : 3891 -3895
PubMed 15993587 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.76 8.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL116402 1 8.57
CHEMBL361816 1 6.64
CHEMBL183796 1 5.72
CHEMBL361975 1 5.51
CHEMBL360745 1 5.40
CHEMBL181105 1 5.15
CHEMBL360237 1 5.09
CHEMBL182539 1 4.89
CHEMBL434132 1 4.89
CHEMBL359612 1 -
CHEMBL183647 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL116402 IC50 = 2.7 nM 8.57
CHEMBL361816 IC50 = 230.0 nM 6.64
CHEMBL183796 IC50 = 1900.0 nM 5.72
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
CHEMBL182539 IC50 = 13000.0 nM 4.89
CHEMBL434132 IC50 = 13000.0 nM 4.89
CHEMBL359612 IC50 > 13000.0 nM -
CHEMBL183647 IC50 > 13000.0 nM -