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Assay Detail

CHEMBL656685

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

Binding
Inhibitory concentration against recombinant human cathepsin K
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

Orally bioavailable small molecule ketoamide-based inhibitors of cathepsin K.
Barrett DG, Catalano JG, Deaton DN, Long ST, Miller LR, Tavares FX, Wells-Knecht KJ, Wright LL, Zhou HQ.
Bioorg Med Chem Lett (2004) 14 : 2543 -2546
PubMed 15109647 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 4.86 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL86088 1 6.00
CHEMBL84691 1 5.60
CHEMBL85977 1 4.89
CHEMBL421544 1 4.85
CHEMBL87961 1 4.85
CHEMBL418935 1 4.75
CHEMBL445898 1 4.72
CHEMBL83563 1 4.64
CHEMBL87332 1 4.52
CHEMBL446669 1 4.36
CHEMBL87946 1 4.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL86088 IC50 = 1000.0 nM 6.00
CHEMBL84691 IC50 = 2500.0 nM 5.60
CHEMBL85977 IC50 = 13000.0 nM 4.89
CHEMBL421544 IC50 = 14000.0 nM 4.85
CHEMBL87961 IC50 = 14000.0 nM 4.85
CHEMBL418935 IC50 = 18000.0 nM 4.75
CHEMBL445898 IC50 = 19000.0 nM 4.72
CHEMBL83563 IC50 = 23000.0 nM 4.64
CHEMBL87332 IC50 = 30000.0 nM 4.52
CHEMBL446669 IC50 = 44000.0 nM 4.36
CHEMBL87946 IC50 = 59000.0 nM 4.23