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Assay Detail

CHEMBL886077

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

Binding
Inhibition of rabbit cathepsin K
11
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Cathepsin K (CHEMBL3349)
Type SINGLE PROTEIN
Organism Oryctolagus cuniculus

Publication

Beta-substituted cyclohexanecarboxamide cathepsin K inhibitors: modification of the 1,2-disubstituted aromatic core.
Robichaud J, Bayly CI, Black WC, Desmarais S, Léger S, Massé F, McKay DJ, Oballa RM, Pâquet J, Percival MD, Truchon JF, Wesolowski G, Crane SN.
Bioorg Med Chem Lett (2007) 17 : 3146 -3151
PubMed 17408953 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 8.89 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL245580 1 10.00
CHEMBL201914 2 9.52
CHEMBL395698 1 9.40
CHEMBL391959 1 9.00
CHEMBL247587 1 9.00
CHEMBL245759 1 8.70
CHEMBL395697 1 8.30
CHEMBL247783 1 8.30
CHEMBL245381 1 8.22
CHEMBL245579 1 8.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL245580 IC50 = 0.1 nM 10.00
CHEMBL201914 IC50 = 0.3 nM 9.52
CHEMBL395698 IC50 = 0.4 nM 9.40
CHEMBL201914 IC50 = 0.5 nM 9.30
CHEMBL391959 IC50 = 1.0 nM 9.00
CHEMBL247587 IC50 = 1.0 nM 9.00
CHEMBL245759 IC50 = 2.0 nM 8.70
CHEMBL395697 IC50 = 5.0 nM 8.30
CHEMBL247783 IC50 = 5.0 nM 8.30
CHEMBL245381 IC50 = 6.0 nM 8.22
CHEMBL245579 IC50 = 9.0 nM 8.05