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Assay Detail

CHEMBL875703

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

Binding
Inhibition of Cbz-Phe-Arg-AMC binding to Cathepsin K cysteine protease
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Cathepsin K (CHEMBL268)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

6-Acylamino-penam derivatives: synthesis and inhibition of cathepsins B, L, K, and S.
Zhou NE, Kaleta J, Purisima E, Menard R, Micetich RG, Singh R.
Bioorg Med Chem Lett (2002) 12 : 3417 -3419
PubMed 12419374 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.89 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL326093 1 9.30
CHEMBL113706 1 8.74
CHEMBL117928 1 8.60
CHEMBL332025 1 8.30
CHEMBL116041 1 8.22
CHEMBL323637 1 8.12
CHEMBL114410 1 8.12
CHEMBL326342 1 7.46
CHEMBL323638 1 6.40
CHEMBL115822 1 5.60
CHEMBL421054 1 -
CHEMBL323704 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL326093 IC50 = 0.5 nM 9.30
CHEMBL113706 IC50 = 1.8 nM 8.74
CHEMBL117928 IC50 = 2.5 nM 8.60
CHEMBL332025 IC50 = 5.0 nM 8.30
CHEMBL116041 IC50 = 6.0 nM 8.22
CHEMBL323637 IC50 = 7.5 nM 8.12
CHEMBL114410 IC50 = 7.6 nM 8.12
CHEMBL326342 IC50 = 35.0 nM 7.46
CHEMBL323638 IC50 = 400.0 nM 6.40
CHEMBL115822 IC50 = 2500.0 nM 5.60
CHEMBL421054 IC50 > 2500.0 nM -
CHEMBL323704 IC50 > 2500.0 nM -