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Assay Detail

CHEMBL659926

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

Binding
In vitro Inhibitory activity against Cathepsin S cysteine protease by using Cbz-Val-Arg-AMC
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cathepsin S (CHEMBL2954)
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 10 7.64 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL114410 1 9.15
CHEMBL323638 1 8.52
CHEMBL113706 1 8.34
CHEMBL116041 1 8.10
CHEMBL326093 1 8.00
CHEMBL117928 1 7.24
CHEMBL326342 1 7.16
CHEMBL323637 1 6.68
CHEMBL115822 1 5.60
CHEMBL323704 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL114410 IC50 = 0.7 nM 9.15
CHEMBL323638 IC50 = 3.0 nM 8.52
CHEMBL113706 IC50 = 4.6 nM 8.34
CHEMBL116041 IC50 = 8.0 nM 8.10
CHEMBL326093 IC50 = 10.0 nM 8.00
CHEMBL117928 IC50 = 58.0 nM 7.24
CHEMBL326342 IC50 = 70.0 nM 7.16
CHEMBL323637 IC50 = 210.0 nM 6.68
CHEMBL115822 IC50 = 2500.0 nM 5.60
CHEMBL323704 IC50 > 2500.0 nM -