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Assay Detail

CHEMBL866102

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

Binding
Inhibition of human cathepsin S
7
Total Activities
7
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 S (CHEMBL2954)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of tetracyclic nonpeptidic biaryl nitrile inhibitors of cathepsin K.
Setti EL, Venkatraman S, Palmer JT, Xie X, Cheung H, Yu W, Wesolowski G, Robichaud J.
Bioorg Med Chem Lett (2006) 16 : 4296 -4299
PubMed 16750630 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 5.37 5.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL184514 1 5.77
CHEMBL213930 1 5.75
CHEMBL213244 1 5.44
CHEMBL212907 1 5.25
CHEMBL212879 1 5.25
CHEMBL213194 1 5.13
CHEMBL211737 1 5.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL184514 Ki = 1695.0 nM 5.77
CHEMBL213930 Ki = 1800.0 nM 5.75
CHEMBL213244 Ki = 3600.0 nM 5.44
CHEMBL212907 Ki = 5600.0 nM 5.25
CHEMBL212879 Ki = 5600.0 nM 5.25
CHEMBL213194 Ki = 7400.0 nM 5.13
CHEMBL211737 Ki = 9500.0 nM 5.02