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Assay Detail

CHEMBL891433

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

Binding
Inhibition of human recombinant cathepsin S
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 Intermediate

Target

Cathepsin S (CHEMBL2954)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Acyclic, orally bioavailable ketone-based cathepsin K inhibitors.
Barrett DG, Catalano JG, Deaton DN, Long ST, McFadyen RB, Miller AB, Miller LR, Samano V, Tavares FX, Wells-Knecht KJ, Wright LL, Zhou HQ.
Bioorg Med Chem Lett (2007) 17 : 22 -27
PubMed 17157021 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 7.75 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL232712 1 8.10
CHEMBL232713 1 8.00
CHEMBL233706 1 8.00
CHEMBL393354 1 7.96
CHEMBL232520 1 7.82
CHEMBL232911 1 7.72
CHEMBL31545 1 7.70
CHEMBL393673 1 7.58
CHEMBL203463 1 7.46
CHEMBL540964 1 7.19
CHEMBL234367 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL232712 IC50 = 7.9 nM 8.10
CHEMBL232713 IC50 = 10.0 nM 8.00
CHEMBL233706 IC50 = 10.0 nM 8.00
CHEMBL393354 IC50 = 11.0 nM 7.96
CHEMBL232520 IC50 = 15.0 nM 7.82
CHEMBL232911 IC50 = 19.0 nM 7.72
CHEMBL31545 IC50 = 20.0 nM 7.70
CHEMBL393673 IC50 = 26.0 nM 7.58
CHEMBL203463 IC50 = 35.0 nM 7.46
CHEMBL540964 IC50 = 64.0 nM 7.19
CHEMBL234367 IC50 = 0.21 nM -