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Assay Detail

CHEMBL868693

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

Functional
Effect of compound on degradation of collagen in osteoclast bone resorption assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Oryctolagus cuniculus
Cell Type Osteoclast
Confidence 1 — Organism
Curated By Intermediate

Target

Osteoclast (CHEMBL612548)
Type CELL-LINE

Publication

Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity.
Falgueyret JP, Desmarais S, Oballa R, Black WC, Cromlish W, Khougaz K, Lamontagne S, Massé F, Riendeau D, Toulmond S, Percival MD.
J Med Chem (2005) 48 : 7535 -7543
PubMed 16302795 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.15 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL426819 1 8.30
CHEMBL199358 1 7.39
CHEMBL371064 BALICATIB 2.0 1 7.01
CHEMBL184514 1 6.83
CHEMBL200301 1 6.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL426819 IC50 = 5.0 nM 8.30
CHEMBL199358 IC50 = 41.0 nM 7.39
CHEMBL371064 BALICATIB IC50 = 97.0 nM 7.01
CHEMBL184514 IC50 = 149.0 nM 6.83
CHEMBL200301 IC50 = 580.0 nM 6.24