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Assay Detail

CHEMBL2174685

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

Functional
Inhibition of osteoclastogenesis in human bone marrow-derived stem cells assessed as reduction of pit formation by measuring TRACP5b activity after 7 days by bone TRAP assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Pharmacokinetic benefits of 3,4-dimethoxy substitution of a phenyl ring and design of isosteres yielding orally available cathepsin K inhibitors.
Crawford JJ, Kenny PW, Bowyer J, Cook CR, Finlayson JE, Heyes C, Highton AJ, Hudson JA, Jestel A, Krapp S, Martin S, Macfaul PA, McDermott BP, McGuire TM, Morley AD, Morris JJ, Page KM, Ribeiro LR, Sawney H, Steinbacher S, Smith C, Dossetter AG.
J Med Chem (2012) 55 : 8827 -8837
PubMed 22984809 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.28 7.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL371064 BALICATIB 2.0 1 7.58
CHEMBL2163587 1 7.50
CHEMBL2172005 1 7.40
CHEMBL481611 ODANACATIB 3.0 1 7.00
CHEMBL2171993 1 6.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL371064 BALICATIB IC50 = 26.6 nM 7.58
CHEMBL2163587 IC50 = 32.0 nM 7.50
CHEMBL2172005 IC50 = 40.0 nM 7.40
CHEMBL481611 ODANACATIB IC50 = 100.0 nM 7.00
CHEMBL2171993 IC50 = 126.0 nM 6.90