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Assay Detail

CHEMBL863710

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

Functional
Effect on collagen accumulation in osteoclast bone resorption assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Osteoclast
Confidence 1 — Organism
Curated By Intermediate

Target

Osteoclast (CHEMBL612548)
Type CELL-LINE

Publication

Structure activity relationships of 5-, 6-, and 7-methyl-substituted azepan-3-one cathepsin K inhibitors.
Yamashita DS, Marquis RW, Xie R, Nidamarthy SD, Oh HJ, Jeong JU, Erhard KF, Ward KW, Roethke TJ, Smith BR, Cheng HY, Geng X, Lin F, Offen PH, Wang B, Nevins N, Head MS, Haltiwanger RC, Narducci Sarjeant AA, Liable-Sands LM, Zhao B, Smith WW, Janson CA, Gao E, Tomaszek T, McQueney M, James IE, Gress CJ, Zembryki DL, Lark MW, Veber DF.
J Med Chem (2006) 49 : 1597 -1612
PubMed 16509577 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.58 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL203665 RELACATIB 2.0 1 7.70
CHEMBL205172 1 7.70
CHEMBL202668 1 7.70
CHEMBL286364 1 7.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL203665 RELACATIB IC50 = 20.0 nM 7.70
CHEMBL205172 IC50 = 20.0 nM 7.70
CHEMBL202668 IC50 = 20.0 nM 7.70
CHEMBL286364 IC50 = 63.0 nM 7.20