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Assay Detail

CHEMBL1073796

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

Functional
Decrease in bone resorption assessed as corrected bone resorption measured as ratio of bone resorption IC50 x humanized rabbit cathepsin K IC50 to rabbit cathepsin K IC50 equation
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Tissue Bone element
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

The discovery of MK-0674, an orally bioavailable cathepsin K inhibitor.
Isabel E, Bateman KP, Chauret N, Cromlish W, Desmarais S, Duong LT, Falgueyret JP, Gauthier JY, Lamontagne S, Lau CK, Léger S, LeRiche T, Lévesque JF, Li CS, Massé F, McKay DJ, Mellon C, Nicoll-Griffith DA, Oballa RM, Percival MD, Riendeau D, Robichaud J, Rodan GA, Rodan SB, Seto C, Thérien M, Truong VL, Wesolowski G, Young RN, Zamboni R, Black WC.
Bioorg Med Chem Lett (2010) 20 : 887 -892
PubMed 20061146 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 7.93 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL481611 ODANACATIB 3.0 1 8.30
CHEMBL599272 1 8.15
CHEMBL605341 1 8.10
CHEMBL600793 1 8.10
CHEMBL603899 1 8.00
CHEMBL597018 1 8.00
CHEMBL598502 1 7.92
CHEMBL605122 1 7.89
CHEMBL598298 1 7.85
CHEMBL597426 1 7.46
CHEMBL598299 1 7.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL481611 ODANACATIB IC50 = 5.0 nM 8.30
CHEMBL599272 IC50 = 7.0 nM 8.15
CHEMBL605341 IC50 = 8.0 nM 8.10
CHEMBL600793 IC50 = 8.0 nM 8.10
CHEMBL603899 IC50 = 10.0 nM 8.00
CHEMBL597018 IC50 = 10.0 nM 8.00
CHEMBL598502 IC50 = 12.0 nM 7.92
CHEMBL605122 IC50 = 13.0 nM 7.89
CHEMBL598298 IC50 = 14.0 nM 7.85
CHEMBL597426 IC50 = 35.0 nM 7.46
CHEMBL598299 IC50 = 35.0 nM 7.46