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Assay Detail

CHEMBL1671573

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

Unclassified
Ratio of product of IC50 for rabbit bone resorption and IC50 for humanized rabbit cathepsin K to IC50 for rabbit cathepsin K
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Unclassified
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Difluoroethylamines as an amide isostere in inhibitors of cathepsin K.
Isabel E, Mellon C, Boyd MJ, Chauret N, Deschênes D, Desmarais S, Falgueyret JP, Gauthier JY, Khougaz K, Lau CK, Léger S, Levorse DA, Li CS, Massé F, Percival MD, Roy B, Scheigetz J, Thérien M, Truong VL, Wesolowski G, Young RN, Zamboni R, Black WC.
Bioorg Med Chem Lett (2011) 21 : 920 -923
PubMed 21232956 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 8.15 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1669442 1 8.70
CHEMBL249495 1 8.52
CHEMBL437501 1 8.52
CHEMBL1669441 1 8.40
CHEMBL481611 ODANACATIB 3.0 1 8.30
CHEMBL1669437 1 8.05
CHEMBL1669436 1 8.00
CHEMBL1669438 1 7.82
CHEMBL1669440 1 7.68
CHEMBL1669439 1 7.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1669442 IC50 = 2.0 nM 8.70
CHEMBL249495 IC50 = 3.0 nM 8.52
CHEMBL437501 IC50 = 3.0 nM 8.52
CHEMBL1669441 IC50 = 4.0 nM 8.40
CHEMBL481611 ODANACATIB IC50 = 5.0 nM 8.30
CHEMBL1669437 IC50 = 9.0 nM 8.05
CHEMBL1669436 IC50 = 10.0 nM 8.00
CHEMBL1669438 IC50 = 15.0 nM 7.82
CHEMBL1669440 IC50 = 21.0 nM 7.68
CHEMBL1669439 IC50 = 32.0 nM 7.50