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Assay Detail

CHEMBL945079

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

Binding
Inhibition of humanized rabbit cathepsin K
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cathepsin K (CHEMBL268)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K.
Gauthier JY, Chauret N, Cromlish W, Desmarais S, Duong LT, Falgueyret JP, Kimmel DB, Lamontagne S, Léger S, LeRiche T, Li CS, Massé F, McKay DJ, Nicoll-Griffith DA, Oballa RM, Palmer JT, Percival MD, Riendeau D, Robichaud J, Rodan GA, Rodan SB, Seto C, Thérien M, Truong VL, Venuti MC, Wesolowski G, Young RN, Zamboni R, Black WC.
Bioorg Med Chem Lett (2008) 18 : 923 -928
PubMed 18226527 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 9.11 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL437501 1 9.70
CHEMBL481611 ODANACATIB 3.0 1 9.70
CHEMBL399733 1 9.70
CHEMBL398910 1 9.52
CHEMBL252383 1 9.52
CHEMBL252571 1 9.40
CHEMBL203665 RELACATIB 2.0 1 9.30
CHEMBL399361 1 9.22
CHEMBL252179 1 9.22
CHEMBL250294 1 8.92
CHEMBL252784 1 8.82
CHEMBL428417 1 8.40
CHEMBL252382 1 8.29
CHEMBL252581 1 7.80
CHEMBL252582 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL437501 IC50 = 0.2 nM 9.70
CHEMBL481611 ODANACATIB IC50 = 0.2 nM 9.70
CHEMBL399733 IC50 = 0.2 nM 9.70
CHEMBL398910 IC50 = 0.3 nM 9.52
CHEMBL252383 IC50 = 0.3 nM 9.52
CHEMBL252571 IC50 = 0.4 nM 9.40
CHEMBL203665 RELACATIB IC50 = 0.5 nM 9.30
CHEMBL399361 IC50 = 0.6 nM 9.22
CHEMBL252179 IC50 = 0.6 nM 9.22
CHEMBL250294 IC50 = 1.2 nM 8.92
CHEMBL252784 IC50 = 1.5 nM 8.82
CHEMBL428417 IC50 = 4.0 nM 8.40
CHEMBL252382 IC50 = 5.1 nM 8.29
CHEMBL252581 IC50 = 16.0 nM 7.80
CHEMBL252582 IC50 < 0.2 nM -