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Assay Detail

CHEMBL945093

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Binding
Inhibition of cathepsin S in human ramos cells
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type Ramos
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Cathepsin S (CHEMBL2954)
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 4 7.00 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL203665 RELACATIB 2.0 1 8.10
CHEMBL481611 ODANACATIB 3.0 1 7.35
CHEMBL437501 1 7.02
CHEMBL371064 BALICATIB 2.0 1 5.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL203665 RELACATIB IC50 = 8.0 nM 8.10
CHEMBL481611 ODANACATIB IC50 = 45.0 nM 7.35
CHEMBL437501 IC50 = 95.0 nM 7.02
CHEMBL371064 BALICATIB IC50 = 2900.0 nM 5.54