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Assay Detail

CHEMBL881773

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Binding
Inhibitory activity against cathepsin S from human
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cathepsin S (CHEMBL2954)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Trifluoroethylamines as amide isosteres in inhibitors of cathepsin K.
Black WC, Bayly CI, Davis DE, Desmarais S, Falgueyret JP, Léger S, Li CS, Massé F, McKay DJ, Palmer JT, Percival MD, Robichaud J, Tsou N, Zamboni R.
Bioorg Med Chem Lett (2005) 15 : 4741 -4744
PubMed 16154747 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.40 6.99

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL182956 1 6.99
CHEMBL372979 1 6.92
CHEMBL195454 1 6.35
CHEMBL195505 1 6.04
CHEMBL184514 1 5.70
CHEMBL426819 1 -
CHEMBL194914 1 -
CHEMBL371133 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL182956 IC50 = 102.0 nM 6.99
CHEMBL372979 IC50 = 121.0 nM 6.92
CHEMBL195454 IC50 = 451.0 nM 6.35
CHEMBL195505 IC50 = 902.0 nM 6.04
CHEMBL184514 IC50 = 2010.0 nM 5.70
CHEMBL426819 IC50 > 10000.0 nM -
CHEMBL194914 IC50 > 10000.0 nM -
CHEMBL371133 IC50 > 10000.0 nM -