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Assay Detail

CHEMBL929238

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Binding
Inhibition of human cathepsin B
13
Total Activities
13
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 B (CHEMBL4072)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of trypanocidal thiosemicarbazone inhibitors of rhodesain and TbcatB.
Mallari JP, Shelat A, Kosinski A, Caffrey CR, Connelly M, Zhu F, McKerrow JH, Guy RK.
Bioorg Med Chem Lett (2008) 18 : 2883 -2885
PubMed 18420405 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 5.64 6.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL407264 1 6.68
CHEMBL260921 1 6.52
CHEMBL259379 1 6.52
CHEMBL404938 1 5.77
CHEMBL261438 1 5.75
CHEMBL410086 1 5.52
CHEMBL261657 THIOSEMICARBAZONE STANDARD 1 5.48
CHEMBL261307 1 5.35
CHEMBL406601 1 5.31
CHEMBL258588 1 5.22
CHEMBL402465 1 4.89
CHEMBL261218 1 4.66
CHEMBL429858 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL407264 IC50 = 210.0 nM 6.68
CHEMBL260921 IC50 = 300.0 nM 6.52
CHEMBL259379 IC50 = 300.0 nM 6.52
CHEMBL404938 IC50 = 1700.0 nM 5.77
CHEMBL261438 IC50 = 1800.0 nM 5.75
CHEMBL410086 IC50 = 3000.0 nM 5.52
CHEMBL261657 THIOSEMICARBAZONE STANDARD IC50 = 3300.0 nM 5.48
CHEMBL261307 IC50 = 4500.0 nM 5.35
CHEMBL406601 IC50 = 4900.0 nM 5.31
CHEMBL258588 IC50 = 6000.0 nM 5.22
CHEMBL402465 IC50 = 13000.0 nM 4.89
CHEMBL261218 IC50 = 22000.0 nM 4.66
CHEMBL429858 IC50 > 25000.0 nM -