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Assay Detail

CHEMBL664074

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Binding
Inhibition of cruzain from Trypanosoma cruzi
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Trypanosoma cruzi
Confidence 9 — Direct single protein target
Curated By Expert

Target

Cruzipain (CHEMBL3563)
Type SINGLE PROTEIN
Organism Trypanosoma cruzi

Publication

Synthesis and structure-activity relationships of parasiticidal thiosemicarbazone cysteine protease inhibitors against Plasmodium falciparum, Trypanosoma brucei, and Trypanosoma cruzi.
Greenbaum DC, Mackey Z, Hansell E, Doyle P, Gut J, Caffrey CR, Lehrman J, Rosenthal PJ, McKerrow JH, Chibale K.
J Med Chem (2004) 47 : 3212 -3219
PubMed 15163200 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 5.42 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL88734 1 7.22
CHEMBL326220 1 5.30
CHEMBL108700 1 5.30
CHEMBL323975 1 5.30
CHEMBL108101 1 5.30
CHEMBL109619 1 5.30
CHEMBL108035 1 5.10
CHEMBL108865 1 5.00
CHEMBL109893 1 5.00
CHEMBL108077 1 -
CHEMBL107612 1 -
CHEMBL416771 1 -
CHEMBL111632 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL88734 IC50 = 60.0 nM 7.22
CHEMBL326220 IC50 = 5000.0 nM 5.30
CHEMBL108700 IC50 = 5000.0 nM 5.30
CHEMBL323975 IC50 = 5000.0 nM 5.30
CHEMBL108101 IC50 = 5000.0 nM 5.30
CHEMBL109619 IC50 = 5000.0 nM 5.30
CHEMBL108035 IC50 = 8000.0 nM 5.10
CHEMBL108865 IC50 = 10000.0 nM 5.00
CHEMBL109893 IC50 = 10000.0 nM 5.00
CHEMBL108077 IC50 > 20000.0 nM -
CHEMBL107612 IC50 > 20000.0 nM -
CHEMBL416771 IC50 > 20000.0 nM -
CHEMBL111632 IC50 > 20000.0 nM -