Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL1109341

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

Binding
Inhibition of Trypanosoma cruzi cruzain after 5 mins
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cruzipain (CHEMBL3563)
Type SINGLE PROTEIN
Organism Trypanosoma cruzi

Publication

Novel non-peptidic vinylsulfones targeting the S2 and S3 subsites of parasite cysteine proteases.
Bryant C, Kerr ID, Debnath M, Ang KK, Ratnam J, Ferreira RS, Jaishankar P, Zhao D, Arkin MR, McKerrow JH, Brinen LS, Renslo AR.
Bioorg Med Chem Lett (2009) 19 : 6218 -6221
PubMed 19773167 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.07 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL91704 K-777 2.0 1 8.40
CHEMBL1079162 1 7.30
CHEMBL1078779 1 6.00
CHEMBL1079067 1 6.00
CHEMBL1078778 1 5.70
CHEMBL1078855 1 5.70
CHEMBL1078981 1 5.30
CHEMBL1079068 1 5.22
CHEMBL1078675 1 5.00
CHEMBL1079105 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL91704 K-777 IC50 = 4.0 nM 8.40
CHEMBL1079162 IC50 = 50.0 nM 7.30
CHEMBL1078779 IC50 = 1000.0 nM 6.00
CHEMBL1079067 IC50 = 1000.0 nM 6.00
CHEMBL1078778 IC50 = 2000.0 nM 5.70
CHEMBL1078855 IC50 = 2000.0 nM 5.70
CHEMBL1078981 IC50 = 5000.0 nM 5.30
CHEMBL1079068 IC50 = 6000.0 nM 5.22
CHEMBL1078675 IC50 = 10000.0 nM 5.00
CHEMBL1079105 IC50 > 100000.0 nM -