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

CHEMBL4322971

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

Binding
Inhibition of recombinant Trypanosoma cruzi Cruzain expressed in Pichia pastoris using Z-Phe-Arg-AMC substrate incubated for 30 mins by fluorescence based assay
16
Total Activities
16
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

Design of Gallinamide A Analogs as Potent Inhibitors of the Cysteine Proteases Human Cathepsin L and <i>Trypanosoma cruzi</i> Cruzain.
Boudreau PD, Miller BW, McCall LI, Almaliti J, Reher R, Hirata K, Le T, Siqueira-Neto JL, Hook V, Gerwick WH.
J Med Chem (2019) 62 : 9026 -9044
PubMed 31539239 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 8.83 9.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4447348 1 9.60
CHEMBL541700 GALLINAMIDE A 1 9.59
CHEMBL4527930 1 9.33
CHEMBL4482954 1 9.31
CHEMBL4445744 1 9.14
CHEMBL4564747 1 9.12
CHEMBL4527329 1 9.08
CHEMBL4441303 1 8.97
CHEMBL4474668 1 8.97
CHEMBL4527867 1 8.94
CHEMBL4475810 1 8.92
CHEMBL4471760 1 8.87
CHEMBL4457500 1 8.54
CHEMBL4582558 1 8.43
CHEMBL4514842 1 7.43
CHEMBL4468530 1 7.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4447348 IC50 = 0.25 nM 9.60
CHEMBL541700 GALLINAMIDE A IC50 = 0.26 nM 9.59
CHEMBL4527930 IC50 = 0.47 nM 9.33
CHEMBL4482954 IC50 = 0.49 nM 9.31
CHEMBL4445744 IC50 = 0.73 nM 9.14
CHEMBL4564747 IC50 = 0.76 nM 9.12
CHEMBL4527329 IC50 = 0.84 nM 9.08
CHEMBL4441303 IC50 = 1.08 nM 8.97
CHEMBL4474668 IC50 = 1.07 nM 8.97
CHEMBL4527867 IC50 = 1.15 nM 8.94
CHEMBL4475810 IC50 = 1.2 nM 8.92
CHEMBL4471760 IC50 = 1.35 nM 8.87
CHEMBL4457500 IC50 = 2.89 nM 8.54
CHEMBL4582558 IC50 = 3.69 nM 8.43
CHEMBL4514842 IC50 = 37.14 nM 7.43
CHEMBL4468530 IC50 = 81.0 nM 7.09