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

CHEMBL4833053

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

Binding
Inhibition of recombinant Trypanosoma cruzi cruzain using Z-FR-AMC as substrate by fluorometry
18
Total Activities
18
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

Structure-Based Optimization of Quinazolines as Cruzain and <i>Tbr</i>CATL Inhibitors.
Barbosa da Silva E, Rocha DA, Fortes IS, Yang W, Monti L, Siqueira-Neto JL, Caffrey CR, McKerrow J, Andrade SF, Ferreira RS.
J Med Chem (2021) 64 : 13054 -13071
PubMed 34461718 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 5.19 7.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1458713 1 7.55
CHEMBL4849695 1 5.62
CHEMBL4855177 1 5.60
CHEMBL4851626 1 5.16
CHEMBL4865594 1 5.14
CHEMBL597248 1 5.10
CHEMBL4848906 1 4.87
CHEMBL4849162 1 4.82
CHEMBL4863654 1 4.80
CHEMBL536813 1 4.75
CHEMBL530354 1 4.75
CHEMBL4878553 1 4.66
CHEMBL4854591 1 4.60
CHEMBL4853084 1 -
CHEMBL4877020 1 -
CHEMBL4856057 1 -
CHEMBL4861314 1 -
CHEMBL4851766 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1458713 IC50 = 28.0 nM 7.55
CHEMBL4849695 IC50 = 2400.0 nM 5.62
CHEMBL4855177 IC50 = 2500.0 nM 5.60
CHEMBL4851626 IC50 = 7000.0 nM 5.16
CHEMBL4865594 IC50 = 7300.0 nM 5.14
CHEMBL597248 IC50 = 8000.0 nM 5.10
CHEMBL4848906 IC50 = 13500.0 nM 4.87
CHEMBL4849162 IC50 = 15000.0 nM 4.82
CHEMBL4863654 IC50 = 16000.0 nM 4.80
CHEMBL536813 IC50 = 18000.0 nM 4.75
CHEMBL530354 IC50 = 18000.0 nM 4.75
CHEMBL4878553 IC50 = 22000.0 nM 4.66
CHEMBL4854591 IC50 = 25000.0 nM 4.60
CHEMBL4853084 IC50 - -
CHEMBL4877020 IC50 - -
CHEMBL4856057 IC50 - -
CHEMBL4861314 IC50 - -
CHEMBL4851766 IC50 - -