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Assay Detail

CHEMBL4389012

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

Binding
Inhibition of Trypanosoma cruzi glucokinase using D-glucose as substrate in presence of ATP and NADPH measured for every 30 secs for 10 mins by resazurin dye based G6PDH-diaphorase coupled fluorescence assay relative to control
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Trypanosoma cruzi
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of antichagasic inhibitors by high-throughput screening with Trypanosoma cruzi glucokinase.
Mercaldi GF, D'Antonio EL, Aguessi A, Rodriguez A, Cordeiro AT.
Bioorg Med Chem Lett (2019) 29 : 1948 -1953
PubMed 31133533 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 5.22 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2430368 1 6.52
CHEMBL1538870 1 6.05
CHEMBL4465026 1 5.80
CHEMBL3290401 1 5.51
CHEMBL4450527 1 5.32
CHEMBL4446779 1 5.28
CHEMBL404233 1 5.26
CHEMBL4524315 1 5.21
CHEMBL4541679 1 5.10
CHEMBL141159 1 5.06
CHEMBL4516907 1 4.84
CHEMBL4541264 1 4.78
CHEMBL1348016 1 4.77
CHEMBL4473339 1 4.52
CHEMBL4515993 1 4.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2430368 IC50 = 300.0 nM 6.52
CHEMBL1538870 IC50 = 900.0 nM 6.05
CHEMBL4465026 IC50 = 1600.0 nM 5.80
CHEMBL3290401 IC50 = 3100.0 nM 5.51
CHEMBL4450527 IC50 = 4800.0 nM 5.32
CHEMBL4446779 IC50 = 5300.0 nM 5.28
CHEMBL404233 IC50 = 5500.0 nM 5.26
CHEMBL4524315 IC50 = 6100.0 nM 5.21
CHEMBL4541679 IC50 = 8000.0 nM 5.10
CHEMBL141159 IC50 = 8700.0 nM 5.06
CHEMBL4516907 IC50 = 14400.0 nM 4.84
CHEMBL4541264 IC50 = 16500.0 nM 4.78
CHEMBL1348016 IC50 = 17100.0 nM 4.77
CHEMBL4473339 IC50 = 30200.0 nM 4.52
CHEMBL4515993 IC50 = 53200.0 nM 4.27