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Assay Detail

CHEMBL1023015

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

Binding
Inhibition of Trypanosoma cruzi recombinant glycosomal GAPDH expressed in Escherichia coli by spectrophotometry
17
Total Activities
17
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Glyceraldehyde-3-phosphate dehydrogenase, glycosomal (CHEMBL5926)
Type SINGLE PROTEIN
Organism Trypanosoma cruzi

Publication

Discovery of novel Trypanosoma cruzi glyceraldehyde-3-phosphate dehydrogenase inhibitors.
Freitas RF, Prokopczyk IM, Zottis A, Oliva G, Andricopulo AD, Trevisan MT, Vilegas W, Silva MG, Montanari CA.
Bioorg Med Chem (2009) 17 : 2476 -2482
PubMed 19254846 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 4.73 7.00
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL552521 1 7.00
CHEMBL366942 1 5.30
CHEMBL464924 1 4.92
CHEMBL67599 1 4.75
CHEMBL464925 1 4.42
CHEMBL266564 TILIROSIDE 1 4.34
CHEMBL1231470 CHALEPIN 1 4.19
CHEMBL465536 1 4.16
CHEMBL474167 1 4.09
CHEMBL464404 CASTANIN 1 4.08
CHEMBL169 URSOLIC ACID 2.0 1 -
CHEMBL6466 COUMARIN 4.0 1 -
CHEMBL277156 1 -
CHEMBL464825 MANGIFERIN 1 -
CHEMBL50 QUERCETIN 3.0 1 -
CHEMBL464507 GUAJAVERIN 1 -
CHEMBL51628 UMBELLIFERONE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL552521 IC50 = 100.0 nM 7.00
CHEMBL366942 IC50 = 5000.0 nM 5.30
CHEMBL464924 IC50 = 12000.0 nM 4.92
CHEMBL67599 IC50 = 17800.0 nM 4.75
CHEMBL464925 IC50 = 38000.0 nM 4.42
CHEMBL266564 TILIROSIDE IC50 = 46000.0 nM 4.34
CHEMBL1231470 CHALEPIN IC50 = 64000.0 nM 4.19
CHEMBL465536 IC50 = 69000.0 nM 4.16
CHEMBL474167 IC50 = 81000.0 nM 4.09
CHEMBL464404 CASTANIN IC50 = 84000.0 nM 4.08
CHEMBL169 URSOLIC ACID Inhibition = 25.0 % -
CHEMBL6466 COUMARIN IC50 = 691830.0 nM -
CHEMBL277156 IC50 = 161000.0 nM -
CHEMBL464825 MANGIFERIN IC50 = 149000.0 nM -
CHEMBL50 QUERCETIN IC50 = 142000.0 nM -
CHEMBL464507 GUAJAVERIN IC50 = 140000.0 nM -
CHEMBL51628 UMBELLIFERONE IC50 = 616580.0 nM -