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Assay Detail

CHEMBL5359218

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Binding
Inhibition of Plasmodium falciparum Threonyl tRNA synthetase
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Plasmodium falciparum
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

threonine--tRNA ligase (CHEMBL5465377)
Type SINGLE PROTEIN
Organism Plasmodium falciparum

Publication

Discovery of Malarial Threonyl tRNA Synthetase Inhibitors by Screening of a Focused Fragment Library.
Bolsakova J, Bobrovs R, Varacheva L, Rudnickiha A, Kanepe I, Parisini E, Jirgensons A.
ACS Med Chem Lett (2024) 15 : 76 -80
PubMed 38229753 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.45 7.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL70590 BORRELIDIN 1 7.37
CHEMBL2311925 1 7.24
CHEMBL1163068 1 6.80
CHEMBL5438745 1 6.36
CHEMBL5400120 1 4.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL70590 BORRELIDIN IC50 = 43.0 nM 7.37
CHEMBL2311925 IC50 = 57.0 nM 7.24
CHEMBL1163068 IC50 = 160.0 nM 6.80
CHEMBL5438745 IC50 = 440.0 nM 6.36
CHEMBL5400120 IC50 = 33000.0 nM 4.48