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Assay Detail

CHEMBL4327289

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Functional
Antiplasmodial activity against Plasmodium falciparum Dd2 infected in human erythrocytes assessed as reduction in [3H]-hypoxanthine incorporation measured after 48 hrs by microbeta liquid scintillation counting method
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Plasmodium falciparum
Confidence 1 — Organism
Curated By Autocuration

Target

Plasmodium falciparum (CHEMBL364)
Type ORGANISM
Organism Plasmodium falciparum

Publication

Identification of novel quinazoline derivatives as potent antiplasmodial agents.
Bouchut A, Rotili D, Pierrot C, Valente S, Lafitte S, Schultz J, Hoglund U, Mazzone R, Lucidi A, Fabrizi G, Pechalrieu D, Arimondo PB, Skinner-Adams TS, Chua MJ, Andrews KT, Mai A, Khalife J.
Eur J Med Chem (2019) 161 : 277 -291
PubMed 30366254 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.81 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3426803 1 8.40
CHEMBL4461581 1 8.21
CHEMBL569864 1 8.01
CHEMBL4550522 1 7.87
CHEMBL1231795 1 7.78
CHEMBL4558658 1 7.73
CHEMBL4537137 1 7.37
CHEMBL4527662 1 7.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3426803 IC50 = 4.0 nM 8.40
CHEMBL4461581 IC50 = 6.1 nM 8.21
CHEMBL569864 IC50 = 9.7 nM 8.01
CHEMBL4550522 IC50 = 13.5 nM 7.87
CHEMBL1231795 IC50 = 16.8 nM 7.78
CHEMBL4558658 IC50 = 18.5 nM 7.73
CHEMBL4537137 IC50 = 42.6 nM 7.37
CHEMBL4527662 IC50 = 81.3 nM 7.09