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Assay Detail

CHEMBL4830600

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

Functional
Antiplasmodial activity against Plasmodium falciparum 3D7 infected in human erythrocyte assessed as intraerythrocytic growth inhibition incubated for 72 hrs by DAPI-staining based imaging analysis
49
Total Activities
49
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

Discovery and Structure-Activity Relationships of Quinazolinone-2-carboxamide Derivatives as Novel Orally Efficacious Antimalarials.
Laleu B, Akao Y, Ochida A, Duffy S, Lucantoni L, Shackleford DM, Chen G, Katneni K, Chiu FCK, White KL, Chen X, Sturm A, Dechering KJ, Crespo B, Sanz LM, Wang B, Wittlin S, Charman SA, Avery VM, Cho N, Kamaura M.
J Med Chem (2021) 64 : 12582 -12602
PubMed 34437804 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 49 6.24 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL361497 ARTESUNATE 4.0 1 9.22
CHEMBL36 PYRIMETHAMINE 4.0 1 8.22
CHEMBL4874145 1 7.60
CHEMBL76 CHLOROQUINE 4.0 1 7.55
CHEMBL4857536 1 7.27
CHEMBL4846372 1 7.14
CHEMBL4846579 1 6.80
CHEMBL4859763 1 6.75
CHEMBL4862256 1 6.55
CHEMBL4871489 1 6.51
CHEMBL4852040 1 6.39
CHEMBL4857901 1 6.38
CHEMBL4872525 1 6.26
CHEMBL4859817 1 6.23
CHEMBL4866642 1 6.05
CHEMBL4853205 1 5.94
CHEMBL4854656 1 5.94
CHEMBL4858796 1 5.94
CHEMBL4859826 1 5.80
CHEMBL4850316 1 5.79
CHEMBL4857112 1 5.78
CHEMBL4846590 1 5.72
CHEMBL4857049 1 5.72
CHEMBL3359091 1 5.62
CHEMBL4875826 1 5.50
CHEMBL4876537 1 5.43
CHEMBL4846594 1 5.35
CHEMBL4856504 1 5.32
CHEMBL4858445 1 5.29
CHEMBL4868499 1 5.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL361497 ARTESUNATE IC50 = 0.6 nM 9.22
CHEMBL36 PYRIMETHAMINE IC50 = 6.0 nM 8.22
CHEMBL4874145 IC50 = 25.0 nM 7.60
CHEMBL76 CHLOROQUINE IC50 = 28.0 nM 7.55
CHEMBL4857536 IC50 = 54.0 nM 7.27
CHEMBL4846372 IC50 = 73.0 nM 7.14
CHEMBL4846579 IC50 = 160.0 nM 6.80
CHEMBL4859763 IC50 = 180.0 nM 6.75
CHEMBL4862256 IC50 = 280.0 nM 6.55
CHEMBL4871489 IC50 = 310.0 nM 6.51
CHEMBL4852040 IC50 = 410.0 nM 6.39
CHEMBL4857901 IC50 = 420.0 nM 6.38
CHEMBL4872525 IC50 = 550.0 nM 6.26
CHEMBL4859817 IC50 = 590.0 nM 6.23
CHEMBL4866642 IC50 = 890.0 nM 6.05
CHEMBL4853205 IC50 = 1160.0 nM 5.94
CHEMBL4858796 IC50 = 1150.0 nM 5.94
CHEMBL4854656 IC50 = 1160.0 nM 5.94
CHEMBL4859826 IC50 = 1580.0 nM 5.80
CHEMBL4850316 IC50 = 1620.0 nM 5.79
CHEMBL4857112 IC50 = 1670.0 nM 5.78
CHEMBL4846590 IC50 = 1900.0 nM 5.72
CHEMBL4857049 IC50 = 1890.0 nM 5.72
CHEMBL3359091 IC50 = 2380.0 nM 5.62
CHEMBL4875826 IC50 = 3190.0 nM 5.50
CHEMBL4876537 IC50 = 3670.0 nM 5.43
CHEMBL4846594 IC50 = 4460.0 nM 5.35
CHEMBL4856504 IC50 = 4760.0 nM 5.32
CHEMBL4858445 IC50 = 5130.0 nM 5.29
CHEMBL4868499 IC50 = 5540.0 nM 5.26
CHEMBL4858666 IC50 = 5940.0 nM 5.23
CHEMBL4871069 IC50 = 6970.0 nM 5.16
CHEMBL3359088 IC50 > 20000.0 nM -
CHEMBL3359090 IC50 > 20000.0 nM -
CHEMBL4856967 IC50 > 20000.0 nM -
CHEMBL4859040 IC50 > 20000.0 nM -
CHEMBL4864167 IC50 > 20000.0 nM -
CHEMBL4873366 IC50 > 20000.0 nM -
CHEMBL4854003 IC50 > 20000.0 nM -
CHEMBL4855410 IC50 > 20000.0 nM -
CHEMBL4857192 IC50 > 20000.0 nM -
CHEMBL4868180 IC50 > 20000.0 nM -
CHEMBL4865937 IC50 > 20000.0 nM -
CHEMBL4861451 IC50 > 20000.0 nM -
CHEMBL4856624 IC50 > 20000.0 nM -
CHEMBL4856479 IC50 > 20000.0 nM -
CHEMBL4848733 IC50 > 20000.0 nM -
CHEMBL269671 ARTEMISININ IC50 - -
CHEMBL1450 ATOVAQUONE IC50 - -