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Assay Detail

CHEMBL4373129

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

Functional
Antiplasmodial activity against chloroquine-sensitive final late stage of Plasmodium falciparum NF54-Mal8p1.16-GFP-Luc gametocytes after 24 hrs by BacTiter-Glo assay
12
Total Activities
12
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

Structure-Activity Relationship Studies and Plasmodium Life Cycle Profiling Identifies Pan-Active N-Aryl-3-trifluoromethyl Pyrido[1,2- a]benzimidazoles Which Are Efficacious in an in Vivo Mouse Model of Malaria.
Mayoka G, Njoroge M, Okombo J, Gibhard L, Sanches-Vaz M, Fontinha D, Birkholtz LM, Reader J, van der Watt M, Coetzer TL, Lauterbach S, Churchyard A, Bezuidenhout B, Egan TJ, Yeates C, Wittlin S, Prudêncio M, Chibale K.
J Med Chem (2019) 62 : 1022 -1035
PubMed 30562027 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.97 6.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4571751 1 6.68
CHEMBL4468890 1 6.57
CHEMBL4459380 1 6.43
CHEMBL4549480 1 6.22
CHEMBL4577940 1 6.16
CHEMBL4464908 1 6.13
CHEMBL405110 METHYLENE BLUE ANHYDROUS 4.0 1 6.05
CHEMBL4457843 1 5.78
CHEMBL4466654 1 5.70
CHEMBL4443956 1 5.61
CHEMBL4576616 1 5.48
CHEMBL367149 DOCONEXENT 3.0 1 4.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4571751 IC50 = 210.0 nM 6.68
CHEMBL4468890 IC50 = 270.0 nM 6.57
CHEMBL4459380 IC50 = 370.0 nM 6.43
CHEMBL4549480 IC50 = 600.0 nM 6.22
CHEMBL4577940 IC50 = 690.0 nM 6.16
CHEMBL4464908 IC50 = 740.0 nM 6.13
CHEMBL405110 METHYLENE BLUE ANHYDROUS IC50 = 900.0 nM 6.05
CHEMBL4457843 IC50 = 1670.0 nM 5.78
CHEMBL4466654 IC50 = 2000.0 nM 5.70
CHEMBL4443956 IC50 = 2480.0 nM 5.61
CHEMBL4576616 IC50 = 3320.0 nM 5.48
CHEMBL367149 DOCONEXENT IC50 = 14000.0 nM 4.85