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Assay Detail

CHEMBL3996812

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

Functional
Anti-plasmodial activity against chloroquine-sensitive Plasmodium falciparum NF54 late 4/5 stage gametocytes assessed as reduction in ATP levels after 24 hrs by BacTiter-Glo reagent based bioluminescence assay
16
Total Activities
16
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

Antimalarial Pyrido[1,2-a]benzimidazoles: Lead Optimization, Parasite Life Cycle Stage Profile, Mechanistic Evaluation, Killing Kinetics, and in Vivo Oral Efficacy in a Mouse Model.
Singh K, Okombo J, Brunschwig C, Ndubi F, Barnard L, Wilkinson C, Njogu PM, Njoroge M, Laing L, Machado M, Prudêncio M, Reader J, Botha M, Nondaba S, Birkholtz LM, Lauterbach S, Churchyard A, Coetzer TL, Burrows JN, Yeates C, Denti P, Wiesner L, Egan TJ, Wittlin S, Chibale K.
J Med Chem (2017) 60 : 1432 -1448
PubMed 28094524 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 5.98 6.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL405110 METHYLENE BLUE ANHYDROUS 4.0 1 6.85
CHEMBL4070434 1 6.34
CHEMBL4100993 1 6.31
CHEMBL4062856 1 6.23
CHEMBL4097609 1 6.17
CHEMBL4074246 1 6.16
CHEMBL4097733 1 6.14
CHEMBL4085896 1 5.99
CHEMBL4079203 1 5.94
CHEMBL4065621 1 5.84
CHEMBL4071478 1 5.78
CHEMBL4097620 1 5.75
CHEMBL4073686 1 5.59
CHEMBL4092272 1 5.58
CHEMBL4071316 1 5.52
CHEMBL4084534 1 5.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL405110 METHYLENE BLUE ANHYDROUS IC50 = 140.0 nM 6.85
CHEMBL4070434 IC50 = 460.0 nM 6.34
CHEMBL4100993 IC50 = 490.0 nM 6.31
CHEMBL4062856 IC50 = 590.0 nM 6.23
CHEMBL4097609 IC50 = 670.0 nM 6.17
CHEMBL4074246 IC50 = 690.0 nM 6.16
CHEMBL4097733 IC50 = 720.0 nM 6.14
CHEMBL4085896 IC50 = 1020.0 nM 5.99
CHEMBL4079203 IC50 = 1160.0 nM 5.94
CHEMBL4065621 IC50 = 1440.0 nM 5.84
CHEMBL4071478 IC50 = 1680.0 nM 5.78
CHEMBL4097620 IC50 = 1770.0 nM 5.75
CHEMBL4073686 IC50 = 2570.0 nM 5.59
CHEMBL4092272 IC50 = 2660.0 nM 5.58
CHEMBL4071316 IC50 = 3020.0 nM 5.52
CHEMBL4084534 IC50 = 3630.0 nM 5.44