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Assay Detail

CHEMBL4835696

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

Functional
Antiplasmodial activity against asexual stage (IV/V) Plasmodium falciparum NF54 late gametocytes transfected with GFP-Luc assessed as inhibition of exflagellation of male gametes incubated for 48 hrs by microscopy based luciferase reporter gene assay relative to control
6
Total Activities
6
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 Benzimidazole Derivatives Incorporating Phenolic Mannich Base Side Chains Inhibit Microtubule and Hemozoin Formation: Structure-Activity Relationship and <i>In Vivo</i> Oral Efficacy Studies.
Dziwornu GA, Coertzen D, Leshabane M, Korkor CM, Cloete CK, Njoroge M, Gibhard L, Lawrence N, Reader J, van der Watt M, Wittlin S, Birkholtz LM, Chibale K, Chibale K.
J Med Chem (2021) 64 : 5198 -5215
PubMed 33844521 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.07 6.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL405110 METHYLENE BLUE ANHYDROUS 4.0 1 6.85
CHEMBL4853530 1 5.72
CHEMBL4853001 1 5.63
CHEMBL4879051 1 -
CHEMBL4846075 1 -
CHEMBL4862272 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL405110 METHYLENE BLUE ANHYDROUS IC50 = 140.0 nM 6.85
CHEMBL4853530 IC50 = 1900.0 nM 5.72
CHEMBL4853001 IC50 = 2330.0 nM 5.63
CHEMBL4879051 IC50 > 5000.0 nM -
CHEMBL4846075 IC50 > 5000.0 nM -
CHEMBL4862272 IC50 > 5000.0 nM -