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Assay Detail

CHEMBL4835672

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

Functional
Antiplasmodial activity against asexual stage (I/III) Plasmodium falciparum NF54 early 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
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 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 16 6.19 7.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4853530 1 7.25
CHEMBL4846075 1 7.01
CHEMBL4851068 1 6.96
CHEMBL405110 METHYLENE BLUE ANHYDROUS 4.0 1 6.72
CHEMBL4853001 1 6.68
CHEMBL4879051 1 6.37
CHEMBL4862272 1 6.34
CHEMBL4870469 1 6.28
CHEMBL4865588 1 6.16
CHEMBL4873869 1 6.06
CHEMBL4869087 1 6.04
CHEMBL4872706 1 6.00
CHEMBL4861409 1 5.84
CHEMBL4871841 1 5.65
CHEMBL4853995 1 5.51
CHEMBL4873489 1 4.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4853530 IC50 = 56.0 nM 7.25
CHEMBL4846075 IC50 = 97.0 nM 7.01
CHEMBL4851068 IC50 = 110.0 nM 6.96
CHEMBL405110 METHYLENE BLUE ANHYDROUS IC50 = 190.0 nM 6.72
CHEMBL4853001 IC50 = 210.0 nM 6.68
CHEMBL4879051 IC50 = 430.0 nM 6.37
CHEMBL4862272 IC50 = 460.0 nM 6.34
CHEMBL4870469 IC50 = 520.0 nM 6.28
CHEMBL4865588 IC50 = 690.0 nM 6.16
CHEMBL4873869 IC50 = 880.0 nM 6.06
CHEMBL4869087 IC50 = 920.0 nM 6.04
CHEMBL4872706 IC50 = 990.0 nM 6.00
CHEMBL4861409 IC50 = 1450.0 nM 5.84
CHEMBL4871841 IC50 = 2230.0 nM 5.65
CHEMBL4853995 IC50 = 3060.0 nM 5.51
CHEMBL4873489 IC50 = 59000.0 nM 4.23