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Assay Detail

CHEMBL2025605

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

Functional
Antiplasmodial activity chloroquine-sensitive Plasmodium falciparum 3D7 infected in human A+ erythrocytes assessed as inhibition of [3H]-hypoxanthine incorporation after 24 hrs by scintillation counting
21
Total Activities
21
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

2-Aminopyrimidine based 4-aminoquinoline anti-plasmodial agents. Synthesis, biological activity, structure-activity relationship and mode of action studies.
Singh K, Kaur H, Chibale K, Balzarini J, Little S, Bharatam PV.
Eur J Med Chem (2012) 52 : 82 -97
PubMed 22459876 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 6.61 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL76 CHLOROQUINE 4.0 1 8.85
CHEMBL361497 ARTESUNATE 4.0 1 8.28
CHEMBL2023610 1 7.74
CHEMBL2023440 1 7.66
CHEMBL2023605 1 7.38
CHEMBL2023604 1 7.20
CHEMBL2023608 1 6.76
CHEMBL2023442 1 6.69
CHEMBL2023441 1 6.61
CHEMBL2023444 1 6.60
CHEMBL2023446 1 6.58
CHEMBL2023450 1 6.54
CHEMBL2023611 1 6.30
CHEMBL2023606 1 6.22
CHEMBL2023448 1 6.19
CHEMBL2023607 1 6.16
CHEMBL2023443 1 5.95
CHEMBL2023445 1 5.75
CHEMBL2023609 1 5.71
CHEMBL2023447 1 4.83
CHEMBL2023449 1 4.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL76 CHLOROQUINE IC50 = 1.4 nM 8.85
CHEMBL361497 ARTESUNATE IC50 = 5.3 nM 8.28
CHEMBL2023610 IC50 = 18.2 nM 7.74
CHEMBL2023440 IC50 = 21.7 nM 7.66
CHEMBL2023605 IC50 = 42.1 nM 7.38
CHEMBL2023604 IC50 = 63.1 nM 7.20
CHEMBL2023608 IC50 = 172.9 nM 6.76
CHEMBL2023442 IC50 = 202.3 nM 6.69
CHEMBL2023441 IC50 = 247.5 nM 6.61
CHEMBL2023444 IC50 = 252.2 nM 6.60
CHEMBL2023446 IC50 = 264.8 nM 6.58
CHEMBL2023450 IC50 = 286.7 nM 6.54
CHEMBL2023611 IC50 = 499.9 nM 6.30
CHEMBL2023606 IC50 = 598.7 nM 6.22
CHEMBL2023448 IC50 = 644.4 nM 6.19
CHEMBL2023607 IC50 = 697.2 nM 6.16
CHEMBL2023443 IC50 = 1134.9 nM 5.95
CHEMBL2023445 IC50 = 1776.8 nM 5.75
CHEMBL2023609 IC50 = 1955.1 nM 5.71
CHEMBL2023447 IC50 = 14828.3 nM 4.83
CHEMBL2023449 IC50 = 15888.5 nM 4.80