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Assay Detail

CHEMBL958385

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

Functional
Antimalarial activity against chloroquine-sensitive Plasmodium falciparum HB3
14
Total Activities
14
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

Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine.
O'Neill PM, Shone AE, Stanford D, Nixon G, Asadollahy E, Park BK, Maggs JL, Roberts P, Stocks PA, Biagini G, Bray PG, Davies J, Berry N, Hall C, Rimmer K, Winstanley PA, Hindley S, Bambal RB, Davis CB, Bates M, Gresham SL, Brigandi RA, Gomez-de-Las-Heras FM, Gargallo DV, Parapini S, Vivas L, Lander H, Taramelli D, Ward SA.
J Med Chem (2009) 52 : 1828 -1844
PubMed 19284751 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 7.66 8.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1630 1 8.26
CHEMBL523342 1 8.09
CHEMBL475811 1 8.04
CHEMBL492914 1 8.02
CHEMBL446386 1 8.00
CHEMBL492326 1 7.91
CHEMBL492722 1 7.91
CHEMBL453384 1 7.84
CHEMBL523677 1 7.82
CHEMBL76 CHLOROQUINE 4.0 1 7.70
CHEMBL492307 1 7.26
CHEMBL502137 1 7.20
CHEMBL492913 1 6.84
CHEMBL475810 1 6.31

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1630 IC50 = 5.5 nM 8.26
CHEMBL523342 IC50 = 8.1 nM 8.09
CHEMBL475811 IC50 = 9.1 nM 8.04
CHEMBL492914 IC50 = 9.6 nM 8.02
CHEMBL446386 IC50 = 10.1 nM 8.00
CHEMBL492326 IC50 = 12.3 nM 7.91
CHEMBL492722 IC50 = 12.3 nM 7.91
CHEMBL453384 IC50 = 14.6 nM 7.84
CHEMBL523677 IC50 = 15.2 nM 7.82
CHEMBL76 CHLOROQUINE IC50 = 20.2 nM 7.70
CHEMBL492307 IC50 = 54.5 nM 7.26
CHEMBL502137 IC50 = 63.7 nM 7.20
CHEMBL492913 IC50 = 144.3 nM 6.84
CHEMBL475810 IC50 = 485.0 nM 6.31