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Assay Detail

CHEMBL762017

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

Functional
In vitro inhibition of chloroquine-resistant Plasmodium falciparum K1
7
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Plasmodium falciparum
Confidence 1 — Organism
Curated By Intermediate

Target

Plasmodium falciparum (CHEMBL364)
Type ORGANISM
Organism Plasmodium falciparum

Publication

Synthesis, antimalarial activity, and molecular modeling of tebuquine analogues.
O'Neill PM, Willock DJ, Hawley SR, Bray PG, Storr RC, Ward SA, Park BK.
J Med Chem (1997) 40 : 437 -448
PubMed 9046333 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.21 7.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL339049 TEBUQUINE 2.0 2 7.68
CHEMBL1630 1 7.57
CHEMBL138786 1 7.13
CHEMBL337981 FLOUROTEBUQUINE 1 7.13
CHEMBL335121 1 6.99
CHEMBL76 CHLOROQUINE 4.0 1 6.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL339049 TEBUQUINE IC50 = 20.8 nM 7.68
CHEMBL1630 IC50 = 27.2 nM 7.57
CHEMBL339049 TEBUQUINE IC50 = 42.1 nM 7.38
CHEMBL138786 IC50 = 74.2 nM 7.13
CHEMBL337981 FLOUROTEBUQUINE IC50 = 74.3 nM 7.13
CHEMBL335121 IC50 = 101.3 nM 6.99
CHEMBL76 CHLOROQUINE IC50 = 250.0 nM 6.60