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Assay Detail

CHEMBL3761500

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

Functional
Antimalarial activity against chloroquine-susceptible Plasmodium falciparum D6 after 48 hrs by [3H]hypoxanthine incorporation assay
24
Total Activities
24
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

Reinvestigating Old Pharmacophores: Are 4-Aminoquinolines and Tetraoxanes Potential Two-Stage Antimalarials?
Terzić N, Konstantinović J, Tot M, Burojević J, Djurković-Djaković O, Srbljanović J, Štajner T, Verbić T, Zlatović M, Machado M, Albuquerque IS, Prudêncio M, Sciotti RJ, Pecic S, D'Alessandro S, Taramelli D, Šolaja BA.
J Med Chem (2016) 59 : 264 -281
PubMed 26640981 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 7.80 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3758628 1 9.00
CHEMBL3759763 1 9.00
CHEMBL3758195 1 8.70
CHEMBL3758274 1 8.40
CHEMBL3759721 1 8.22
CHEMBL3758907 1 8.15
CHEMBL3758254 1 8.15
CHEMBL3758943 1 8.15
CHEMBL269671 ARTEMISININ 3.0 1 8.05
CHEMBL3758754 1 8.05
CHEMBL3758349 1 8.00
CHEMBL3759173 1 7.92
CHEMBL76 CHLOROQUINE 4.0 1 7.92
CHEMBL3759800 1 7.89
CHEMBL172 (S,R)-MEFLOQUINE 1 7.80
CHEMBL3760015 1 7.77
CHEMBL3758372 1 7.68
CHEMBL3759599 1 7.29
CHEMBL3759887 1 7.22
CHEMBL3758840 1 6.87
CHEMBL3759536 1 6.84
CHEMBL3759740 1 6.81
CHEMBL3759566 1 6.70
CHEMBL3759710 1 6.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3758628 IC50 = 1.0 nM 9.00
CHEMBL3759763 IC50 = 1.0 nM 9.00
CHEMBL3758195 IC50 = 2.0 nM 8.70
CHEMBL3758274 IC50 = 4.0 nM 8.40
CHEMBL3759721 IC50 = 6.0 nM 8.22
CHEMBL3758907 IC50 = 7.0 nM 8.15
CHEMBL3758254 IC50 = 7.0 nM 8.15
CHEMBL3758943 IC50 = 7.0 nM 8.15
CHEMBL269671 ARTEMISININ IC50 = 9.0 nM 8.05
CHEMBL3758754 IC50 = 9.0 nM 8.05
CHEMBL3758349 IC50 = 10.0 nM 8.00
CHEMBL3759173 IC50 = 12.0 nM 7.92
CHEMBL76 CHLOROQUINE IC50 = 12.0 nM 7.92
CHEMBL3759800 IC50 = 13.0 nM 7.89
CHEMBL172 (S,R)-MEFLOQUINE IC50 = 16.0 nM 7.80
CHEMBL3760015 IC50 = 17.0 nM 7.77
CHEMBL3758372 IC50 = 21.0 nM 7.68
CHEMBL3759599 IC50 = 51.0 nM 7.29
CHEMBL3759887 IC50 = 60.0 nM 7.22
CHEMBL3758840 IC50 = 135.0 nM 6.87
CHEMBL3759536 IC50 = 143.0 nM 6.84
CHEMBL3759740 IC50 = 154.0 nM 6.81
CHEMBL3759566 IC50 = 198.0 nM 6.70
CHEMBL3759710 IC50 = 288.0 nM 6.54