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Assay Detail

CHEMBL3108258

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

Functional
Antiplasmodial activity against chloroquine/pyrimethamine-resistant Plasmodium falciparum K1 infected in human red blood cells assessed as [3H]-hypoxanthine incorporation incubated for 48 hrs prior to [3H]-hypoxanthine addition measured after 24 hrs by liquid scintillation counting analysis
28
Total Activities
28
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

Antiprotozoal activity of dicationic 3,5-diphenylisoxazoles, their prodrugs and aza-analogues.
Patrick DA, Bakunov SA, Bakunova SM, Wenzler T, Brun R, Tidwell RR.
Bioorg Med Chem (2014) 22 : 559 -576
PubMed 24268543 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 7.97 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3217270 1 9.40
CHEMBL3216850 1 9.40
CHEMBL3217053 1 9.30
CHEMBL3216167 1 8.96
CHEMBL3216615 1 8.77
CHEMBL3217052 1 8.46
CHEMBL3217049 1 8.43
CHEMBL269671 ARTEMISININ 3.0 1 8.40
CHEMBL3215723 1 8.39
CHEMBL3105253 1 8.32
CHEMBL3215961 1 8.30
CHEMBL3217057 1 8.15
CHEMBL3216376 1 8.13
CHEMBL3217055 1 8.02
CHEMBL24057 FURAMIDINE -1.0 1 7.85
CHEMBL3105271 1 7.82
CHEMBL3217056 1 7.78
CHEMBL3215955 1 7.75
CHEMBL3216848 1 7.72
CHEMBL3217269 1 7.66
CHEMBL3217274 1 7.60
CHEMBL55 PENTAMIDINE 4.0 1 7.34
CHEMBL3216614 1 7.24
CHEMBL76 CHLOROQUINE 4.0 1 6.90
CHEMBL3215722 1 6.87
CHEMBL3216170 1 6.85
CHEMBL3215956 1 6.84
CHEMBL3217058 1 6.49

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3217270 IC50 = 0.4 nM 9.40
CHEMBL3216850 IC50 = 0.4 nM 9.40
CHEMBL3217053 IC50 = 0.5 nM 9.30
CHEMBL3216167 IC50 = 1.1 nM 8.96
CHEMBL3216615 IC50 = 1.7 nM 8.77
CHEMBL3217052 IC50 = 3.5 nM 8.46
CHEMBL3217049 IC50 = 3.7 nM 8.43
CHEMBL269671 ARTEMISININ IC50 = 4.0 nM 8.40
CHEMBL3215723 IC50 = 4.1 nM 8.39
CHEMBL3105253 IC50 = 4.8 nM 8.32
CHEMBL3215961 IC50 = 5.0 nM 8.30
CHEMBL3217057 IC50 = 7.0 nM 8.15
CHEMBL3216376 IC50 = 7.4 nM 8.13
CHEMBL3217055 IC50 = 9.6 nM 8.02
CHEMBL24057 FURAMIDINE IC50 = 14.0 nM 7.85
CHEMBL3105271 IC50 = 15.0 nM 7.82
CHEMBL3217056 IC50 = 16.7 nM 7.78
CHEMBL3215955 IC50 = 18.0 nM 7.75
CHEMBL3216848 IC50 = 18.9 nM 7.72
CHEMBL3217269 IC50 = 21.7 nM 7.66
CHEMBL3217274 IC50 = 24.9 nM 7.60
CHEMBL55 PENTAMIDINE IC50 = 46.0 nM 7.34
CHEMBL3216614 IC50 = 58.0 nM 7.24
CHEMBL76 CHLOROQUINE IC50 = 125.0 nM 6.90
CHEMBL3215722 IC50 = 134.0 nM 6.87
CHEMBL3216170 IC50 = 142.0 nM 6.85
CHEMBL3215956 IC50 = 144.0 nM 6.84
CHEMBL3217058 IC50 = 327.0 nM 6.49