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Assay Detail

CHEMBL3225044

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

Functional
Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 infected in human erythrocytes assessed as [3H]hypoxanthine incorporation after 48 hrs by betaplate liquid scintillation counting analysis
20
Total Activities
20
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

Second generation analogues of RKA182: synthetic tetraoxanes with outstanding in vitro and in vivo antimalarial activities
Marti F, Chadwick J, Amewu RK, Burrell-Saward H, Srivastava A, Ward SA, Sharma R, Berry N, O'Neill PM
Medchemcomm (2011) 2 : 661 -665
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 8.91 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3218240 1 9.70
CHEMBL3218241 1 9.70
CHEMBL3218235 1 9.40
CHEMBL3218232 1 9.40
CHEMBL3218238 1 9.40
CHEMBL3218234 1 9.05
CHEMBL3218233 1 9.00
CHEMBL3218236 1 8.96
CHEMBL2387268 1 8.95
CHEMBL3218242 1 8.92
CHEMBL3218239 1 8.89
CHEMBL3218237 1 8.60
CHEMBL361497 ARTESUNATE 4.0 1 8.31
CHEMBL76 CHLOROQUINE 4.0 1 6.49
CHEMBL3218243 1 -
CHEMBL3218244 1 -
CHEMBL3218245 1 -
CHEMBL3218246 1 -
CHEMBL3218247 1 -
CHEMBL3218248 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3218240 IC50 = 0.2 nM 9.70
CHEMBL3218241 IC50 = 0.2 nM 9.70
CHEMBL3218235 IC50 = 0.4 nM 9.40
CHEMBL3218232 IC50 = 0.4 nM 9.40
CHEMBL3218238 IC50 = 0.4 nM 9.40
CHEMBL3218234 IC50 = 0.9 nM 9.05
CHEMBL3218233 IC50 = 1.0 nM 9.00
CHEMBL3218236 IC50 = 1.1 nM 8.96
CHEMBL2387268 IC50 = 1.119 nM 8.95
CHEMBL3218242 IC50 = 1.2 nM 8.92
CHEMBL3218239 IC50 = 1.3 nM 8.89
CHEMBL3218237 IC50 = 2.5 nM 8.60
CHEMBL361497 ARTESUNATE IC50 = 4.9 nM 8.31
CHEMBL76 CHLOROQUINE IC50 = 325.0 nM 6.49
CHEMBL3218243 IC50 - -
CHEMBL3218244 IC50 - -
CHEMBL3218245 IC50 - -
CHEMBL3218246 IC50 - -
CHEMBL3218247 IC50 - -
CHEMBL3218248 IC50 - -