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Assay Detail

CHEMBL2039532

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

Functional
Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 infected in O-positive human RBC assessed as [3H]-hypoxanthine incorporation after 48 hrs by scintillation counting in presence of BSA
11
Total Activities
11
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

Sphingolipid analogues inhibit development of malaria parasites.
Meyer EV, Holt JJ, Girard KR, Ballie MT, Bushnev AS, Lapp S, Menaldino DS, Arrendale RF, Reddy GP, Evers TJ, Howard RB, Culver DG, Liotta DC, Galinski MR, Natchus MG.
ACS Med Chem Lett (2012) 3 : 43 -47
PubMed 24900369 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.94 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL172 (S,R)-MEFLOQUINE 1 9.40
CHEMBL76 CHLOROQUINE 4.0 1 7.03
CHEMBL2036000 1 6.60
CHEMBL1951765 1 6.05
CHEMBL2036001 1 5.58
CHEMBL2035998 1 5.33
CHEMBL2035989 1 5.14
CHEMBL2035999 1 5.13
CHEMBL1951761 ENIGMOL 1 5.04
CHEMBL2035997 1 5.00
CHEMBL2036002 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL172 (S,R)-MEFLOQUINE IC50 = 0.4 nM 9.40
CHEMBL76 CHLOROQUINE IC50 = 93.0 nM 7.03
CHEMBL2036000 IC50 = 250.0 nM 6.60
CHEMBL1951765 IC50 = 900.0 nM 6.05
CHEMBL2036001 IC50 = 2600.0 nM 5.58
CHEMBL2035998 IC50 = 4700.0 nM 5.33
CHEMBL2035989 IC50 = 7200.0 nM 5.14
CHEMBL2035999 IC50 = 7400.0 nM 5.13
CHEMBL1951761 ENIGMOL IC50 = 9200.0 nM 5.04
CHEMBL2035997 IC50 = 9900.0 nM 5.00
CHEMBL2036002 IC50 = 10000.0 nM 5.00