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Assay Detail

CHEMBL2329982

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

Functional
Antimalarial activity against wild type early trophozoite stage of Plasmodium falciparum D6 in human red blood cells assessed as [3H]hypoxanthine uptake after 96 hrs
9
Total Activities
9
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

Acyclic nucleoside phosphonates containing a second phosphonate group are potent inhibitors of 6-oxopurine phosphoribosyltransferases and have antimalarial activity.
Keough DT, Špaček P, Hocková D, Tichý T, Vrbková S, Slavětínská L, Janeba Z, Naesens L, Edstein MD, Chavchich M, Wang TH, de Jersey J, Guddat LW.
J Med Chem (2013) 56 : 2513 -2526
PubMed 23448281 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.30 7.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL76 CHLOROQUINE 4.0 1 7.77
CHEMBL2325750 1 5.42
CHEMBL2325751 1 5.18
CHEMBL2063188 1 5.12
CHEMBL2325749 1 5.01
CHEMBL2325756 1 4.38
CHEMBL2063186 1 4.23
CHEMBL1229838 1 -
CHEMBL2325752 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL76 CHLOROQUINE IC50 = 17.0 nM 7.77
CHEMBL2325750 IC50 = 3800.0 nM 5.42
CHEMBL2325751 IC50 = 6600.0 nM 5.18
CHEMBL2063188 IC50 = 7600.0 nM 5.12
CHEMBL2325749 IC50 = 9700.0 nM 5.01
CHEMBL2325756 IC50 = 42000.0 nM 4.38
CHEMBL2063186 IC50 = 59000.0 nM 4.23
CHEMBL1229838 IC50 = 242000.0 nM -
CHEMBL2325752 IC50 - -