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Assay Detail

CHEMBL4340145

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Functional
Antimalarial activity against CQ-resistant Plasmodium falciparum W2 infected in human type A-positive red blood cells assessed as inhibition of parasite growth incubated for for 72 hrs by spectrophotometry based parasite lactate dehydrogenase assay
14
Total Activities
14
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

Covalent Inhibitors of <i>Plasmodium falciparum</i> Glyceraldehyde 3-Phosphate Dehydrogenase with Antimalarial Activity in Vitro.
Cullia G, Bruno S, Parapini S, Margiotta M, Tamborini L, Pinto A, Galbiati A, Mozzarelli A, Persico M, Paladino A, Fattorusso C, Taramelli D, Conti P.
ACS Med Chem Lett (2019) 10 : 590 -595
PubMed 30996801 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.37 6.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4436101 1 6.60
CHEMBL3329248 1 6.58
CHEMBL1971775 1 6.47
CHEMBL76 CHLOROQUINE 4.0 1 6.40
CHEMBL4562798 1 6.32
CHEMBL4467084 1 6.14
CHEMBL3329246 1 6.06
CHEMBL4581512 1 -
CHEMBL4455992 1 -
CHEMBL4589757 1 -
CHEMBL4529769 1 -
CHEMBL4446183 1 -
CHEMBL4459115 1 -
CHEMBL4465533 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4436101 IC50 = 250.0 nM 6.60
CHEMBL3329248 IC50 = 260.0 nM 6.58
CHEMBL1971775 IC50 = 340.0 nM 6.47
CHEMBL76 CHLOROQUINE IC50 = 400.0 nM 6.40
CHEMBL4562798 IC50 = 480.0 nM 6.32
CHEMBL4467084 IC50 = 720.0 nM 6.14
CHEMBL3329246 IC50 = 880.0 nM 6.06
CHEMBL4581512 IC50 - -
CHEMBL4455992 IC50 - -
CHEMBL4589757 IC50 - -
CHEMBL4529769 IC50 - -
CHEMBL4446183 IC50 - -
CHEMBL4459115 IC50 - -
CHEMBL4465533 IC50 - -