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Assay Detail

CHEMBL4481287

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

Functional
Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 infected in human RBC assessed as reduction in parasite growth after 35 to 56 hrs by nucleic acid staining based flow cytometry
5
Total Activities
5
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

3,3'-Disubstituted 5,5'-Bi(1,2,4-triazine) Derivatives with Potent in Vitro and in Vivo Antimalarial Activity.
Xue L, Shi DH, Harjani JR, Huang F, Beveridge JG, Dingjan T, Ban K, Diab S, Duffy S, Lucantoni L, Fletcher S, Chiu FCK, Blundell S, Ellis K, Ralph SA, Wirjanata G, Teguh S, Noviyanti R, Chavchich M, Creek D, Price RN, Marfurt J, Charman SA, Cuellar ME, Strasser JM, Dahlin JL, Walters MA, Edstein MD, Avery VM, Baell JB.
J Med Chem (2019) 62 : 2485 -2498
PubMed 30715882 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.68 8.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL361497 ARTESUNATE 4.0 1 8.64
CHEMBL172 (S,R)-MEFLOQUINE 1 8.21
CHEMBL1255726 1 7.33
CHEMBL303933 PIPERAQUINE 3.0 1 7.29
CHEMBL76 CHLOROQUINE 4.0 1 6.95

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL361497 ARTESUNATE IC50 = 2.3 nM 8.64
CHEMBL172 (S,R)-MEFLOQUINE IC50 = 6.1 nM 8.21
CHEMBL1255726 IC50 = 46.5 nM 7.33
CHEMBL303933 PIPERAQUINE IC50 = 50.8 nM 7.29
CHEMBL76 CHLOROQUINE IC50 = 111.2 nM 6.95