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Assay Detail

CHEMBL1248673

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Functional
Antimalarial activity against Plasmodium falciparum Dd2 containing attB site inserted in parasite genome and using CAM promoter driven expressing ATP4 D1247Y mutant after 72 hrs by SYBR green based fluorescence assay
4
Total Activities
4
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

Spiroindolones, a potent compound class for the treatment of malaria.
Rottmann M, McNamara C, Yeung BK, Lee MC, Zou B, Russell B, Seitz P, Plouffe DM, Dharia NV, Tan J, Cohen SB, Spencer KR, González-Páez GE, Lakshminarayana SB, Goh A, Suwanarusk R, Jegla T, Schmitt EK, Beck HP, Brun R, Nosten F, Renia L, Dartois V, Keller TH, Fidock DA, Winzeler EA, Diagana TT.
Science (2010) 329 : 1175 -1180
PubMed 20813948 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.81 8.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1082723 CIPARGAMIN 2.0 1 8.41
CHEMBL416956 MEFLOQUINE 4.0 1 7.96
CHEMBL269671 ARTEMISININ 3.0 1 7.79
CHEMBL1083769 1 7.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1082723 CIPARGAMIN IC50 = 3.9 nM 8.41
CHEMBL416956 MEFLOQUINE IC50 = 11.04 nM 7.96
CHEMBL269671 ARTEMISININ IC50 = 16.25 nM 7.79
CHEMBL1083769 IC50 = 81.02 nM 7.09