Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL1248664

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

Functional
Antimalarial activity against NITD609-resistant Plasmodium falciparum Dd2 Clone2 bearing P-type ATPase4 T418N and P990R mutations after 72 hrs by SYBR green based fluorescence assay
12
Total Activities
12
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 12 7.43 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1450 ATOVAQUONE 4.0 1 9.10
CHEMBL1082723 CIPARGAMIN 2.0 1 8.43
CHEMBL416956 MEFLOQUINE 4.0 1 8.15
CHEMBL1241239 CONCANAMYCIN A 1 8.10
CHEMBL423192 ANISOMYCIN 1 8.04
CHEMBL269671 ARTEMISININ 3.0 1 7.75
CHEMBL1241238 CYCLOMARIN A 1 7.46
CHEMBL1083769 1 6.81
CHEMBL123292 CYCLOHEXIMIDE 2.0 1 6.51
CHEMBL96926 THAPSIGARGIN 1 5.96
CHEMBL480627 CYCLOPIAZONIC ACID 1 5.38
CHEMBL36 PYRIMETHAMINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1450 ATOVAQUONE IC50 = 0.8 nM 9.10
CHEMBL1082723 CIPARGAMIN IC50 = 3.7 nM 8.43
CHEMBL416956 MEFLOQUINE IC50 = 7.0 nM 8.15
CHEMBL1241239 CONCANAMYCIN A IC50 = 8.0 nM 8.10
CHEMBL423192 ANISOMYCIN IC50 = 9.2 nM 8.04
CHEMBL269671 ARTEMISININ IC50 = 18.0 nM 7.75
CHEMBL1241238 CYCLOMARIN A IC50 = 35.0 nM 7.46
CHEMBL1083769 IC50 = 153.9 nM 6.81
CHEMBL123292 CYCLOHEXIMIDE IC50 = 310.0 nM 6.51
CHEMBL96926 THAPSIGARGIN IC50 = 1109.0 nM 5.96
CHEMBL480627 CYCLOPIAZONIC ACID IC50 = 4160.0 nM 5.38
CHEMBL36 PYRIMETHAMINE IC50 > 20000.0 nM -