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Assay Detail

CHEMBL3998652

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

Functional
Antimalarial activity against chloroquine and mefloquine resistant Plasmodium falciparum W2mef infected in human erythrocytes incubated for 72 hrs by LDH assay
11
Total Activities
11
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

Optimization of 2-Anilino 4-Amino Substituted Quinazolines into Potent Antimalarial Agents with Oral in Vivo Activity.
Gilson PR, Tan C, Jarman KE, Lowes KN, Curtis JM, Nguyen W, Di Rago AE, Bullen HE, Prinz B, Duffy S, Baell JB, Hutton CA, Jousset Subroux H, Crabb BS, Avery VM, Cowman AF, Sleebs BE.
J Med Chem (2017) 60 : 1171 -1188
PubMed 28080063 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 11 7.28 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL269671 ARTEMISININ 3.0 1 8.22
CHEMBL361497 ARTESUNATE 4.0 1 8.22
CHEMBL4069899 1 7.31
CHEMBL4075337 1 7.27
CHEMBL4096235 1 7.24
CHEMBL4070931 1 7.21
CHEMBL4103101 1 7.12
CHEMBL4092899 1 7.10
CHEMBL4101637 1 6.91
CHEMBL4065240 1 6.89
CHEMBL76 CHLOROQUINE 4.0 1 6.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL269671 ARTEMISININ EC50 = 6.0 nM 8.22
CHEMBL361497 ARTESUNATE EC50 = 6.0 nM 8.22
CHEMBL4069899 EC50 = 49.0 nM 7.31
CHEMBL4075337 EC50 = 54.0 nM 7.27
CHEMBL4096235 EC50 = 57.0 nM 7.24
CHEMBL4070931 EC50 = 61.0 nM 7.21
CHEMBL4103101 EC50 = 75.0 nM 7.12
CHEMBL4092899 EC50 = 80.0 nM 7.10
CHEMBL4101637 EC50 = 122.0 nM 6.91
CHEMBL4065240 EC50 = 128.0 nM 6.89
CHEMBL76 CHLOROQUINE EC50 = 250.0 nM 6.60