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Assay Detail

CHEMBL1930671

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

Functional
Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2mef infected in human erythrocytes assessed as inhibition of [3H]hypoxanthine incorporation after 48 hrs by beta liquid scintillation counting method
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

Synthesis and antimalarial evaluation of novel isocryptolepine derivatives.
Whittell LR, Batty KT, Wong RP, Bolitho EM, Fox SA, Davis TM, Murray PE.
Bioorg Med Chem (2011) 19 : 7519 -7525
PubMed 22055713 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.72 7.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL38827 LUMEFANTRINE 4.0 1 7.25
CHEMBL1927688 1 7.07
CHEMBL1927690 1 7.00
CHEMBL1927689 1 6.95
CHEMBL1927691 1 6.88
CHEMBL76 CHLOROQUINE 4.0 1 6.84
CHEMBL1927687 1 6.74
CHEMBL1927692 1 6.66
CHEMBL1927685 1 6.50
CHEMBL1927686 1 6.12
CHEMBL502768 ISOCRYPTOLEPINE HYDROCHLORIDE 1 5.93

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL38827 LUMEFANTRINE IC50 = 56.0 nM 7.25
CHEMBL1927688 IC50 = 85.0 nM 7.07
CHEMBL1927690 IC50 = 100.0 nM 7.00
CHEMBL1927689 IC50 = 112.0 nM 6.95
CHEMBL1927691 IC50 = 131.0 nM 6.88
CHEMBL76 CHLOROQUINE IC50 = 144.0 nM 6.84
CHEMBL1927687 IC50 = 184.0 nM 6.74
CHEMBL1927692 IC50 = 218.0 nM 6.66
CHEMBL1927685 IC50 = 316.0 nM 6.50
CHEMBL1927686 IC50 = 760.0 nM 6.12
CHEMBL502768 ISOCRYPTOLEPINE HYDROCHLORIDE IC50 = 1177.0 nM 5.93