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Assay Detail

CHEMBL1788078

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

Functional
Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 synchronized ring stage parasites infected in erythrocytes assessed as reduction in parasitemia after 48 hrs by Giemsa staining
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

Artemisinin-dipeptidyl vinyl sulfone hybrid molecules: design, synthesis and preliminary SAR for antiplasmodial activity and falcipain-2 inhibition.
Capela R, Oliveira R, Gonçalves LM, Domingos A, Gut J, Rosenthal PJ, Lopes F, Moreira R.
Bioorg Med Chem Lett (2009) 19 : 3229 -3232
PubMed 19435664 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 7.98 8.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1782073 1 8.68
CHEMBL1783729 1 8.64
CHEMBL1783730 1 8.40
CHEMBL1783728 1 8.39
CHEMBL1783732 1 8.38
CHEMBL1783731 1 8.32
CHEMBL1208264 ARTELINIC ACID 1 8.25
CHEMBL269671 ARTEMISININ 3.0 1 7.92
CHEMBL76 CHLOROQUINE 4.0 1 7.11
CHEMBL374508 E-64 1 5.71
CHEMBL1783733 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1782073 IC50 = 2.08 nM 8.68
CHEMBL1783729 IC50 = 2.27 nM 8.64
CHEMBL1783730 IC50 = 3.94 nM 8.40
CHEMBL1783728 IC50 = 4.09 nM 8.39
CHEMBL1783732 IC50 = 4.21 nM 8.38
CHEMBL1783731 IC50 = 4.81 nM 8.32
CHEMBL1208264 ARTELINIC ACID IC50 = 5.66 nM 8.25
CHEMBL269671 ARTEMISININ IC50 = 12.0 nM 7.92
CHEMBL76 CHLOROQUINE IC50 = 78.1 nM 7.11
CHEMBL374508 E-64 IC50 = 1955.0 nM 5.71
CHEMBL1783733 IC50 > 10000.0 nM -