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Assay Detail

CHEMBL945976

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

Functional
Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2
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 Intermediate

Target

Plasmodium falciparum (CHEMBL364)
Type ORGANISM
Organism Plasmodium falciparum

Publication

Cryptolepine analogues containing basic aminoalkyl side-chains at C-11: synthesis, antiplasmodial activity, and cytotoxicity.
Lavrado J, Paulo A, Gut J, Rosenthal PJ, Moreira R.
Bioorg Med Chem Lett (2008) 18 : 1378 -1381
PubMed 18207399 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.09 7.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL253716 1 7.66
CHEMBL253508 1 7.52
CHEMBL253715 1 7.50
CHEMBL404523 1 7.44
CHEMBL404321 1 7.36
CHEMBL439424 1 7.30
CHEMBL252504 1 7.09
CHEMBL253717 1 6.90
CHEMBL267856 1 6.88
CHEMBL404522 1 6.74
CHEMBL76 CHLOROQUINE 4.0 1 6.60
CHEMBL92129 CRYPTOLEPINE HYDROCHLORIDE 1 6.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL253716 IC50 = 22.0 nM 7.66
CHEMBL253508 IC50 = 30.0 nM 7.52
CHEMBL253715 IC50 = 32.0 nM 7.50
CHEMBL404523 IC50 = 36.0 nM 7.44
CHEMBL404321 IC50 = 44.0 nM 7.36
CHEMBL439424 IC50 = 50.0 nM 7.30
CHEMBL252504 IC50 = 82.0 nM 7.09
CHEMBL253717 IC50 = 127.0 nM 6.90
CHEMBL267856 IC50 = 132.0 nM 6.88
CHEMBL404522 IC50 = 184.0 nM 6.74
CHEMBL76 CHLOROQUINE IC50 = 249.0 nM 6.60
CHEMBL92129 CRYPTOLEPINE HYDROCHLORIDE IC50 = 755.0 nM 6.12