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Assay Detail

CHEMBL3607575

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

Functional
Antiplasmodial activity against Plasmodium falciparum W2 infected in human erythrocytes after 48 hrs by [3H]-hypoxanthine incorporation assay
15
Total Activities
15
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

Antimalarial benzoheterocyclic 4-aminoquinolines: Structure-activity relationship, in vivo evaluation, mechanistic and bioactivation studies.
Ongarora DS, Strydom N, Wicht K, Njoroge M, Wiesner L, Egan TJ, Wittlin S, Jurva U, Masimirembwa CM, Chibale K.
Bioorg Med Chem (2015) 23 : 5419 -5432
PubMed 26264839 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 7.15 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL682 AMODIAQUINE 4.0 1 8.30
CHEMBL2058036 1 8.10
CHEMBL2058034 1 7.96
CHEMBL2057721 1 7.92
CHEMBL2057722 1 7.89
CHEMBL2058040 1 7.68
CHEMBL2058033 1 7.40
CHEMBL2058041 1 7.39
CHEMBL76 CHLOROQUINE 4.0 1 7.31
CHEMBL3604374 1 6.72
CHEMBL2058039 1 6.70
CHEMBL2058035 1 6.31
CHEMBL2058037 1 6.30
CHEMBL2057720 1 5.94
CHEMBL2058038 1 5.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL682 AMODIAQUINE IC50 = 5.0 nM 8.30
CHEMBL2058036 IC50 = 8.0 nM 8.10
CHEMBL2058034 IC50 = 11.0 nM 7.96
CHEMBL2057721 IC50 = 12.0 nM 7.92
CHEMBL2057722 IC50 = 13.0 nM 7.89
CHEMBL2058040 IC50 = 21.0 nM 7.68
CHEMBL2058033 IC50 = 40.0 nM 7.40
CHEMBL2058041 IC50 = 41.0 nM 7.39
CHEMBL76 CHLOROQUINE IC50 = 49.0 nM 7.31
CHEMBL3604374 IC50 = 189.0 nM 6.72
CHEMBL2058039 IC50 = 200.0 nM 6.70
CHEMBL2058035 IC50 = 491.0 nM 6.31
CHEMBL2058037 IC50 = 501.0 nM 6.30
CHEMBL2057720 IC50 = 1158.0 nM 5.94
CHEMBL2058038 IC50 = 4580.0 nM 5.34