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Assay Detail

CHEMBL1037602

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

Functional
Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 assessed as inhibition of parasite growth after 48 hrs by [3H]hypoxanthine reuptake assay
23
Total Activities
23
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

A new series of amodiaquine analogues modified in the basic side chain with in vitro antileishmanial and antiplasmodial activity.
Guglielmo S, Bertinaria M, Rolando B, Crosetti M, Fruttero R, Yardley V, Croft SL, Gasco A.
Eur J Med Chem (2009) 44 : 5071 -5079
PubMed 19811859 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 7.19 9.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL575286 1 9.38
CHEMBL576926 1 8.85
CHEMBL577389 1 8.81
CHEMBL576964 1 8.74
CHEMBL572593 1 8.67
CHEMBL361497 ARTESUNATE 4.0 1 8.61
CHEMBL575523 1 8.26
CHEMBL573295 1 8.19
CHEMBL573984 1 8.15
CHEMBL1630 1 8.06
CHEMBL572461 1 8.00
CHEMBL572595 1 7.98
CHEMBL584808 1 6.65
CHEMBL575071 1 6.62
CHEMBL572594 1 6.54
CHEMBL575525 1 6.41
CHEMBL575910 1 6.25
CHEMBL575909 1 5.85
CHEMBL573296 1 5.83
CHEMBL573754 1 4.92
CHEMBL573506 1 4.85
CHEMBL573053 1 4.85
CHEMBL575728 1 4.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL575286 IC50 = 0.42 nM 9.38
CHEMBL576926 IC50 = 1.4 nM 8.85
CHEMBL577389 IC50 = 1.54 nM 8.81
CHEMBL576964 IC50 = 1.8 nM 8.74
CHEMBL572593 IC50 = 2.12 nM 8.67
CHEMBL361497 ARTESUNATE IC50 = 2.46 nM 8.61
CHEMBL575523 IC50 = 5.47 nM 8.26
CHEMBL573295 IC50 = 6.5 nM 8.19
CHEMBL573984 IC50 = 7.04 nM 8.15
CHEMBL1630 IC50 = 8.61 nM 8.06
CHEMBL572461 IC50 = 10.1 nM 8.00
CHEMBL572595 IC50 = 10.4 nM 7.98
CHEMBL584808 IC50 = 225.0 nM 6.65
CHEMBL575071 IC50 = 238.0 nM 6.62
CHEMBL572594 IC50 = 290.0 nM 6.54
CHEMBL575525 IC50 = 387.0 nM 6.41
CHEMBL575910 IC50 = 557.0 nM 6.25
CHEMBL575909 IC50 = 1420.0 nM 5.85
CHEMBL573296 IC50 = 1480.0 nM 5.83
CHEMBL573754 IC50 = 12100.0 nM 4.92
CHEMBL573506 IC50 = 14100.0 nM 4.85
CHEMBL573053 IC50 = 14100.0 nM 4.85
CHEMBL575728 IC50 = 14300.0 nM 4.84