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Assay Detail

CHEMBL5155604

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

Functional
Antiplasmodial activity CQ-resistant Plasmodium falciparum W2 infected in human erythrocytes assessed as inhibition of parasite growth measured after 72 hrs by HRP2-ELISA
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Plasmodium falciparum
Cell Type Erythrocyte
Confidence 1 — Organism
Curated By Autocuration

Target

Plasmodium falciparum (CHEMBL364)
Type ORGANISM
Organism Plasmodium falciparum

Publication

Design, synthesis, and characterization of novel aminoalcohol quinolines with strong in vitro antimalarial activity.
Dassonville-Klimpt A, Schneider J, Damiani C, Tisnerat C, Cohen A, Azas N, Marchivie M, Guillon J, Mullié C, Agnamey P, Totet A, Dormoi J, Taudon N, Pradines B, Sonnet P.
Eur J Med Chem (2022) 228 : 113981 -113981
PubMed 34782182 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 7.39 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL307261 ARTENIMOL 3.0 1 8.52
CHEMBL5183354 1 7.96
CHEMBL5172366 1 7.85
CHEMBL5174893 1 7.82
CHEMBL5200928 1 7.81
CHEMBL5178359 1 7.80
CHEMBL5207890 1 7.74
CHEMBL5173490 1 7.68
CHEMBL172 (S,R)-MEFLOQUINE 1 7.55
CHEMBL5183115 1 7.41
CHEMBL5207162 1 7.40
CHEMBL5184272 1 7.21
CHEMBL5175462 1 7.20
CHEMBL5180511 1 7.08
CHEMBL5193684 1 7.05
CHEMBL1235 DESETHYL AMODIAQUINE 1 7.00
CHEMBL5208723 1 6.64
CHEMBL76 CHLOROQUINE 4.0 1 6.33
CHEMBL170 QUININE 4.0 1 6.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL307261 ARTENIMOL IC50 = 3.0 nM 8.52
CHEMBL5183354 IC50 = 11.0 nM 7.96
CHEMBL5172366 IC50 = 14.1 nM 7.85
CHEMBL5174893 IC50 = 15.3 nM 7.82
CHEMBL5200928 IC50 = 15.4 nM 7.81
CHEMBL5178359 IC50 = 15.8 nM 7.80
CHEMBL5207890 IC50 = 18.2 nM 7.74
CHEMBL5173490 IC50 = 20.7 nM 7.68
CHEMBL172 (S,R)-MEFLOQUINE IC50 = 28.3 nM 7.55
CHEMBL5183115 IC50 = 39.4 nM 7.41
CHEMBL5207162 IC50 = 39.9 nM 7.40
CHEMBL5184272 IC50 = 61.9 nM 7.21
CHEMBL5175462 IC50 = 63.8 nM 7.20
CHEMBL5180511 IC50 = 82.7 nM 7.08
CHEMBL5193684 IC50 = 89.3 nM 7.05
CHEMBL1235 DESETHYL AMODIAQUINE IC50 = 100.0 nM 7.00
CHEMBL5208723 IC50 = 229.0 nM 6.64
CHEMBL76 CHLOROQUINE IC50 = 469.2 nM 6.33
CHEMBL170 QUININE IC50 = 473.9 nM 6.32