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Assay Detail

CHEMBL3225245

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Functional
Antiplasmodial activity against liver stage of Plasmodium berghei sporozoites expressing firefly luciferase infected in human Huh7 cells assessed as inhibition of parasite development treated 1 hr prior to infection followed by compound replenisment at 24 hrs post-infection measured 48 hrs after infection by bioluminescence analysis
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Plasmodium berghei
Tissue Liver
Cell Type Huh-7
Confidence 1 — Organism
Curated By Autocuration

Target

Plasmodium berghei (CHEMBL612653)
Type ORGANISM
Organism Plasmodium berghei

Publication

PRIMACINS, N-cinnamoyl-primaquine conjugates, with improved liver-stage antimalarial activity
Perez B, Teixeira C, Albuquerque IS, Gut J, Rosenthal PJ, Prudencio M, Gomes P
Medchemcomm (2012) 3 : 1170 -1172
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.65 5.86

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3220026 1 5.86
CHEMBL3220022 1 5.81
CHEMBL3220023 1 5.79
CHEMBL3220020 1 5.70
CHEMBL3220021 1 5.67
CHEMBL3220028 1 5.67
CHEMBL3220029 1 5.65
CHEMBL2316805 1 5.63
CHEMBL3220024 1 5.63
CHEMBL3220027 1 5.63
CHEMBL3220025 1 5.62
CHEMBL506 PRIMAQUINE 4.0 1 5.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3220026 IC50 = 1380.0 nM 5.86
CHEMBL3220022 IC50 = 1540.0 nM 5.81
CHEMBL3220023 IC50 = 1630.0 nM 5.79
CHEMBL3220020 IC50 = 2010.0 nM 5.70
CHEMBL3220021 IC50 = 2130.0 nM 5.67
CHEMBL3220028 IC50 = 2120.0 nM 5.67
CHEMBL3220029 IC50 = 2240.0 nM 5.65
CHEMBL2316805 IC50 = 2350.0 nM 5.63
CHEMBL3220024 IC50 = 2330.0 nM 5.63
CHEMBL3220027 IC50 = 2360.0 nM 5.63
CHEMBL3220025 IC50 = 2390.0 nM 5.62
CHEMBL506 PRIMAQUINE IC50 = 7500.0 nM 5.12