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Assay Detail

CHEMBL4680973

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

Functional
Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in human red blood cells assessed as growth inhibition by SYBR Green fluorescence assay
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Plasmodium falciparum (CHEMBL364)
Type ORGANISM
Organism Plasmodium falciparum

Publication

Discovery of a Quinoline-4-carboxamide Derivative with a Novel Mechanism of Action, Multistage Antimalarial Activity, and Potent in Vivo Efficacy.
Baragaña B,Norcross NR,Wilson C,Porzelle A,Hallyburton I,Grimaldi R,Osuna-Cabello M,Norval S,Riley J,Stojanovski L,Simeons FR,Wyatt PG,Delves MJ,Meister S,Duffy S,Avery VM,Winzeler EA,Sinden RE,Wittlin S,Frearson JA,Gray DW,Fairlamb AH,Waterson D,Campbell SF,Willis P,Read KD,Gilbert IH
J Med Chem (2016) 59 : 9672 -9685
PubMed 27631715 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 42 6.76 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4781034 1 9.22
CHEMBL4743214 1 9.22
CHEMBL4091762 CABAMIQUINE 2.0 1 9.00
CHEMBL4748314 1 8.70
CHEMBL4755125 1 8.70
CHEMBL4799086 1 8.70
CHEMBL4776095 1 8.52
CHEMBL4765126 1 8.40
CHEMBL4783407 1 8.40
CHEMBL4781713 1 8.40
CHEMBL4764214 1 8.22
CHEMBL4787015 1 8.15
CHEMBL4754403 1 7.92
CHEMBL4756468 1 7.16
CHEMBL4792468 1 7.06
CHEMBL3637888 1 6.92
CHEMBL4763266 1 6.85
CHEMBL4798637 1 6.82
CHEMBL4780190 1 6.72
CHEMBL4789144 1 6.54
CHEMBL4784227 1 6.50
CHEMBL4745218 1 6.46
CHEMBL4760148 1 6.36
CHEMBL4745414 1 6.22
CHEMBL4750855 1 6.17
CHEMBL4747859 1 6.16
CHEMBL4749067 1 6.09
CHEMBL4749190 1 6.05
CHEMBL4757727 1 6.00
CHEMBL4740773 1 5.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4781034 EC50 = 0.6 nM 9.22
CHEMBL4743214 EC50 = 0.6 nM 9.22
CHEMBL4091762 CABAMIQUINE EC50 = 1.0 nM 9.00
CHEMBL4748314 EC50 = 2.0 nM 8.70
CHEMBL4755125 EC50 = 2.0 nM 8.70
CHEMBL4799086 EC50 = 2.0 nM 8.70
CHEMBL4776095 EC50 = 3.0 nM 8.52
CHEMBL4765126 EC50 = 4.0 nM 8.40
CHEMBL4783407 EC50 = 4.0 nM 8.40
CHEMBL4781713 EC50 = 4.0 nM 8.40
CHEMBL4764214 EC50 = 6.0 nM 8.22
CHEMBL4787015 EC50 = 7.0 nM 8.15
CHEMBL4754403 EC50 = 12.0 nM 7.92
CHEMBL4756468 EC50 = 70.0 nM 7.16
CHEMBL4792468 EC50 = 87.0 nM 7.06
CHEMBL3637888 EC50 = 120.0 nM 6.92
CHEMBL4763266 EC50 = 140.0 nM 6.85
CHEMBL4798637 EC50 = 150.0 nM 6.82
CHEMBL4780190 EC50 = 190.0 nM 6.72
CHEMBL4789144 EC50 = 290.0 nM 6.54
CHEMBL4784227 EC50 = 320.0 nM 6.50
CHEMBL4745218 EC50 = 350.0 nM 6.46
CHEMBL4760148 EC50 = 440.0 nM 6.36
CHEMBL4745414 EC50 = 600.0 nM 6.22
CHEMBL4750855 EC50 = 680.0 nM 6.17
CHEMBL4747859 EC50 = 700.0 nM 6.16
CHEMBL4749067 EC50 = 810.0 nM 6.09
CHEMBL4749190 EC50 = 900.0 nM 6.05
CHEMBL4757727 EC50 = 990.0 nM 6.00
CHEMBL4740773 EC50 = 1200.0 nM 5.92
CHEMBL4749365 EC50 = 2500.0 nM 5.60
CHEMBL4742384 EC50 = 3300.0 nM 5.48
CHEMBL4785303 EC50 = 3600.0 nM 5.44
CHEMBL4756596 EC50 = 5800.0 nM 5.24
CHEMBL4800400 EC50 = 6700.0 nM 5.17
CHEMBL4755190 EC50 = 8900.0 nM 5.05
CHEMBL4785091 EC50 = 11000.0 nM 4.96
CHEMBL4742956 EC50 = 15000.0 nM 4.82
CHEMBL4744834 EC50 = 18000.0 nM 4.75
CHEMBL4789980 EC50 = 34000.0 nM 4.47
CHEMBL4742857 EC50 = 36000.0 nM 4.44
CHEMBL4743613 EC50 > 50000.0 nM -