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Assay Detail

CHEMBL758316

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Functional
In vitro antimalarial activity against chloroquine-resistant Plasmodium falciparum K1
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Plasmodium falciparum
Confidence 1 — Organism
Curated By Intermediate

Target

Plasmodium falciparum (CHEMBL364)
Type ORGANISM
Organism Plasmodium falciparum

Publication

Isoquine and related amodiaquine analogues: a new generation of improved 4-aminoquinoline antimalarials.
O'Neill PM, Mukhtar A, Stocks PA, Randle LE, Hindley S, Ward SA, Storr RC, Bickley JF, O'Neil IA, Maggs JL, Hughes RH, Winstanley PA, Bray PG, Park BK.
J Med Chem (2003) 46 : 4933 -4945
PubMed 14584944 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 7.54 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL147860 1 8.22
CHEMBL1630 1 7.82
CHEMBL147587 ISOQUINE 1 7.75
CHEMBL147876 1 7.73
CHEMBL147616 1 7.69
CHEMBL342575 1 7.66
CHEMBL147541 1 7.58
CHEMBL433926 1 7.51
CHEMBL147806 GSK-369796 1.0 1 7.49
CHEMBL146826 DESETHYL ISOQUINE 1 7.49
CHEMBL148326 1 7.43
CHEMBL148170 1 6.95
CHEMBL76 CHLOROQUINE 4.0 1 6.74

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL147860 IC50 = 6.01 nM 8.22
CHEMBL1630 IC50 = 15.08 nM 7.82
CHEMBL147587 ISOQUINE IC50 = 17.63 nM 7.75
CHEMBL147876 IC50 = 18.65 nM 7.73
CHEMBL147616 IC50 = 20.28 nM 7.69
CHEMBL342575 IC50 = 21.75 nM 7.66
CHEMBL147541 IC50 = 26.22 nM 7.58
CHEMBL433926 IC50 = 30.63 nM 7.51
CHEMBL147806 GSK-369796 IC50 = 32.75 nM 7.49
CHEMBL146826 DESETHYL ISOQUINE IC50 = 32.42 nM 7.49
CHEMBL148326 IC50 = 37.21 nM 7.43
CHEMBL148170 IC50 = 112.37 nM 6.95
CHEMBL76 CHLOROQUINE IC50 = 183.82 nM 6.74