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Assay Detail

CHEMBL3241687

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Functional
Antimalarial activity against drug-sensitive Plasmodium falciparum NF54
62
Total Activities
62
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

Medicinal chemistry optimization of antiplasmodial imidazopyridazine hits from high throughput screening of a SoftFocus kinase library: part 1.
Le Manach C, Gonzàlez Cabrera D, Douelle F, Nchinda AT, Younis Y, Taylor D, Wiesner L, White KL, Ryan E, March C, Duffy S, Avery VM, Waterson D, Witty MJ, Wittlin S, Charman SA, Street LJ, Chibale K.
J Med Chem (2014) 57 : 2789 -2798
PubMed 24568587 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 62 6.98 9.18

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3234067 1 9.18
CHEMBL3234068 1 8.46
CHEMBL361497 ARTESUNATE 4.0 1 8.40
CHEMBL3234069 1 8.36
CHEMBL3234070 1 8.21
CHEMBL3234072 1 8.19
CHEMBL3234071 1 8.14
CHEMBL172 (S,R)-MEFLOQUINE 1 7.92
CHEMBL3234073 1 7.85
CHEMBL3234074 1 7.82
CHEMBL76 CHLOROQUINE 4.0 1 7.80
CHEMBL3234041 1 7.80
CHEMBL3234042 1 7.80
CHEMBL3234094 1 7.75
CHEMBL3234075 1 7.72
CHEMBL3234043 1 7.59
CHEMBL3234076 1 7.50
CHEMBL3234044 1 7.34
CHEMBL3234077 1 7.10
CHEMBL3234093 1 7.03
CHEMBL3234045 1 7.02
CHEMBL3234078 1 7.00
CHEMBL3234079 1 6.99
CHEMBL3234080 1 6.97
CHEMBL3234081 1 6.93
CHEMBL3234047 1 6.86
CHEMBL3234046 1 6.84
CHEMBL3234083 1 6.81
CHEMBL3234085 1 6.80
CHEMBL3234084 1 6.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3234067 IC50 = 0.66 nM 9.18
CHEMBL3234068 IC50 = 3.5 nM 8.46
CHEMBL361497 ARTESUNATE IC50 = 4.0 nM 8.40
CHEMBL3234069 IC50 = 4.4 nM 8.36
CHEMBL3234070 IC50 = 6.1 nM 8.21
CHEMBL3234072 IC50 = 6.5 nM 8.19
CHEMBL3234071 IC50 = 7.3 nM 8.14
CHEMBL172 (S,R)-MEFLOQUINE IC50 = 12.0 nM 7.92
CHEMBL3234073 IC50 = 14.0 nM 7.85
CHEMBL3234074 IC50 = 15.0 nM 7.82
CHEMBL76 CHLOROQUINE IC50 = 16.0 nM 7.80
CHEMBL3234041 IC50 = 16.0 nM 7.80
CHEMBL3234042 IC50 = 16.0 nM 7.80
CHEMBL3234094 IC50 = 18.0 nM 7.75
CHEMBL3234075 IC50 = 19.0 nM 7.72
CHEMBL3234043 IC50 = 25.9 nM 7.59
CHEMBL3234076 IC50 = 32.0 nM 7.50
CHEMBL3234044 IC50 = 46.0 nM 7.34
CHEMBL3234077 IC50 = 79.0 nM 7.10
CHEMBL3234093 IC50 = 93.0 nM 7.03
CHEMBL3234045 IC50 = 95.0 nM 7.02
CHEMBL3234078 IC50 = 99.0 nM 7.00
CHEMBL3234079 IC50 = 102.0 nM 6.99
CHEMBL3234080 IC50 = 107.0 nM 6.97
CHEMBL3234081 IC50 = 117.0 nM 6.93
CHEMBL3234047 IC50 = 137.0 nM 6.86
CHEMBL3234046 IC50 = 146.0 nM 6.84
CHEMBL3234083 IC50 = 154.0 nM 6.81
CHEMBL3234085 IC50 = 159.0 nM 6.80
CHEMBL3234084 IC50 = 179.0 nM 6.75
CHEMBL3234086 IC50 = 183.0 nM 6.74
CHEMBL3234048 IC50 = 186.0 nM 6.73
CHEMBL3234082 IC50 = 189.0 nM 6.72
CHEMBL3234049 IC50 = 202.0 nM 6.70
CHEMBL3234050 IC50 = 223.0 nM 6.65
CHEMBL3234051 IC50 = 272.0 nM 6.57
CHEMBL3234052 IC50 = 283.0 nM 6.55
CHEMBL3234056 IC50 = 289.0 nM 6.54
CHEMBL3234055 IC50 = 335.0 nM 6.47
CHEMBL3234087 IC50 = 393.0 nM 6.41
CHEMBL3234053 IC50 = 496.0 nM 6.30
CHEMBL3234054 IC50 = 603.0 nM 6.22
CHEMBL3234089 IC50 = 706.0 nM 6.15
CHEMBL3234059 IC50 = 739.0 nM 6.13
CHEMBL3234088 IC50 = 763.0 nM 6.12
CHEMBL3234098 IC50 = 763.0 nM 6.12
CHEMBL3234097 IC50 = 764.0 nM 6.12
CHEMBL3234057 IC50 = 964.0 nM 6.02
CHEMBL3234058 IC50 = 1061.0 nM 5.97
CHEMBL3234091 IC50 = 1273.0 nM 5.89