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Assay Detail

CHEMBL3102586

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Functional
Antiplasmodial activity against chloroquine-resistant ring stage Plasmodium falciparum W2 assessed as parasitemia after 48 hrs by flow cytometry
25
Total Activities
25
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

Urea/oxalamide tethered β-lactam-7-chloroquinoline conjugates: synthesis and in vitro antimalarial evaluation.
Singh P, Raj R, Singh P, Gut J, Rosenthal PJ, Kumar V.
Eur J Med Chem (2014) 71 : 128 -134
PubMed 24287561 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 7.18 7.97

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL269671 ARTEMISININ 3.0 1 7.97
CHEMBL170 QUININE 4.0 1 7.73
CHEMBL3098963 1 7.46
CHEMBL3098959 1 7.37
CHEMBL3098964 1 7.35
CHEMBL3098967 1 7.29
CHEMBL3098957 1 7.29
CHEMBL3098955 1 7.28
CHEMBL3098956 1 7.28
CHEMBL76 CHLOROQUINE 4.0 1 7.23
CHEMBL3098960 1 7.21
CHEMBL3098962 1 7.16
CHEMBL3098953 1 7.14
CHEMBL3098966 1 7.08
CHEMBL3098965 1 7.05
CHEMBL3098961 1 6.92
CHEMBL3098958 1 6.83
CHEMBL3098952 1 6.80
CHEMBL3098954 1 6.71
CHEMBL1235 DESETHYL AMODIAQUINE 1 6.40
CHEMBL3098951 1 -
CHEMBL3098950 1 -
CHEMBL3098949 1 -
CHEMBL3098948 1 -
CHEMBL3098947 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL269671 ARTEMISININ IC50 = 10.63 nM 7.97
CHEMBL170 QUININE IC50 = 18.67 nM 7.73
CHEMBL3098963 IC50 = 34.97 nM 7.46
CHEMBL3098959 IC50 = 42.38 nM 7.37
CHEMBL3098964 IC50 = 44.78 nM 7.35
CHEMBL3098967 IC50 = 50.82 nM 7.29
CHEMBL3098957 IC50 = 51.02 nM 7.29
CHEMBL3098955 IC50 = 52.09 nM 7.28
CHEMBL3098956 IC50 = 53.11 nM 7.28
CHEMBL76 CHLOROQUINE IC50 = 59.09 nM 7.23
CHEMBL3098960 IC50 = 61.34 nM 7.21
CHEMBL3098962 IC50 = 68.63 nM 7.16
CHEMBL3098953 IC50 = 73.03 nM 7.14
CHEMBL3098966 IC50 = 82.19 nM 7.08
CHEMBL3098965 IC50 = 88.7 nM 7.05
CHEMBL3098961 IC50 = 120.65 nM 6.92
CHEMBL3098958 IC50 = 149.45 nM 6.83
CHEMBL3098952 IC50 = 157.25 nM 6.80
CHEMBL3098954 IC50 = 193.15 nM 6.71
CHEMBL1235 DESETHYL AMODIAQUINE IC50 = 400.7 nM 6.40
CHEMBL3098951 IC50 > 1000.0 nM -
CHEMBL3098950 IC50 > 1000.0 nM -
CHEMBL3098949 IC50 > 1000.0 nM -
CHEMBL3098948 IC50 > 1000.0 nM -
CHEMBL3098947 IC50 > 1000.0 nM -