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Assay Detail

CHEMBL928090

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Functional
Antimalarial activity against Plasmodium falciparum 3D7
22
Total Activities
22
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

Two-step synthesis of achiral dispiro-1,2,4,5-tetraoxanes with outstanding antimalarial activity, low toxicity, and high-stability profiles.
Ellis GL, Amewu R, Sabbani S, Stocks PA, Shone A, Stanford D, Gibbons P, Davies J, Vivas L, Charnaud S, Bongard E, Hall C, Rimmer K, Lozanom S, Jesús M, Gargallo D, Ward SA, O'Neill PM.
J Med Chem (2008) 51 : 2170 -2177
PubMed 18341274 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 7.84 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL207675 SODIUM ARESUNATE 1 9.22
CHEMBL566534 ARTEMETHER 4.0 1 8.49
CHEMBL405944 1 8.45
CHEMBL259023 1 8.33
CHEMBL406928 1 8.30
CHEMBL410640 1 8.26
CHEMBL261818 1 8.26
CHEMBL261816 1 8.23
CHEMBL269671 ARTEMISININ 3.0 1 8.04
CHEMBL402472 1 7.99
CHEMBL260683 1 7.84
CHEMBL261066 1 7.80
CHEMBL409431 1 7.78
CHEMBL258908 1 7.68
CHEMBL258763 1 7.64
CHEMBL258875 1 7.56
CHEMBL436908 1 7.54
CHEMBL405885 1 7.22
CHEMBL430041 1 7.06
CHEMBL405884 1 6.88
CHEMBL261500 1 6.15
CHEMBL405890 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL207675 SODIUM ARESUNATE IC50 = 0.6 nM 9.22
CHEMBL566534 ARTEMETHER IC50 = 3.2 nM 8.49
CHEMBL405944 IC50 = 3.52 nM 8.45
CHEMBL259023 IC50 = 4.7 nM 8.33
CHEMBL406928 IC50 = 4.98 nM 8.30
CHEMBL410640 IC50 = 5.46 nM 8.26
CHEMBL261818 IC50 = 5.55 nM 8.26
CHEMBL261816 IC50 = 5.87 nM 8.23
CHEMBL269671 ARTEMISININ IC50 = 9.2 nM 8.04
CHEMBL402472 IC50 = 10.18 nM 7.99
CHEMBL260683 IC50 = 14.35 nM 7.84
CHEMBL261066 IC50 = 16.0 nM 7.80
CHEMBL409431 IC50 = 16.73 nM 7.78
CHEMBL258908 IC50 = 20.73 nM 7.68
CHEMBL258763 IC50 = 22.73 nM 7.64
CHEMBL258875 IC50 = 27.75 nM 7.56
CHEMBL436908 IC50 = 29.13 nM 7.54
CHEMBL405885 IC50 = 60.57 nM 7.22
CHEMBL430041 IC50 = 86.37 nM 7.06
CHEMBL405884 IC50 = 131.07 nM 6.88
CHEMBL261500 IC50 = 710.0 nM 6.15
CHEMBL405890 IC50 > 1000.0 nM -