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Assay Detail

CHEMBL1678152

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

Functional
Antiplasmodial activity against Plasmodium falciparum 3D7 infected in RBCs by firefly luciferase reporter gene assay
94
Total Activities
94
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

Discovery of potent small-molecule inhibitors of multidrug-resistant Plasmodium falciparum using a novel miniaturized high-throughput luciferase-based assay.
Lucumi E, Darling C, Jo H, Napper AD, Chandramohanadas R, Fisher N, Shone AE, Jing H, Ward SA, Biagini GA, DeGrado WF, Diamond SL, Greenbaum DC.
Antimicrob Agents Chemother (2010) 54 : 3597 -3604
PubMed 20547797 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 94 6.60 10.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL577736 TYROTHRICIN 2.0 1 10.30
CHEMBL1450 ATOVAQUONE 4.0 1 9.39
CHEMBL307261 ARTENIMOL 3.0 1 9.22
CHEMBL90555 VINCRISTINE 4.0 1 9.00
CHEMBL554190 QUINACRINE DIHYDROCHLORIDE 1 9.00
CHEMBL1255782 EMETINE DIHYDROCHLORIDE HYDRATE 1 9.00
CHEMBL159 VINBLASTINE 4.0 1 8.70
CHEMBL416956 MEFLOQUINE 4.0 1 8.68
CHEMBL361497 ARTESUNATE 4.0 1 8.48
CHEMBL1256647 1 8.40
CHEMBL1256788 1 8.30
CHEMBL588619 CINCHONINE -1.0 1 8.30
CHEMBL1673264 1 8.28
CHEMBL438 SULFAMERAZINE 4.0 1 8.22
CHEMBL599514 1 7.96
CHEMBL581889 1 7.85
CHEMBL585145 1 7.85
CHEMBL76 CHLOROQUINE 4.0 1 7.66
CHEMBL599937 1 7.60
CHEMBL58510 CHLOROQUINE PHOSPHATE 4.0 1 7.52
CHEMBL1673265 1 7.50
CHEMBL1257106 AMPEROZIDE HYDROCHLORIDE 1 7.46
CHEMBL1673240 1 7.44
CHEMBL935 1 7.38
CHEMBL3707183 QUINIDINE SULFATE 4.0 1 7.25
CHEMBL464538 1 6.97
CHEMBL1673241 1 6.96
CHEMBL1673242 1 6.89
CHEMBL587714 3',4' DICHLOROBENZAMIL 1 6.84
CHEMBL1673243 1 6.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL577736 TYROTHRICIN IC50 = 0.05 nM 10.30
CHEMBL1450 ATOVAQUONE IC50 = 0.41 nM 9.39
CHEMBL307261 ARTENIMOL IC50 = 0.6 nM 9.22
CHEMBL90555 VINCRISTINE IC50 = 1.0 nM 9.00
CHEMBL554190 QUINACRINE DIHYDROCHLORIDE IC50 = 1.0 nM 9.00
CHEMBL1255782 EMETINE DIHYDROCHLORIDE HYDRATE IC50 = 1.0 nM 9.00
CHEMBL159 VINBLASTINE IC50 = 2.0 nM 8.70
CHEMBL416956 MEFLOQUINE IC50 = 2.1 nM 8.68
CHEMBL361497 ARTESUNATE IC50 = 3.3 nM 8.48
CHEMBL1256647 IC50 = 4.0 nM 8.40
CHEMBL1256788 IC50 = 5.0 nM 8.30
CHEMBL588619 CINCHONINE IC50 = 5.0 nM 8.30
CHEMBL1673264 IC50 = 5.3 nM 8.28
CHEMBL438 SULFAMERAZINE IC50 = 6.0 nM 8.22
CHEMBL599514 IC50 = 11.0 nM 7.96
CHEMBL581889 IC50 = 14.0 nM 7.85
CHEMBL585145 IC50 = 14.0 nM 7.85
CHEMBL76 CHLOROQUINE IC50 = 22.0 nM 7.66
CHEMBL599937 IC50 = 25.0 nM 7.60
CHEMBL58510 CHLOROQUINE PHOSPHATE IC50 = 30.0 nM 7.52
CHEMBL1673265 IC50 = 32.0 nM 7.50
CHEMBL1257106 AMPEROZIDE HYDROCHLORIDE IC50 = 35.0 nM 7.46
CHEMBL1673240 IC50 = 36.0 nM 7.44
CHEMBL935 IC50 = 42.0 nM 7.38
CHEMBL3707183 QUINIDINE SULFATE IC50 = 56.0 nM 7.25
CHEMBL464538 IC50 = 107.0 nM 6.97
CHEMBL1673241 IC50 = 110.0 nM 6.96
CHEMBL1673242 IC50 = 130.0 nM 6.89
CHEMBL587714 3',4' DICHLOROBENZAMIL IC50 = 143.0 nM 6.84
CHEMBL1673243 IC50 = 180.0 nM 6.75
CHEMBL1256878 BENZAMIL HYDROCHLORIDE IC50 = 217.0 nM 6.66
CHEMBL1348834 IC50 = 250.0 nM 6.60
CHEMBL296419 ASTEMIZOLE IC50 = 254.0 nM 6.59
CHEMBL1673244 IC50 = 270.0 nM 6.57
CHEMBL2359966 QUININE SULFATE IC50 = 280.0 nM 6.55
CHEMBL1673245 IC50 = 290.0 nM 6.54
CHEMBL1673246 IC50 = 330.0 nM 6.48
CHEMBL3187985 APOMORPHINE HYDROCHLORIDE IC50 = 373.0 nM 6.43
CHEMBL1671882 IC50 = 410.0 nM 6.39
CHEMBL1673247 IC50 = 420.0 nM 6.38
CHEMBL1673248 IC50 = 430.0 nM 6.37
CHEMBL1673255 IC50 = 440.0 nM 6.36
CHEMBL2092874 AMPEROZIDE DIHYDROCHLORIDE IC50 = 443.0 nM 6.35
CHEMBL1673256 IC50 = 490.0 nM 6.31
CHEMBL1673257 IC50 = 490.0 nM 6.31
CHEMBL1673258 IC50 = 520.0 nM 6.28
CHEMBL1256180 5-(N-METHYL-N-ISOBUTYL)AMILORIDE IC50 = 549.0 nM 6.26
CHEMBL90 HISTAMINE IC50 = 660.0 nM 6.18
CHEMBL1673249 IC50 = 680.0 nM 6.17
CHEMBL1673250 IC50 = 710.0 nM 6.15