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Assay Detail

CHEMBL4185063

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

Functional
Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 infected in human erythrocytes
28
Total Activities
28
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

Semisynthesis, cytotoxicity, antimalarial evaluation and structure-activity relationship of two series of triterpene derivatives.
Cargnin ST, Staudt AF, Medeiros P, de Medeiros Sol Sol D, de Azevedo Dos Santos AP, Zanchi FB, Gosmann G, Puyet A, Garcia Teles CB, Gnoatto SB.
Bioorg Med Chem Lett (2018) 28 : 265 -272
PubMed 29326018 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 5.07 7.79

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL269671 ARTEMISININ 3.0 1 7.79
CHEMBL76 CHLOROQUINE 4.0 1 6.81
CHEMBL4216644 1 5.47
CHEMBL607802 1 5.28
CHEMBL431525 BETUNOLIC ACID 1 5.10
CHEMBL4210469 1 5.05
CHEMBL410525 O-ACETYLURSOLIC ACID 1 5.04
CHEMBL2147688 1 5.04
CHEMBL4216396 1 4.98
CHEMBL571294 1 4.92
CHEMBL269277 BETULINIC ACID 1.0 1 4.89
CHEMBL611923 1 4.88
CHEMBL4209684 1 4.87
CHEMBL487887 URSONIC ACID 1 4.62
CHEMBL4208831 1 4.53
CHEMBL169 URSOLIC ACID 2.0 1 4.30
CHEMBL2147682 1 4.30
CHEMBL4205923 1 4.24
CHEMBL312687 1 4.18
CHEMBL605530 1 -
CHEMBL4218455 1 -
CHEMBL4213811 1 -
CHEMBL4217631 1 -
CHEMBL376266 METHYL BETULONATE 1 -
CHEMBL508907 1 -
CHEMBL4212196 1 -
CHEMBL4203723 1 -
CHEMBL4216252 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL269671 ARTEMISININ IC50 = 16.3 nM 7.79
CHEMBL76 CHLOROQUINE IC50 = 156.0 nM 6.81
CHEMBL4216644 IC50 = 3400.0 nM 5.47
CHEMBL607802 IC50 = 5200.0 nM 5.28
CHEMBL431525 BETUNOLIC ACID IC50 = 7870.0 nM 5.10
CHEMBL4210469 IC50 = 8900.0 nM 5.05
CHEMBL410525 O-ACETYLURSOLIC ACID IC50 = 9080.0 nM 5.04
CHEMBL2147688 IC50 = 9070.0 nM 5.04
CHEMBL4216396 IC50 = 10390.0 nM 4.98
CHEMBL571294 IC50 = 12110.0 nM 4.92
CHEMBL269277 BETULINIC ACID IC50 = 12780.0 nM 4.89
CHEMBL611923 IC50 = 13320.0 nM 4.88
CHEMBL4209684 IC50 = 13590.0 nM 4.87
CHEMBL487887 URSONIC ACID IC50 = 24260.0 nM 4.62
CHEMBL4208831 IC50 = 29610.0 nM 4.53
CHEMBL169 URSOLIC ACID IC50 = 50640.0 nM 4.30
CHEMBL2147682 IC50 = 50640.0 nM 4.30
CHEMBL4205923 IC50 = 57620.0 nM 4.24
CHEMBL312687 IC50 = 65500.0 nM 4.18
CHEMBL605530 IC50 > 100000.0 nM -
CHEMBL4218455 IC50 > 100000.0 nM -
CHEMBL4213811 IC50 > 100000.0 nM -
CHEMBL4217631 IC50 > 100000.0 nM -
CHEMBL376266 METHYL BETULONATE IC50 > 100000.0 nM -
CHEMBL508907 IC50 > 100000.0 nM -
CHEMBL4212196 IC50 > 100000.0 nM -
CHEMBL4203723 IC50 > 100000.0 nM -
CHEMBL4216252 IC50 > 100000.0 nM -