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Assay Detail

CHEMBL4180223

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

Functional
Antimalarial activity against Plasmodium falciparum 3D7 infected in ARh+ human erythrocytes after 42 to 48 hrs by Picogreen staining-based 96 well microplate assay
41
Total Activities
41
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

Astemizole analogues with reduced hERG inhibition as potent antimalarial compounds.
Tian J, Vandermosten L, Peigneur S, Moreels L, Rozenski J, Tytgat J, Herdewijn P, Van den Steen PE, De Jonghe S.
Bioorg Med Chem (2017) 25 : 6332 -6344
PubMed 29042223 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 41 6.13 7.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4217155 1 7.55
CHEMBL4205490 1 7.54
CHEMBL4217209 1 7.54
CHEMBL4207128 1 7.41
CHEMBL4204991 1 7.30
CHEMBL4213322 1 7.11
CHEMBL4208355 1 7.07
CHEMBL4208389 1 6.96
CHEMBL58025 1 6.90
CHEMBL296419 ASTEMIZOLE 4.0 1 6.79
CHEMBL236609 1 6.71
CHEMBL4212002 1 6.62
CHEMBL59081 1 6.46
CHEMBL4212778 1 6.38
CHEMBL432296 1 6.14
CHEMBL4207613 1 6.08
CHEMBL4217373 1 6.07
CHEMBL236785 1 5.72
CHEMBL4213619 1 5.65
CHEMBL61301 TECASTEMIZOLE 2.0 1 5.64
CHEMBL59015 1 5.51
CHEMBL4206159 1 5.40
CHEMBL4217400 1 5.33
CHEMBL4202777 1 5.27
CHEMBL4210527 1 5.21
CHEMBL4209466 1 5.20
CHEMBL4203304 1 5.18
CHEMBL4205028 1 5.17
CHEMBL4205096 1 5.16
CHEMBL4218790 1 5.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4217155 IC50 = 28.0 nM 7.55
CHEMBL4205490 IC50 = 29.0 nM 7.54
CHEMBL4217209 IC50 = 29.0 nM 7.54
CHEMBL4207128 IC50 = 39.4 nM 7.41
CHEMBL4204991 IC50 = 50.0 nM 7.30
CHEMBL4213322 IC50 = 78.0 nM 7.11
CHEMBL4208355 IC50 = 85.0 nM 7.07
CHEMBL4208389 IC50 = 111.0 nM 6.96
CHEMBL58025 IC50 = 125.0 nM 6.90
CHEMBL296419 ASTEMIZOLE IC50 = 162.0 nM 6.79
CHEMBL236609 IC50 = 196.0 nM 6.71
CHEMBL4212002 IC50 = 240.0 nM 6.62
CHEMBL59081 IC50 = 344.0 nM 6.46
CHEMBL4212778 IC50 = 416.0 nM 6.38
CHEMBL432296 IC50 = 718.0 nM 6.14
CHEMBL4207613 IC50 = 829.0 nM 6.08
CHEMBL4217373 IC50 = 857.0 nM 6.07
CHEMBL236785 IC50 = 1902.0 nM 5.72
CHEMBL4213619 IC50 = 2245.0 nM 5.65
CHEMBL61301 TECASTEMIZOLE IC50 = 2304.0 nM 5.64
CHEMBL59015 IC50 = 3089.0 nM 5.51
CHEMBL4206159 IC50 = 3956.0 nM 5.40
CHEMBL4217400 IC50 = 4642.0 nM 5.33
CHEMBL4202777 IC50 = 5322.0 nM 5.27
CHEMBL4210527 IC50 = 6178.0 nM 5.21
CHEMBL4209466 IC50 = 6280.0 nM 5.20
CHEMBL4203304 IC50 = 6527.0 nM 5.18
CHEMBL4205028 IC50 = 6740.0 nM 5.17
CHEMBL4205096 IC50 = 6848.0 nM 5.16
CHEMBL4218790 IC50 = 8142.0 nM 5.09
CHEMBL4209978 IC50 = 8287.0 nM 5.08
CHEMBL4206953 IC50 = 10040.0 nM 5.00
CHEMBL4208506 IC50 > 10000.0 nM -
CHEMBL4204167 IC50 > 10000.0 nM -
CHEMBL4214370 IC50 > 10000.0 nM -
CHEMBL4213858 IC50 > 10000.0 nM -
CHEMBL4205611 IC50 > 10000.0 nM -
CHEMBL4217321 IC50 > 10000.0 nM -
CHEMBL4207868 IC50 > 10000.0 nM -
CHEMBL4216701 IC50 > 10000.0 nM -
CHEMBL4210677 IC50 > 10000.0 nM -