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Assay Detail

CHEMBL4811093

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

Functional
Antimalarial activity against chloroquine-sensitive plasmodium falciparum 3D7 infected in human erythrocytes assessed as parasite growth inhibition measured after 72 hrs by SYBR green dye based fluorescence analysis
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Plasmodium falciparum
Cell Type Erythrocyte
Confidence 1 — Organism
Curated By Autocuration

Target

Plasmodium falciparum (CHEMBL364)
Type ORGANISM
Organism Plasmodium falciparum

Publication

Preparation, biological & cheminformatics-based assessment of N<sup>2</sup>,N<sup>4</sup>-diphenylpyrimidine-2,4-diamine as potential Kinase-targeted antimalarials.
Toviwek B, Phuangsawai O, Konsue A, Hannongbua S, Riley J, Mutter N, Anderson M, Webster L, Hallyburton I, Read KD, Gleeson MP.
Bioorg Med Chem (2021) 46 : 116348 -116348
PubMed 34479064 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 33 5.92 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL36 PYRIMETHAMINE 4.0 1 8.40
CHEMBL172 (S,R)-MEFLOQUINE 1 7.85
CHEMBL307261 ARTENIMOL 3.0 1 7.51
CHEMBL527864 1 7.40
CHEMBL189862 1 6.92
CHEMBL4850121 1 6.38
CHEMBL4869308 1 6.22
CHEMBL4858727 1 6.18
CHEMBL4855763 1 6.11
CHEMBL4855061 1 6.11
CHEMBL4852173 1 6.06
CHEMBL4869819 1 6.01
CHEMBL4854098 1 5.96
CHEMBL4879064 1 5.85
CHEMBL4874210 1 5.80
CHEMBL4858018 1 5.70
CHEMBL4857511 1 5.66
CHEMBL4854275 1 5.62
CHEMBL4848690 1 5.60
CHEMBL4873694 1 5.60
CHEMBL4875807 1 5.58
CHEMBL4857289 1 5.55
CHEMBL4855638 1 5.50
CHEMBL4845852 1 5.50
CHEMBL4869115 1 5.44
CHEMBL4846172 1 5.38
CHEMBL4847999 1 5.38
CHEMBL4858355 1 5.27
CHEMBL4874204 1 5.09
CHEMBL4866479 1 5.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL36 PYRIMETHAMINE IC50 = 4.0 nM 8.40
CHEMBL172 (S,R)-MEFLOQUINE IC50 = 14.0 nM 7.85
CHEMBL307261 ARTENIMOL IC50 = 31.0 nM 7.51
CHEMBL527864 IC50 = 40.0 nM 7.40
CHEMBL189862 IC50 = 120.0 nM 6.92
CHEMBL4850121 IC50 = 420.0 nM 6.38
CHEMBL4869308 IC50 = 600.0 nM 6.22
CHEMBL4858727 IC50 = 660.0 nM 6.18
CHEMBL4855763 IC50 = 780.0 nM 6.11
CHEMBL4855061 IC50 = 770.0 nM 6.11
CHEMBL4852173 IC50 = 870.0 nM 6.06
CHEMBL4869819 IC50 = 980.0 nM 6.01
CHEMBL4854098 IC50 = 1100.0 nM 5.96
CHEMBL4879064 IC50 = 1400.0 nM 5.85
CHEMBL4874210 IC50 = 1600.0 nM 5.80
CHEMBL4858018 IC50 = 2000.0 nM 5.70
CHEMBL4857511 IC50 = 2200.0 nM 5.66
CHEMBL4854275 IC50 = 2400.0 nM 5.62
CHEMBL4848690 IC50 = 2500.0 nM 5.60
CHEMBL4873694 IC50 = 2500.0 nM 5.60
CHEMBL4875807 IC50 = 2600.0 nM 5.58
CHEMBL4857289 IC50 = 2800.0 nM 5.55
CHEMBL4855638 IC50 = 3200.0 nM 5.50
CHEMBL4845852 IC50 = 3200.0 nM 5.50
CHEMBL4869115 IC50 = 3600.0 nM 5.44
CHEMBL4846172 IC50 = 4200.0 nM 5.38
CHEMBL4847999 IC50 = 4200.0 nM 5.38
CHEMBL4858355 IC50 = 5400.0 nM 5.27
CHEMBL4874204 IC50 = 8200.0 nM 5.09
CHEMBL4866479 IC50 = 8200.0 nM 5.09
CHEMBL4849865 IC50 = 10000.0 nM 5.00
CHEMBL3819014 IC50 = 13000.0 nM 4.89
CHEMBL4879046 IC50 = 19000.0 nM 4.72