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Assay Detail

CHEMBL4839279

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Functional
Antiplasmodial activity against chloroquine-sensitive synchronized Plasmodium falciparum NF54 late trophozoite stage assessed as reduction in parasite survival incubated for 72 hrs under hypoxic condition by parasite lactate dehydrogenase based NBT microplate reader assay
48
Total Activities
48
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

Structure-Activity Relationship Studies Reveal New Astemizole Analogues Active against <i>Plasmodium falciparum</i> In Vitro.
Mambwe D, Kumar M, Ferger R, Taylor D, Njoroge M, Coertzen D, Reader J, van der Watt M, Birkholtz LM, Chibale K.
ACS Med Chem Lett (2021) 12 : 1333 -1341
PubMed 34413963 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 48 6.43 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL76 CHLOROQUINE 4.0 1 8.40
CHEMBL4870498 1 7.60
CHEMBL4878008 1 7.46
CHEMBL4845682 1 7.37
CHEMBL4873570 1 7.17
CHEMBL4867115 1 7.15
CHEMBL296419 ASTEMIZOLE 4.0 1 7.07
CHEMBL4856116 1 6.97
CHEMBL4870175 1 6.81
CHEMBL4848003 1 6.81
CHEMBL4864536 1 6.79
CHEMBL4854035 1 6.73
CHEMBL4853871 1 6.70
CHEMBL4852576 1 6.69
CHEMBL4870928 1 6.62
CHEMBL4855930 1 6.60
CHEMBL4864996 1 6.60
CHEMBL4863264 1 6.58
CHEMBL4858358 1 6.53
CHEMBL4865822 1 6.50
CHEMBL4849566 1 6.50
CHEMBL4868855 1 6.48
CHEMBL4856394 1 6.45
CHEMBL4847937 1 6.31
CHEMBL4870154 1 6.25
CHEMBL4868736 1 6.24
CHEMBL4874966 1 6.23
CHEMBL4857256 1 6.21
CHEMBL4871227 1 6.19
CHEMBL4869885 1 6.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL76 CHLOROQUINE IC50 = 4.0 nM 8.40
CHEMBL4870498 IC50 = 25.0 nM 7.60
CHEMBL4878008 IC50 = 35.0 nM 7.46
CHEMBL4845682 IC50 = 43.0 nM 7.37
CHEMBL4873570 IC50 = 67.0 nM 7.17
CHEMBL4867115 IC50 = 71.0 nM 7.15
CHEMBL296419 ASTEMIZOLE IC50 = 86.0 nM 7.07
CHEMBL4856116 IC50 = 108.0 nM 6.97
CHEMBL4870175 IC50 = 156.0 nM 6.81
CHEMBL4848003 IC50 = 156.0 nM 6.81
CHEMBL4864536 IC50 = 163.0 nM 6.79
CHEMBL4854035 IC50 = 185.0 nM 6.73
CHEMBL4853871 IC50 = 199.0 nM 6.70
CHEMBL4852576 IC50 = 204.0 nM 6.69
CHEMBL4870928 IC50 = 238.0 nM 6.62
CHEMBL4855930 IC50 = 253.0 nM 6.60
CHEMBL4864996 IC50 = 249.0 nM 6.60
CHEMBL4863264 IC50 = 261.0 nM 6.58
CHEMBL4858358 IC50 = 295.0 nM 6.53
CHEMBL4865822 IC50 = 318.0 nM 6.50
CHEMBL4849566 IC50 = 314.0 nM 6.50
CHEMBL4868855 IC50 = 330.0 nM 6.48
CHEMBL4856394 IC50 = 357.0 nM 6.45
CHEMBL4847937 IC50 = 485.0 nM 6.31
CHEMBL4870154 IC50 = 565.0 nM 6.25
CHEMBL4868736 IC50 = 579.0 nM 6.24
CHEMBL4874966 IC50 = 591.0 nM 6.23
CHEMBL4857256 IC50 = 624.0 nM 6.21
CHEMBL4871227 IC50 = 640.0 nM 6.19
CHEMBL4869885 IC50 = 691.0 nM 6.16
CHEMBL4862830 IC50 = 706.0 nM 6.15
CHEMBL4848243 IC50 = 755.0 nM 6.12
CHEMBL4869345 IC50 = 759.0 nM 6.12
CHEMBL4875062 IC50 = 1248.0 nM 5.90
CHEMBL4852936 IC50 = 1386.0 nM 5.86
CHEMBL4850317 IC50 = 1542.0 nM 5.81
CHEMBL4849683 IC50 = 1613.0 nM 5.79
CHEMBL4876459 IC50 = 1677.0 nM 5.78
CHEMBL4856501 IC50 = 1810.0 nM 5.74
CHEMBL4871162 IC50 = 1912.0 nM 5.72
CHEMBL1504080 IC50 = 2890.0 nM 5.54
CHEMBL4848964 IC50 = 3180.0 nM 5.50
CHEMBL4846897 IC50 = 4152.0 nM 5.38
CHEMBL4858498 IC50 = 5080.0 nM 5.29
CHEMBL4859285 IC50 > 6000.0 nM -
CHEMBL4856218 IC50 > 6000.0 nM -
CHEMBL4846385 IC50 > 6000.0 nM -
CHEMBL4860373 IC50 > 6000.0 nM -