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Assay Detail

CHEMBL3999952

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

Functional
Antiplasmodial activity against chloroquine resistant Plasmodium falciparum K1 erythrocytic stage assessed as reduction in [3H]hypoxanthine incorporation after 48 hrs by liquid scintillation counting assay
29
Total Activities
29
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

Synthesis and activity of nucleoside-based antiprotozoan compounds.
Tran HA, Zheng Z, Wen X, Manivannan S, Pastor A, Kaiser M, Brun R, Snyder FF, Back TG.
Bioorg Med Chem (2017) 25 : 2091 -2104
PubMed 28284860 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 4.99 6.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL76 CHLOROQUINE 4.0 1 6.85
CHEMBL4075657 1 6.05
CHEMBL4060076 1 5.96
CHEMBL4070000 1 5.82
CHEMBL4091995 1 5.55
CHEMBL4074699 1 5.41
CHEMBL4093177 1 5.24
CHEMBL4090399 1 5.10
CHEMBL4084731 1 5.01
CHEMBL4097315 1 5.00
CHEMBL4076916 1 4.92
CHEMBL4076818 1 4.89
CHEMBL4076721 1 4.85
CHEMBL4094270 1 4.72
CHEMBL4066090 1 4.72
CHEMBL4071448 1 4.69
CHEMBL4100225 1 4.64
CHEMBL4085214 1 4.60
CHEMBL4081985 1 4.54
CHEMBL4105508 1 4.43
CHEMBL4091532 1 4.35
CHEMBL4067099 1 4.19
CHEMBL4062813 1 4.17
CHEMBL4073644 1 4.06
CHEMBL4085977 1 -
CHEMBL4088363 1 -
CHEMBL4093664 1 -
CHEMBL4090762 1 -
CHEMBL4061466 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL76 CHLOROQUINE IC50 = 140.0 nM 6.85
CHEMBL4075657 IC50 = 890.0 nM 6.05
CHEMBL4060076 IC50 = 1100.0 nM 5.96
CHEMBL4070000 IC50 = 1500.0 nM 5.82
CHEMBL4091995 IC50 = 2800.0 nM 5.55
CHEMBL4074699 IC50 = 3900.0 nM 5.41
CHEMBL4093177 IC50 = 5800.0 nM 5.24
CHEMBL4090399 IC50 = 8000.0 nM 5.10
CHEMBL4084731 IC50 = 9800.0 nM 5.01
CHEMBL4097315 IC50 = 10000.0 nM 5.00
CHEMBL4076916 IC50 = 12000.0 nM 4.92
CHEMBL4076818 IC50 = 13000.0 nM 4.89
CHEMBL4076721 IC50 = 14000.0 nM 4.85
CHEMBL4094270 IC50 = 19000.0 nM 4.72
CHEMBL4066090 IC50 = 19000.0 nM 4.72
CHEMBL4071448 IC50 = 20500.0 nM 4.69
CHEMBL4100225 IC50 = 23000.0 nM 4.64
CHEMBL4085214 IC50 = 25000.0 nM 4.60
CHEMBL4081985 IC50 = 29000.0 nM 4.54
CHEMBL4105508 IC50 = 37000.0 nM 4.43
CHEMBL4091532 IC50 = 45000.0 nM 4.35
CHEMBL4067099 IC50 = 65000.0 nM 4.19
CHEMBL4062813 IC50 = 68000.0 nM 4.17
CHEMBL4073644 IC50 = 88000.0 nM 4.06
CHEMBL4085977 IC50 = 102000.0 nM -
CHEMBL4088363 IC50 > 170000.0 nM -
CHEMBL4093664 IC50 = 150000.0 nM -
CHEMBL4090762 IC50 > 168000.0 nM -
CHEMBL4061466 IC50 = 106000.0 nM -