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Assay Detail

CHEMBL1763092

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

Functional
Cytostatic activity against human HeLa cells in presence of 20 uM 2'-deoxyuridine
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HeLa
Confidence 1 — Organism
Curated By Autocuration

Target

HeLa (CHEMBL399)
Type CELL-LINE
Organism Homo sapiens

Publication

Synthesis and biological evaluation of unsaturated keto and exomethylene D-arabinopyranonucleoside analogs: novel 5-fluorouracil analogs that target thymidylate synthase.
Tzioumaki N, Manta S, Tsoukala E, Vande Voorde J, Liekens S, Komiotis D, Balzarini J.
Eur J Med Chem (2011) 46 : 993 -1005
PubMed 21330014 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.51 7.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL917 FLOXURIDINE 4.0 1 7.68
CHEMBL54918 5-FLUOROURIDINE 2.0 1 7.66
CHEMBL185 FLUOROURACIL 4.0 1 6.75
CHEMBL1762220 1 6.21
CHEMBL1762225 1 5.85
CHEMBL1762230 1 4.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL917 FLOXURIDINE IC50 = 21.0 nM 7.68
CHEMBL54918 5-FLUOROURIDINE IC50 = 22.0 nM 7.66
CHEMBL185 FLUOROURACIL IC50 = 180.0 nM 6.75
CHEMBL1762220 IC50 = 620.0 nM 6.21
CHEMBL1762225 IC50 = 1400.0 nM 5.85
CHEMBL1762230 IC50 = 12000.0 nM 4.92