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Assay Detail

CHEMBL2186929

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Functional
Cytostatic activity against human CEM cells expressing human ENT1 transporter after 72 hrs by cell counting
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CCRF-CEM
Confidence 1 — Organism
Curated By Autocuration

Target

CCRF-CEM (CHEMBL382)
Type CELL-LINE
Organism Homo sapiens

Publication

Phosphoramidate ProTides of the anticancer agent FUDR successfully deliver the preformed bioactive monophosphate in cells and confer advantage over the parent nucleoside.
McGuigan C, Murziani P, Slusarczyk M, Gonczy B, Vande Voorde J, Liekens S, Balzarini J.
J Med Chem (2011) 54 : 7247 -7258
PubMed 21892829 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.01 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL917 FLOXURIDINE 4.0 1 7.40
CHEMBL886 5-FLUORODEOXYURIDYLATE 1 7.30
CHEMBL2181355 1 7.30
CHEMBL2181367 FOSIFLOXURIDINE NAFALBENAMIDE 2.0 1 7.30
CHEMBL2181556 1 6.89
CHEMBL2181565 1 6.77
CHEMBL2181376 1 6.68
CHEMBL2181564 1 6.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL917 FLOXURIDINE IC50 = 40.0 nM 7.40
CHEMBL886 5-FLUORODEOXYURIDYLATE IC50 = 50.0 nM 7.30
CHEMBL2181355 IC50 = 50.0 nM 7.30
CHEMBL2181367 FOSIFLOXURIDINE NAFALBENAMIDE IC50 = 50.0 nM 7.30
CHEMBL2181556 IC50 = 130.0 nM 6.89
CHEMBL2181565 IC50 = 170.0 nM 6.77
CHEMBL2181376 IC50 = 210.0 nM 6.68
CHEMBL2181564 IC50 = 370.0 nM 6.43