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Assay Detail

CHEMBL2186945

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

Functional
Cytostatic activity against human CEM/0 cells after 72 hrs by cell counting
41
Total Activities
41
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 41 6.68 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2181358 1 7.82
CHEMBL917 FLOXURIDINE 4.0 1 7.66
CHEMBL2181361 1 7.46
CHEMBL2181364 1 7.28
CHEMBL2181362 1 7.24
CHEMBL2181365 1 7.23
CHEMBL2181357 1 7.19
CHEMBL2181367 FOSIFLOXURIDINE NAFALBENAMIDE 2.0 1 7.17
CHEMBL2181370 1 7.15
CHEMBL2181360 1 7.14
CHEMBL2181359 1 7.10
CHEMBL2181366 1 7.10
CHEMBL2181374 1 7.00
CHEMBL2181373 1 7.00
CHEMBL2181368 1 6.96
CHEMBL2181371 1 6.89
CHEMBL2181356 1 6.85
CHEMBL2181354 1 6.85
CHEMBL2181355 1 6.80
CHEMBL2181555 1 6.77
CHEMBL2181556 1 6.75
CHEMBL2181375 1 6.72
CHEMBL2181565 1 6.64
CHEMBL2181558 1 6.62
CHEMBL2181566 1 6.60
CHEMBL2181560 1 6.60
CHEMBL2181562 1 6.55
CHEMBL2181561 1 6.46
CHEMBL2181376 1 6.44
CHEMBL2181372 1 6.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2181358 IC50 = 15.0 nM 7.82
CHEMBL917 FLOXURIDINE IC50 = 22.0 nM 7.66
CHEMBL2181361 IC50 = 35.0 nM 7.46
CHEMBL2181364 IC50 = 53.0 nM 7.28
CHEMBL2181362 IC50 = 57.0 nM 7.24
CHEMBL2181365 IC50 = 59.0 nM 7.23
CHEMBL2181357 IC50 = 64.0 nM 7.19
CHEMBL2181367 FOSIFLOXURIDINE NAFALBENAMIDE IC50 = 68.0 nM 7.17
CHEMBL2181370 IC50 = 71.0 nM 7.15
CHEMBL2181360 IC50 = 73.0 nM 7.14
CHEMBL2181366 IC50 = 79.0 nM 7.10
CHEMBL2181359 IC50 = 80.0 nM 7.10
CHEMBL2181374 IC50 = 100.0 nM 7.00
CHEMBL2181373 IC50 = 100.0 nM 7.00
CHEMBL2181368 IC50 = 110.0 nM 6.96
CHEMBL2181371 IC50 = 130.0 nM 6.89
CHEMBL2181356 IC50 = 140.0 nM 6.85
CHEMBL2181354 IC50 = 140.0 nM 6.85
CHEMBL2181355 IC50 = 160.0 nM 6.80
CHEMBL2181555 IC50 = 170.0 nM 6.77
CHEMBL2181556 IC50 = 180.0 nM 6.75
CHEMBL2181375 IC50 = 190.0 nM 6.72
CHEMBL2181565 IC50 = 230.0 nM 6.64
CHEMBL2181558 IC50 = 240.0 nM 6.62
CHEMBL2181566 IC50 = 250.0 nM 6.60
CHEMBL2181560 IC50 = 250.0 nM 6.60
CHEMBL2181562 IC50 = 280.0 nM 6.55
CHEMBL2181561 IC50 = 350.0 nM 6.46
CHEMBL2181376 IC50 = 360.0 nM 6.44
CHEMBL2181372 IC50 = 460.0 nM 6.34
CHEMBL2181363 IC50 = 490.0 nM 6.31
CHEMBL2181564 IC50 = 650.0 nM 6.19
CHEMBL2046836 IC50 = 700.0 nM 6.16
CHEMBL2181369 IC50 = 800.0 nM 6.10
CHEMBL2177147 IC50 = 890.0 nM 6.05
CHEMBL2181553 IC50 = 920.0 nM 6.04
CHEMBL2181563 IC50 = 980.0 nM 6.01
CHEMBL2181557 IC50 = 1000.0 nM 6.00
CHEMBL2181559 IC50 = 1000.0 nM 6.00
CHEMBL2181554 IC50 = 1000.0 nM 6.00
CHEMBL185 FLUOROURACIL IC50 = 18000.0 nM 4.75