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Assay Detail

CHEMBL811734

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

Binding
Inhibitory effect against phosphorylation of [methyl-3H]dThd by Thymidine Kinase 2 (TK-2)
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Thymidine kinase, cytosolic (CHEMBL2883)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Acyclic nucleoside analogues as novel inhibitors of human mitochondrial thymidine kinase.
Hernández AI, Balzarini J, Karlsson A, Camarasa MJ, Pérez-Pérez MJ.
J Med Chem (2002) 45 : 4254 -4263
PubMed 12213066 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 4.92 5.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL101135 1 5.82
CHEMBL134471 1 5.48
CHEMBL341163 1 5.44
CHEMBL337264 1 5.34
CHEMBL335866 1 5.34
CHEMBL134857 1 5.01
CHEMBL134449 1 4.96
CHEMBL135863 1 4.77
CHEMBL135496 1 4.72
CHEMBL334803 1 4.70
CHEMBL132921 1 4.66
CHEMBL422810 1 4.60
CHEMBL135079 1 4.55
CHEMBL335521 1 4.52
CHEMBL2403290 1 4.48
CHEMBL435798 1 4.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL101135 IC50 = 1500.0 nM 5.82
CHEMBL134471 IC50 = 3300.0 nM 5.48
CHEMBL341163 IC50 = 3600.0 nM 5.44
CHEMBL337264 IC50 = 4600.0 nM 5.34
CHEMBL335866 IC50 = 4600.0 nM 5.34
CHEMBL134857 IC50 = 9800.0 nM 5.01
CHEMBL134449 IC50 = 11000.0 nM 4.96
CHEMBL135863 IC50 = 17000.0 nM 4.77
CHEMBL135496 IC50 = 19000.0 nM 4.72
CHEMBL334803 IC50 = 20000.0 nM 4.70
CHEMBL132921 IC50 = 22000.0 nM 4.66
CHEMBL422810 IC50 = 25000.0 nM 4.60
CHEMBL135079 IC50 = 28000.0 nM 4.55
CHEMBL335521 IC50 = 30000.0 nM 4.52
CHEMBL2403290 IC50 = 33000.0 nM 4.48
CHEMBL435798 IC50 = 40000.0 nM 4.40