Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL908767

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

Binding
Inhibition of [3H]methyl dThd phosphorylation by TK2
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Thymidine kinase 2, mitochondrial (CHEMBL4580)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

N1-substituted thymine derivatives as mitochondrial thymidine kinase (TK-2) inhibitors.
Hernandez AI, Familiar O, Negri A, Rodríguez-Barrios F, Gago F, Karlsson A, Camarasa MJ, Balzarini J, Pérez-Pérez MJ.
J Med Chem (2006) 49 : 7766 -7773
PubMed 17181158 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 5.43 6.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL219299 1 6.41
CHEMBL220459 1 6.33
CHEMBL216998 1 6.30
CHEMBL101135 1 5.82
CHEMBL373998 1 5.75
CHEMBL385954 1 5.72
CHEMBL219960 1 5.72
CHEMBL373997 1 5.62
CHEMBL216997 1 5.60
CHEMBL219367 1 5.33
CHEMBL219458 1 5.28
CHEMBL219905 1 5.01
CHEMBL438603 1 4.64
CHEMBL219510 1 4.64
CHEMBL374244 1 4.35
CHEMBL384435 1 4.35
CHEMBL219908 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL219299 IC50 = 390.0 nM 6.41
CHEMBL220459 IC50 = 470.0 nM 6.33
CHEMBL216998 IC50 = 500.0 nM 6.30
CHEMBL101135 IC50 = 1500.0 nM 5.82
CHEMBL373998 IC50 = 1800.0 nM 5.75
CHEMBL385954 IC50 = 1900.0 nM 5.72
CHEMBL219960 IC50 = 1900.0 nM 5.72
CHEMBL373997 IC50 = 2400.0 nM 5.62
CHEMBL216997 IC50 = 2500.0 nM 5.60
CHEMBL219367 IC50 = 4700.0 nM 5.33
CHEMBL219458 IC50 = 5200.0 nM 5.28
CHEMBL219905 IC50 = 9700.0 nM 5.01
CHEMBL438603 IC50 = 23000.0 nM 4.64
CHEMBL219510 IC50 = 23000.0 nM 4.64
CHEMBL374244 IC50 = 45000.0 nM 4.35
CHEMBL384435 IC50 = 45000.0 nM 4.35
CHEMBL219908 IC50 = 114000.0 nM -