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Assay Detail

CHEMBL3381706

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

Binding
Inhibition of dCK in human CCRF-CEM cells assessed as inhibition of [3H]-dC uptake by scintillation counting analysis
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CCRF-CEM
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Deoxycytidine kinase (CHEMBL2447)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-guided development of deoxycytidine kinase inhibitors with nanomolar affinity and improved metabolic stability.
Nomme J, Li Z, Gipson RM, Wang J, Armijo AL, Le T, Poddar S, Smith T, Santarsiero BD, Nguyen HA, Czernin J, Alexandrova AN, Jung ME, Radu CG, Lavie A.
J Med Chem (2014) 57 : 9480 -9494
PubMed 25341194 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 7.98 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2426567 1 9.05
CHEMBL2426570 1 8.94
CHEMBL3358096 1 8.90
CHEMBL2426573 1 8.85
CHEMBL3358097 1 8.43
CHEMBL2426574 1 8.31
CHEMBL3358094 1 8.15
CHEMBL3358093 1 8.00
CHEMBL2426565 1 7.94
CHEMBL2426568 1 7.73
CHEMBL3358091 1 7.66
CHEMBL3358090 1 7.03
CHEMBL3358092 1 6.40
CHEMBL3358095 1 6.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2426567 IC50 = 0.9 nM 9.05
CHEMBL2426570 IC50 = 1.15 nM 8.94
CHEMBL3358096 IC50 = 1.25 nM 8.90
CHEMBL2426573 IC50 = 1.4 nM 8.85
CHEMBL3358097 IC50 = 3.7 nM 8.43
CHEMBL2426574 IC50 = 4.9 nM 8.31
CHEMBL3358094 IC50 = 7.0 nM 8.15
CHEMBL3358093 IC50 = 10.0 nM 8.00
CHEMBL2426565 IC50 = 11.6 nM 7.94
CHEMBL2426568 IC50 = 18.6 nM 7.73
CHEMBL3358091 IC50 = 21.8 nM 7.66
CHEMBL3358090 IC50 = 94.0 nM 7.03
CHEMBL3358092 IC50 = 395.0 nM 6.40
CHEMBL3358095 IC50 = 429.5 nM 6.37