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Assay Detail

CHEMBL2429676

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 tritiated deoxycytidine [3H]-dC uptake
38
Total Activities
38
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

Development of new deoxycytidine kinase inhibitors and noninvasive in vivo evaluation using positron emission tomography.
Murphy JM, Armijo AL, Nomme J, Lee CH, Smith QA, Li Z, Campbell DO, Liao HI, Nathanson DA, Austin WR, Lee JT, Darvish R, Wei L, Wang J, Su Y, Damoiseaux R, Sadeghi S, Phelps ME, Herschman HR, Czernin J, Alexandrova AN, Jung ME, Lavie A, Radu CG.
J Med Chem (2013) 56 : 6696 -6708
PubMed 23947754 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 38 7.36 8.97

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2426563 1 8.97
CHEMBL2426570 1 8.94
CHEMBL2426573 1 8.84
CHEMBL2426569 1 8.81
CHEMBL2426562 1 8.61
CHEMBL2426567 1 8.59
CHEMBL2426564 1 8.55
CHEMBL2426572 1 8.54
CHEMBL2426571 1 8.54
CHEMBL2426558 1 8.52
CHEMBL2426574 1 8.31
CHEMBL2426598 1 8.15
CHEMBL2426566 1 8.10
CHEMBL2426557 1 7.96
CHEMBL2426565 1 7.94
CHEMBL2426588 1 7.75
CHEMBL2426568 1 7.73
CHEMBL2426561 1 7.51
CHEMBL2426560 1 7.43
CHEMBL2426460 1 7.08
CHEMBL2426591 1 7.04
CHEMBL2426589 1 6.82
CHEMBL2426459 1 6.79
CHEMBL2426559 1 6.76
CHEMBL2426585 1 6.71
CHEMBL2426590 1 6.64
CHEMBL2426582 1 6.64
CHEMBL2426583 1 6.60
CHEMBL2426596 1 6.53
CHEMBL2426581 1 6.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2426563 IC50 = 1.07 nM 8.97
CHEMBL2426570 IC50 = 1.15 nM 8.94
CHEMBL2426573 IC50 = 1.44 nM 8.84
CHEMBL2426569 IC50 = 1.55 nM 8.81
CHEMBL2426562 IC50 = 2.45 nM 8.61
CHEMBL2426567 IC50 = 2.59 nM 8.59
CHEMBL2426564 IC50 = 2.83 nM 8.55
CHEMBL2426572 IC50 = 2.85 nM 8.54
CHEMBL2426571 IC50 = 2.9 nM 8.54
CHEMBL2426558 IC50 = 3.0 nM 8.52
CHEMBL2426574 IC50 = 4.89 nM 8.31
CHEMBL2426598 IC50 = 7.0 nM 8.15
CHEMBL2426566 IC50 = 8.01 nM 8.10
CHEMBL2426557 IC50 = 11.0 nM 7.96
CHEMBL2426565 IC50 = 11.58 nM 7.94
CHEMBL2426588 IC50 = 18.0 nM 7.75
CHEMBL2426568 IC50 = 18.62 nM 7.73
CHEMBL2426561 IC50 = 31.0 nM 7.51
CHEMBL2426560 IC50 = 37.0 nM 7.43
CHEMBL2426460 IC50 = 83.0 nM 7.08
CHEMBL2426591 IC50 = 92.0 nM 7.04
CHEMBL2426589 IC50 = 150.0 nM 6.82
CHEMBL2426459 IC50 = 162.0 nM 6.79
CHEMBL2426559 IC50 = 173.0 nM 6.76
CHEMBL2426585 IC50 = 197.0 nM 6.71
CHEMBL2426590 IC50 = 230.0 nM 6.64
CHEMBL2426582 IC50 = 230.0 nM 6.64
CHEMBL2426583 IC50 = 251.0 nM 6.60
CHEMBL2426596 IC50 = 297.0 nM 6.53
CHEMBL2426581 IC50 = 421.0 nM 6.38
CHEMBL2426593 IC50 = 506.0 nM 6.30
CHEMBL2426594 IC50 = 512.0 nM 6.29
CHEMBL2426592 IC50 = 534.0 nM 6.27
CHEMBL2426597 IC50 = 849.0 nM 6.07
CHEMBL2426586 IC50 = 1041.0 nM 5.98
CHEMBL2426595 IC50 = 1922.0 nM 5.72
CHEMBL2426584 IC50 = 1960.0 nM 5.71
CHEMBL2426587 IC50 = 2367.0 nM 5.63