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Assay Detail

CHEMBL4222674

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

Binding
Inhibition of CK2alpha in human HCT116 or human DLD1 cells assessed as decrease in AKT phosphorylation at S129 residue after 3 to 24 hrs by Western blot method
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Casein kinase II subunit alpha (CHEMBL3629)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of 2,6-disubstituted pyrazine derivatives as inhibitors of CK2 and PIM kinases.
Gingipalli L, Block MH, Bao L, Cooke E, Dakin LA, Denz CR, Ferguson AD, Johannes JW, Larsen NA, Lyne PD, Pontz TW, Wang T, Wu X, Wu A, Zhang HJ, Zheng X, Dowling JE, Lamb ML.
Bioorg Med Chem Lett (2018) 28 : 1336 -1341
PubMed 29559278 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.20 7.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4225287 1 7.02
CHEMBL4228654 1 6.96
CHEMBL4224859 1 6.75
CHEMBL4227817 1 6.47
CHEMBL4228363 1 6.00
CHEMBL1231683 1 5.57
CHEMBL4227886 1 5.47
CHEMBL4225224 1 5.37
CHEMBL4228394 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4225287 IC50 = 96.0 nM 7.02
CHEMBL4228654 IC50 = 110.0 nM 6.96
CHEMBL4224859 IC50 = 180.0 nM 6.75
CHEMBL4227817 IC50 = 340.0 nM 6.47
CHEMBL4228363 IC50 = 1000.0 nM 6.00
CHEMBL1231683 IC50 = 2700.0 nM 5.57
CHEMBL4227886 IC50 = 3400.0 nM 5.47
CHEMBL4225224 IC50 = 4300.0 nM 5.37
CHEMBL4228394 IC50 > 3300.0 nM -