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Assay Detail

CHEMBL2065441

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

Binding
Inhibition of CK2alpha in human HCT116 cells assessed as decrease in AKT phosphorylation at S129 residue after 3 to 24 hrs by Western blot analysis
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HCT-116
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Potent and Selective Inhibitors of CK2 Kinase Identified through Structure-Guided Hybridization.
Dowling JE, Chuaqui C, Pontz TW, Lyne PD, Larsen NA, Block MH, Chen H, Su N, Wu A, Russell D, Pollard H, Lee JW, Peng B, Thakur K, Ye Q, Zhang T, Brassil P, Racicot V, Bao L, Denz CR, Cooke E.
ACS Med Chem Lett (2012) 3 : 278 -283
PubMed 24900464 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 6.59 7.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2062580 1 7.57
CHEMBL2062577 1 7.47
CHEMBL2062571 1 7.24
CHEMBL2062581 1 7.11
CHEMBL2062579 1 7.08
CHEMBL2062572 1 6.72
CHEMBL2062583 1 6.68
CHEMBL2062573 1 6.34
CHEMBL2062582 1 6.30
CHEMBL2062574 1 6.11
CHEMBL2062578 1 6.08
CHEMBL2062576 1 6.07
CHEMBL2062575 1 5.92
CHEMBL2062585 1 5.51
CHEMBL2062584 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2062580 IC50 = 27.0 nM 7.57
CHEMBL2062577 IC50 = 34.0 nM 7.47
CHEMBL2062571 IC50 = 57.0 nM 7.24
CHEMBL2062581 IC50 = 77.0 nM 7.11
CHEMBL2062579 IC50 = 83.0 nM 7.08
CHEMBL2062572 IC50 = 190.0 nM 6.72
CHEMBL2062583 IC50 = 210.0 nM 6.68
CHEMBL2062573 IC50 = 460.0 nM 6.34
CHEMBL2062582 IC50 = 500.0 nM 6.30
CHEMBL2062574 IC50 = 780.0 nM 6.11
CHEMBL2062578 IC50 = 830.0 nM 6.08
CHEMBL2062576 IC50 = 860.0 nM 6.07
CHEMBL2062575 IC50 = 1200.0 nM 5.92
CHEMBL2062585 IC50 = 3100.0 nM 5.51
CHEMBL2062584 IC50 - -