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Assay Detail

CHEMBL4768882

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

Binding
Inhibition of recombinant human CK2alpha (1 to 336 residues) expressed in Escherichia coli BL21 (DE3) using RRADDSDDDD as substrate incubated for 10 mins in presence of [gamma-33P]-ATP by scintillation counting assay
16
Total Activities
16
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

A novel class of selective CK2 inhibitors targeting its open hinge conformation.
Dalle Vedove A,Zonta F,Zanforlin E,Demitri N,Ribaudo G,Cazzanelli G,Ongaro A,Sarno S,Zagotto G,Battistutta R,Ruzzene M,Lolli G
Eur J Med Chem (2020) 195 : 112267 -112267
PubMed 32283296 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 6.52 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1230165 SILMITASERTIB 2.0 1 9.00
CHEMBL4795023 1 6.55
CHEMBL4784643 1 6.50
CHEMBL4776391 1 6.48
CHEMBL4778120 1 6.44
CHEMBL4798710 1 6.43
CHEMBL4789806 1 6.43
CHEMBL4070389 1 6.43
CHEMBL4783065 1 6.15
CHEMBL4799521 1 6.06
CHEMBL4796675 1 5.89
CHEMBL4792639 1 5.86
CHEMBL4785453 1 -
CHEMBL4781256 1 -
CHEMBL4788189 1 -
CHEMBL4795570 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1230165 SILMITASERTIB IC50 = 1.0 nM 9.00
CHEMBL4795023 IC50 = 280.0 nM 6.55
CHEMBL4784643 IC50 = 320.0 nM 6.50
CHEMBL4776391 IC50 = 330.0 nM 6.48
CHEMBL4778120 IC50 = 360.0 nM 6.44
CHEMBL4798710 IC50 = 370.0 nM 6.43
CHEMBL4789806 IC50 = 370.0 nM 6.43
CHEMBL4070389 IC50 = 370.0 nM 6.43
CHEMBL4783065 IC50 = 710.0 nM 6.15
CHEMBL4799521 IC50 = 880.0 nM 6.06
CHEMBL4796675 IC50 = 1300.0 nM 5.89
CHEMBL4792639 IC50 = 1370.0 nM 5.86
CHEMBL4785453 IC50 - -
CHEMBL4781256 IC50 - -
CHEMBL4788189 IC50 - -
CHEMBL4795570 IC50 - -