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Assay Detail

CHEMBL3760461

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

Binding
Inhibition of GST-tagged human CK2alpha' (1 to 350 residues) using CK2tide as substrate incubated for 1 hr by off-chip mobility shift assay
18
Total Activities
18
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' (CHEMBL4070)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-activity relationship study of 4-(thiazol-5-yl)benzoic acid derivatives as potent protein kinase CK2 inhibitors.
Ohno H, Minamiguchi D, Nakamura S, Shu K, Okazaki S, Honda M, Misu R, Moriwaki H, Nakanishi S, Oishi S, Kinoshita T, Nakanishi I, Fujii N.
Bioorg Med Chem (2016) 24 : 1136 -1141
PubMed 26850376 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 7.83 8.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3760043 1 8.34
CHEMBL3759871 1 8.06
CHEMBL3758606 1 8.02
CHEMBL3758317 1 8.02
CHEMBL3759512 1 8.01
CHEMBL3759755 1 8.00
CHEMBL3758519 1 8.00
CHEMBL1230165 SILMITASERTIB 2.0 1 7.96
CHEMBL2087023 1 7.96
CHEMBL3759349 1 7.96
CHEMBL3760009 1 7.96
CHEMBL3760064 1 7.92
CHEMBL3758270 1 7.92
CHEMBL3758895 1 7.89
CHEMBL3758777 1 7.85
CHEMBL3759193 1 7.72
CHEMBL3759388 1 6.80
CHEMBL3758475 1 6.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3760043 IC50 = 4.6 nM 8.34
CHEMBL3759871 IC50 = 8.8 nM 8.06
CHEMBL3758606 IC50 = 9.5 nM 8.02
CHEMBL3758317 IC50 = 9.6 nM 8.02
CHEMBL3759512 IC50 = 9.8 nM 8.01
CHEMBL3759755 IC50 = 10.0 nM 8.00
CHEMBL3758519 IC50 = 10.0 nM 8.00
CHEMBL1230165 SILMITASERTIB IC50 = 11.0 nM 7.96
CHEMBL2087023 IC50 = 11.0 nM 7.96
CHEMBL3759349 IC50 = 11.0 nM 7.96
CHEMBL3760009 IC50 = 11.0 nM 7.96
CHEMBL3760064 IC50 = 12.0 nM 7.92
CHEMBL3758270 IC50 = 12.0 nM 7.92
CHEMBL3758895 IC50 = 13.0 nM 7.89
CHEMBL3758777 IC50 = 14.0 nM 7.85
CHEMBL3759193 IC50 = 19.0 nM 7.72
CHEMBL3759388 IC50 = 160.0 nM 6.80
CHEMBL3758475 IC50 = 280.0 nM 6.55