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Assay Detail

CHEMBL5382173

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

Binding
Inhibition of rat liver CK2 phosphorylation using RRRADDSDDDDD as substrate in presence of [32p]-ATP
22
Total Activities
16
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Casein kinase 2 (CHEMBL3988629)
Type PROTEIN COMPLEX
Organism Rattus norvegicus

Publication

Strategies of Targeting CK2 in Drug Discovery: Challenges, Opportunities, and Emerging Prospects.
Chen Y, Wang Y, Wang J, Zhou Z, Cao S, Zhang J.
J Med Chem (2023) 66 : 2257 -2281
PubMed 36745746 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 6.03 7.00
Ki 6 6.89 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL373937 2 7.40
CHEMBL273101 2 7.22
CHEMBL270724 2 7.11
CHEMBL270722 2 6.66
CHEMBL376505 2 6.52
CHEMBL31574 FISETIN 2.0 1 6.46
CHEMBL177820 TETRABROMOBENZOTRIAZOLE 2 6.40
CHEMBL150 KAEMPFEROL 1.0 1 6.40
CHEMBL151 LUTEOLIN 2.0 1 6.30
CHEMBL50 QUERCETIN 3.0 1 6.26
CHEMBL28 APIGENIN 1 6.10
CHEMBL164 MYRICETIN 1 6.04
CHEMBL117 CHRYSIN 1 5.05
CHEMBL28626 MORIN 1 5.00
CHEMBL8260 BAICALEIN 2.0 1 5.00
CHEMBL44 GENISTEIN 2.0 1 4.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL373937 Ki = 40.0 nM 7.40
CHEMBL273101 Ki = 60.0 nM 7.22
CHEMBL270724 Ki = 77.0 nM 7.11
CHEMBL273101 IC50 = 100.0 nM 7.00
CHEMBL270724 IC50 = 110.0 nM 6.96
CHEMBL373937 IC50 = 140.0 nM 6.85
CHEMBL270722 Ki = 220.0 nM 6.66
CHEMBL376505 Ki = 300.0 nM 6.52
CHEMBL31574 FISETIN IC50 = 350.0 nM 6.46
CHEMBL270722 IC50 = 370.0 nM 6.43
CHEMBL150 KAEMPFEROL IC50 = 400.0 nM 6.40
CHEMBL177820 TETRABROMOBENZOTRIAZOLE Ki = 400.0 nM 6.40
CHEMBL376505 IC50 = 500.0 nM 6.30
CHEMBL151 LUTEOLIN IC50 = 500.0 nM 6.30
CHEMBL50 QUERCETIN IC50 = 550.0 nM 6.26
CHEMBL28 APIGENIN IC50 = 800.0 nM 6.10
CHEMBL164 MYRICETIN IC50 = 920.0 nM 6.04
CHEMBL177820 TETRABROMOBENZOTRIAZOLE IC50 = 1600.0 nM 5.80
CHEMBL117 CHRYSIN IC50 = 9000.0 nM 5.05
CHEMBL28626 MORIN IC50 = 10000.0 nM 5.00
CHEMBL8260 BAICALEIN IC50 = 10000.0 nM 5.00
CHEMBL44 GENISTEIN IC50 = 32000.0 nM 4.50