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Assay Detail

CHEMBL5166479

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

Binding
Displacement of [3H]HOCPCA from recombinant full length CaMK2alpha (unknown origin) expressed in HEK293 cell homogenates assessed as inhibition constant measured after 60 mins by liquid scintillation counting method
3
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Discovery and Optimization of 5-Hydroxy-Diclofenac toward a New Class of Ligands with Nanomolar Affinity for the CaMKIIα Hub Domain.
Tian Y, Shehata MA, Gauger SJ, Ng CKL, Solbak S, Thiesen L, Bruus-Jensen J, Krall J, Bundgaard C, Gibson KM, Wellendorph P, Frølund B.
J Med Chem (2022) 65 : 6656 -6676
PubMed 35500061 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 6.23 6.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5191835 2 6.30
CHEMBL5175277 1 6.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5191835 Ki = 500.0 nM 6.30
CHEMBL5191835 Ki = 501.19 nM 6.30
CHEMBL5175277 Ki = 800.0 nM 6.10