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Assay Detail

CHEMBL5166511

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Binding
Inhibition of [3H]NCS-382 binding to CaMK2alpha in rat cerebrocortical membranes
4
Total Activities
2
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Cerebral cortex
Subcellular Membrane
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
IC50 2 9.29 9.89
Ki 2 6.30 6.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL190035 3-Hydroxyphenylacetate 2 9.89
CHEMBL240714 2 8.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL190035 3-Hydroxyphenylacetate IC50 = 0.13 nM 9.89
CHEMBL240714 IC50 = 2.1 nM 8.68
CHEMBL190035 3-Hydroxyphenylacetate Ki = 125.89 nM 6.90
CHEMBL240714 Ki = 1995.26 nM 5.70