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Assay Detail

CHEMBL5166487

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

Binding
Binding affinity to recombinant human CaMK2alpha Phe467Met mutant expressed in Escherichia coli BL21 DE3 assessed as dissociation constant by surface plasmon resonance assay
4
Total Activities
4
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

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
Kd 4 6.49 6.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5191835 1 6.66
CHEMBL5196669 1 6.66
CHEMBL5181927 1 6.45
CHEMBL5198167 1 6.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5191835 Kd = 219.0 nM 6.66
CHEMBL5196669 Kd = 219.0 nM 6.66
CHEMBL5181927 Kd = 353.0 nM 6.45
CHEMBL5198167 Kd = 670.0 nM 6.17