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Assay Detail

CHEMBL4184427

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Binding
Inhibition of CaMK2alpha/beta in neonatal rat cortical neurons assessed as phospholamban phosphorylation after 4 hrs by Hoechst 33342 fluorescence-based assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

CaM kinase II alpha/beta (CHEMBL4296089)
Type PROTEIN COMPLEX
Organism Rattus norvegicus

Publication

Discovery of potent and selective inhibitors of calmodulin-dependent kinase II (CaMKII).
Koltun DO, Parkhill EQ, Kalla R, Perry TD, Elzein E, Li X, Simonovich SP, Ziebenhaus C, Hansen TR, Marchand B, Hung WK, Lagpacan L, Hung M, Aoyama RG, Murray BP, Perry JK, Somoza JR, Villaseñor AG, Pagratis N, Zablocki JA.
Bioorg Med Chem Lett (2018) 28 : 541 -546
PubMed 29254643 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 6.74 6.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4215300 1 6.92
CHEMBL4210359 1 6.56

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4215300 EC50 = 120.0 nM 6.92
CHEMBL4210359 EC50 = 274.0 nM 6.56