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Assay Detail

CHEMBL5166512

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Binding
Inhibition of [3H]NCS-382 binding to CaMK2alpha (unknown origin)
8
Total Activities
6
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
Ki 8 5.93 7.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5175277 1 7.46
CHEMBL1772 2 5.70
CHEMBL1030 4'-HYDROXY-DICLOFENAC 2 5.70
CHEMBL1342 OXYBATE 4.0 1 5.37
CHEMBL27246 CINNAMIC ACID 1 -
CHEMBL66879 COUMARIC ACID 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5175277 Ki = 35.0 nM 7.46
CHEMBL1772 Ki = 1995.26 nM 5.70
CHEMBL1030 4'-HYDROXY-DICLOFENAC Ki = 1995.26 nM 5.70
CHEMBL1030 4'-HYDROXY-DICLOFENAC Ki = 2100.0 nM 5.68
CHEMBL1772 Ki = 2200.0 nM 5.66
CHEMBL1342 OXYBATE Ki = 4300.0 nM 5.37
CHEMBL27246 CINNAMIC ACID Ki > 100000.0 nM -
CHEMBL66879 COUMARIC ACID Ki > 100000.0 nM -