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Assay Detail

CHEMBL4184342

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

Binding
Inhibition of recombinant human full length His-tagged CaMK2delta expressed in baculovirus using Biotin labelled STK1 as substrate after 1 hr in presence of ATP by fluorescence assay
36
Total Activities
36
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 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
IC50 36 8.31 10.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4218769 1 10.30
CHEMBL4208018 1 10.22
CHEMBL4215817 1 10.15
CHEMBL4218245 1 10.10
CHEMBL4217261 1 10.05
CHEMBL4210359 1 10.00
CHEMBL4215300 1 10.00
CHEMBL4206514 1 10.00
CHEMBL4209816 1 9.66
CHEMBL4213838 1 9.64
CHEMBL4210881 1 9.55
CHEMBL4205997 1 9.52
CHEMBL4209443 1 9.04
CHEMBL4205708 1 8.80
CHEMBL4211430 1 8.66
CHEMBL4213305 1 8.48
CHEMBL4209840 1 8.47
CHEMBL4210568 1 8.46
CHEMBL4208717 1 8.40
CHEMBL4216080 1 8.24
CHEMBL4213540 1 8.14
CHEMBL4214345 1 8.04
CHEMBL4215541 1 7.43
CHEMBL4211934 1 7.39
CHEMBL4210073 1 7.36
CHEMBL4209789 1 7.28
CHEMBL4205405 1 7.24
CHEMBL4209139 1 7.19
CHEMBL4204410 1 6.90
CHEMBL4218994 1 6.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4218769 IC50 = 0.05 nM 10.30
CHEMBL4208018 IC50 = 0.06 nM 10.22
CHEMBL4215817 IC50 = 0.07 nM 10.15
CHEMBL4218245 IC50 = 0.08 nM 10.10
CHEMBL4217261 IC50 = 0.09 nM 10.05
CHEMBL4210359 IC50 = 0.1 nM 10.00
CHEMBL4215300 IC50 = 0.1 nM 10.00
CHEMBL4206514 IC50 = 0.1 nM 10.00
CHEMBL4209816 IC50 = 0.22 nM 9.66
CHEMBL4213838 IC50 = 0.23 nM 9.64
CHEMBL4210881 IC50 = 0.28 nM 9.55
CHEMBL4205997 IC50 = 0.3 nM 9.52
CHEMBL4209443 IC50 = 0.92 nM 9.04
CHEMBL4205708 IC50 = 1.6 nM 8.80
CHEMBL4211430 IC50 = 2.17 nM 8.66
CHEMBL4213305 IC50 = 3.3 nM 8.48
CHEMBL4209840 IC50 = 3.4 nM 8.47
CHEMBL4210568 IC50 = 3.5 nM 8.46
CHEMBL4208717 IC50 = 4.0 nM 8.40
CHEMBL4216080 IC50 = 5.8 nM 8.24
CHEMBL4213540 IC50 = 7.2 nM 8.14
CHEMBL4214345 IC50 = 9.1 nM 8.04
CHEMBL4215541 IC50 = 37.0 nM 7.43
CHEMBL4211934 IC50 = 41.0 nM 7.39
CHEMBL4210073 IC50 = 44.0 nM 7.36
CHEMBL4209789 IC50 = 53.0 nM 7.28
CHEMBL4205405 IC50 = 57.0 nM 7.24
CHEMBL4209139 IC50 = 65.0 nM 7.19
CHEMBL4204410 IC50 = 125.0 nM 6.90
CHEMBL4218994 IC50 = 191.0 nM 6.72
CHEMBL4214991 IC50 = 245.0 nM 6.61
CHEMBL4215635 IC50 = 254.0 nM 6.59
CHEMBL4207271 IC50 = 325.0 nM 6.49
CHEMBL4211112 IC50 = 454.0 nM 6.34
CHEMBL4205811 IC50 = 474.0 nM 6.32
CHEMBL4211047 IC50 = 4436.0 nM 5.35