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Assay Detail

CHEMBL5729945

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Binding
Kinase Assay: The effectiveness of compounds of the present invention as inhibitors of protein kinases can be readily tested by assays known to those skilled in the art. For example, in vitro protein kinase assays may be conducted with a relevant purified protein kinase and an appropriate synthetic substrate to determine the inhibitory activity of the compounds. Assays for inhibition of CK2 by the instant compounds were performed in 384-well plates with reaction mixtures containing 10 uM of peptide substrate (RRRADDSDDDDD-NH2), [gamma-33P]ATP (10 uCi) at 25 uM (CK2A1) or 5 uM (CK2A2), 20 mM Hepes (pH 7.4), 100 mM NaCl, 10 mM MgCl2, 0.25 mM dithiothreitol, Brij-35 at 0.015%, and recombinant CK2A1 (10 nM, Invitrogen) or CK2A2 (5 nM, Upstate Biotechnology). Reaction mixtures were incubated at 30 C. for 1 hour, and reaction products were captured by binding to phosphocellulose (P81) filter plates.
ChEMBL ↗
213
Total Activities
71
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Casein kinase II subunit alpha (CHEMBL3629) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Imidazotriazinecarbonitriles useful as kinase inhibitors
(2015)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 71 8.75 9.89
kon 71 - -
k_off 71 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3699289 — — 3 9.89
CHEMBL3699277 — — 3 9.85
CHEMBL3699234 — — 3 9.82
CHEMBL3699295 — — 3 9.80
CHEMBL3699235 — — 3 9.77
CHEMBL3699266 — — 3 9.68
CHEMBL3699253 — — 3 9.68
CHEMBL3699244 — — 3 9.66
CHEMBL3699292 — — 3 9.66
CHEMBL3699237 — — 3 9.64
CHEMBL3699294 — — 3 9.64
CHEMBL3699252 — — 3 9.62
CHEMBL3699276 — — 3 9.57
CHEMBL3699291 — — 3 9.57
CHEMBL3699254 — — 3 9.57
CHEMBL3699280 — — 3 9.55
CHEMBL3699278 — — 3 9.54
CHEMBL3699238 — — 3 9.54
CHEMBL3699250 — — 3 9.52
CHEMBL3699239 — — 3 9.52
CHEMBL3699255 — — 3 9.52
CHEMBL3699262 — — 3 9.51
CHEMBL3699287 — — 3 9.41
CHEMBL3699256 — — 3 9.39
CHEMBL3699282 — — 3 9.28
CHEMBL3699257 — — 3 9.14
CHEMBL3699297 — — 3 8.88
CHEMBL3699285 — — 3 8.88
CHEMBL3699251 — — 3 8.88
CHEMBL3699259 — — 3 8.87

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3699289 — IC50 = 0.13 nM 9.89
CHEMBL3699277 — IC50 = 0.14 nM 9.85
CHEMBL3699234 — IC50 = 0.15 nM 9.82
CHEMBL3699295 — IC50 = 0.16 nM 9.80
CHEMBL3699235 — IC50 = 0.17 nM 9.77
CHEMBL3699253 — IC50 = 0.21 nM 9.68
CHEMBL3699266 — IC50 = 0.21 nM 9.68
CHEMBL3699292 — IC50 = 0.22 nM 9.66
CHEMBL3699244 — IC50 = 0.22 nM 9.66
CHEMBL3699294 — IC50 = 0.23 nM 9.64
CHEMBL3699237 — IC50 = 0.23 nM 9.64
CHEMBL3699252 — IC50 = 0.24 nM 9.62
CHEMBL3699291 — IC50 = 0.27 nM 9.57
CHEMBL3699254 — IC50 = 0.27 nM 9.57
CHEMBL3699276 — IC50 = 0.27 nM 9.57
CHEMBL3699280 — IC50 = 0.28 nM 9.55
CHEMBL3699278 — IC50 = 0.29 nM 9.54
CHEMBL3699238 — IC50 = 0.29 nM 9.54
CHEMBL3699250 — IC50 = 0.3 nM 9.52
CHEMBL3699239 — IC50 = 0.3 nM 9.52
CHEMBL3699255 — IC50 = 0.3 nM 9.52
CHEMBL3699262 — IC50 = 0.31 nM 9.51
CHEMBL3699287 — IC50 = 0.39 nM 9.41
CHEMBL3699256 — IC50 = 0.41 nM 9.39
CHEMBL3699282 — IC50 = 0.52 nM 9.28
CHEMBL3699257 — IC50 = 0.72 nM 9.14
CHEMBL3699285 — IC50 = 1.33 nM 8.88
CHEMBL3699297 — IC50 = 1.32 nM 8.88
CHEMBL3699251 — IC50 = 1.31 nM 8.88
CHEMBL3699267 — IC50 = 1.35 nM 8.87
CHEMBL3699259 — IC50 = 1.36 nM 8.87
CHEMBL3699264 — IC50 = 1.34 nM 8.87
CHEMBL3699240 — IC50 = 1.35 nM 8.87
CHEMBL3699296 — IC50 = 1.39 nM 8.86
CHEMBL3699303 — IC50 = 1.39 nM 8.86
CHEMBL3699286 — IC50 = 1.37 nM 8.86
CHEMBL3699260 — IC50 = 1.37 nM 8.86
CHEMBL3699242 — IC50 = 1.37 nM 8.86
CHEMBL3699284 — IC50 = 1.42 nM 8.85
CHEMBL3699279 — IC50 = 1.4 nM 8.85
CHEMBL3699236 — IC50 = 1.4 nM 8.85
CHEMBL3699274 — IC50 = 1.42 nM 8.85
CHEMBL3699293 — IC50 = 1.44 nM 8.84
CHEMBL3699241 — IC50 = 1.44 nM 8.84
CHEMBL3699269 — IC50 = 1.5 nM 8.82
CHEMBL3699245 — IC50 = 1.56 nM 8.81
CHEMBL3699258 — IC50 = 1.53 nM 8.81
CHEMBL3699268 — IC50 = 3.83 nM 8.42
CHEMBL3699281 — IC50 = 4.71 nM 8.33
CHEMBL3699265 — IC50 = 5.87 nM 8.23