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Assay Detail

CHEMBL1937305

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

Binding
Inhibition of human recombinant CK2alpha/CK2beta using RRRDDDSDDD peptide as substrate by radiometric assay
38
Total Activities
37
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Casein kinase II alpha'/ beta (CHEMBL3883328)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Synthesis and SAR of inhibitors of protein kinase CK2: novel tricyclic quinoline analogs.
Haddach M, Pierre F, Regan CF, Borsan C, Michaux J, Stefan E, Kerdoncuff P, Schwaebe MK, Chua PC, Siddiqui-Jain A, Macalino D, Drygin D, O'Brien SE, Rice WG, Ryckman DM.
Bioorg Med Chem Lett (2012) 22 : 45 -48
PubMed 22169261 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 37 8.18 9.52
Ki 1 9.66 9.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1230165 SILMITASERTIB 2.0 2 9.66
CHEMBL1934184 1 9.40
CHEMBL1934182 1 9.30
CHEMBL1934181 1 9.30
CHEMBL1934172 1 9.30
CHEMBL1934180 1 9.22
CHEMBL1934318 1 9.00
CHEMBL1934166 1 9.00
CHEMBL1934160 1 8.96
CHEMBL1934173 1 8.92
CHEMBL1934164 1 8.89
CHEMBL1934319 1 8.68
CHEMBL1934165 1 8.57
CHEMBL1934163 1 8.54
CHEMBL1934171 1 8.46
CHEMBL1934178 1 8.46
CHEMBL1934193 1 8.43
CHEMBL1934183 1 8.38
CHEMBL1934168 1 8.24
CHEMBL1934192 1 8.05
CHEMBL1934170 1 7.96
CHEMBL1934177 1 7.92
CHEMBL1934169 1 7.89
CHEMBL1934176 1 7.82
CHEMBL1934179 1 7.77
CHEMBL1934174 1 7.70
CHEMBL1934189 1 7.70
CHEMBL1934186 1 7.52
CHEMBL1934167 1 7.47
CHEMBL1934162 1 7.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1230165 SILMITASERTIB Ki = 0.22 nM 9.66
CHEMBL1230165 SILMITASERTIB IC50 = 0.3 nM 9.52
CHEMBL1934184 IC50 = 0.4 nM 9.40
CHEMBL1934182 IC50 = 0.5 nM 9.30
CHEMBL1934181 IC50 = 0.5 nM 9.30
CHEMBL1934172 IC50 = 0.5 nM 9.30
CHEMBL1934180 IC50 = 0.6 nM 9.22
CHEMBL1934166 IC50 = 1.0 nM 9.00
CHEMBL1934318 IC50 = 1.0 nM 9.00
CHEMBL1934160 IC50 = 1.1 nM 8.96
CHEMBL1934173 IC50 = 1.2 nM 8.92
CHEMBL1934164 IC50 = 1.3 nM 8.89
CHEMBL1934319 IC50 = 2.1 nM 8.68
CHEMBL1934165 IC50 = 2.7 nM 8.57
CHEMBL1934163 IC50 = 2.9 nM 8.54
CHEMBL1934171 IC50 = 3.5 nM 8.46
CHEMBL1934178 IC50 = 3.5 nM 8.46
CHEMBL1934193 IC50 = 3.7 nM 8.43
CHEMBL1934183 IC50 = 4.2 nM 8.38
CHEMBL1934168 IC50 = 5.7 nM 8.24
CHEMBL1934192 IC50 = 8.9 nM 8.05
CHEMBL1934170 IC50 = 11.0 nM 7.96
CHEMBL1934177 IC50 = 12.0 nM 7.92
CHEMBL1934169 IC50 = 13.0 nM 7.89
CHEMBL1934176 IC50 = 15.0 nM 7.82
CHEMBL1934179 IC50 = 17.0 nM 7.77
CHEMBL1934189 IC50 = 20.0 nM 7.70
CHEMBL1934174 IC50 = 20.0 nM 7.70
CHEMBL1934186 IC50 = 30.0 nM 7.52
CHEMBL1934167 IC50 = 34.0 nM 7.47
CHEMBL1934162 IC50 = 35.0 nM 7.46
CHEMBL1934175 IC50 = 39.0 nM 7.41
CHEMBL1934190 IC50 = 164.0 nM 6.79
CHEMBL1934185 IC50 = 395.0 nM 6.40
CHEMBL1934187 IC50 = 444.0 nM 6.35
CHEMBL1934191 IC50 = 2025.0 nM 5.69
CHEMBL1934188 IC50 > 2500.0 nM -
CHEMBL1934161 IC50 > 2500.0 nM -