Assay Detail
Binding
CHEMBL3760461
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Inhibition of GST-tagged human CK2alpha' (1 to 350 residues) using CK2tide as substrate incubated for 1 hr by off-chip mobility shift assay
18
Total Activities
18
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
Structure-activity relationship study of 4-(thiazol-5-yl)benzoic acid derivatives as potent protein kinase CK2 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.83 | 8.34 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3760043 | — | — | 1 | 8.34 |
| CHEMBL3759871 | — | — | 1 | 8.06 |
| CHEMBL3758606 | — | — | 1 | 8.02 |
| CHEMBL3758317 | — | — | 1 | 8.02 |
| CHEMBL3759512 | — | — | 1 | 8.01 |
| CHEMBL3759755 | — | — | 1 | 8.00 |
| CHEMBL3758519 | — | — | 1 | 8.00 |
| CHEMBL1230165 | SILMITASERTIB | 2.0 | 1 | 7.96 |
| CHEMBL2087023 | — | — | 1 | 7.96 |
| CHEMBL3759349 | — | — | 1 | 7.96 |
| CHEMBL3760009 | — | — | 1 | 7.96 |
| CHEMBL3760064 | — | — | 1 | 7.92 |
| CHEMBL3758270 | — | — | 1 | 7.92 |
| CHEMBL3758895 | — | — | 1 | 7.89 |
| CHEMBL3758777 | — | — | 1 | 7.85 |
| CHEMBL3759193 | — | — | 1 | 7.72 |
| CHEMBL3759388 | — | — | 1 | 6.80 |
| CHEMBL3758475 | — | — | 1 | 6.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3760043 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL3759871 | — | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL3758606 | — | IC50 | = | 9.5 | nM | 8.02 |
| CHEMBL3758317 | — | IC50 | = | 9.6 | nM | 8.02 |
| CHEMBL3759512 | — | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL3759755 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3758519 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1230165 | SILMITASERTIB | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2087023 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3759349 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3760009 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3760064 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3758270 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3758895 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3758777 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3759193 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3759388 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL3758475 | — | IC50 | = | 280.0 | nM | 6.55 |