Assay Detail
Binding
CHEMBL4768882
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Inhibition of recombinant human CK2alpha (1 to 336 residues) expressed in Escherichia coli BL21 (DE3) using RRADDSDDDD as substrate incubated for 10 mins in presence of [gamma-33P]-ATP by scintillation counting assay
16
Total Activities
16
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
A novel class of selective CK2 inhibitors targeting its open hinge conformation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 6.52 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1230165 | SILMITASERTIB | 2.0 | 1 | 9.00 |
| CHEMBL4795023 | — | — | 1 | 6.55 |
| CHEMBL4784643 | — | — | 1 | 6.50 |
| CHEMBL4776391 | — | — | 1 | 6.48 |
| CHEMBL4778120 | — | — | 1 | 6.44 |
| CHEMBL4798710 | — | — | 1 | 6.43 |
| CHEMBL4789806 | — | — | 1 | 6.43 |
| CHEMBL4070389 | — | — | 1 | 6.43 |
| CHEMBL4783065 | — | — | 1 | 6.15 |
| CHEMBL4799521 | — | — | 1 | 6.06 |
| CHEMBL4796675 | — | — | 1 | 5.89 |
| CHEMBL4792639 | — | — | 1 | 5.86 |
| CHEMBL4785453 | — | — | 1 | - |
| CHEMBL4781256 | — | — | 1 | - |
| CHEMBL4788189 | — | — | 1 | - |
| CHEMBL4795570 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1230165 | SILMITASERTIB | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4795023 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4784643 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL4776391 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL4778120 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL4798710 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL4789806 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL4070389 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL4783065 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL4799521 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL4796675 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4792639 | — | IC50 | = | 1370.0 | nM | 5.86 |
| CHEMBL4785453 | — | IC50 | - | — | - | |
| CHEMBL4781256 | — | IC50 | - | — | - | |
| CHEMBL4788189 | — | IC50 | - | — | - | |
| CHEMBL4795570 | — | IC50 | - | — | - |