Assay Detail
Binding
CHEMBL4222674
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Inhibition of CK2alpha in human HCT116 or human DLD1 cells assessed as decrease in AKT phosphorylation at S129 residue after 3 to 24 hrs by Western blot method
9
Total Activities
9
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 2,6-disubstituted pyrazine derivatives as inhibitors of CK2 and PIM kinases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 6.20 | 7.02 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4225287 | — | — | 1 | 7.02 |
| CHEMBL4228654 | — | — | 1 | 6.96 |
| CHEMBL4224859 | — | — | 1 | 6.75 |
| CHEMBL4227817 | — | — | 1 | 6.47 |
| CHEMBL4228363 | — | — | 1 | 6.00 |
| CHEMBL1231683 | — | — | 1 | 5.57 |
| CHEMBL4227886 | — | — | 1 | 5.47 |
| CHEMBL4225224 | — | — | 1 | 5.37 |
| CHEMBL4228394 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4225287 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL4228654 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4224859 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4227817 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL4228363 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL1231683 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL4227886 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL4225224 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL4228394 | — | IC50 | > | 3300.0 | nM | - |