Assay Detail
Binding
CHEMBL4222671
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Inhibition of recombinant human full length N-terminal His6-tagged CK2alpha expressed in Sf21 insect cells using CK2tide as substrate treated for 20 mins measured after 90 mins in presence of MgCl2 by caliper mobility shift assay
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf21 |
| 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 | 31 | 6.75 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4225287 | — | — | 1 | 8.52 |
| CHEMBL4228654 | — | — | 1 | 8.30 |
| CHEMBL4227817 | — | — | 1 | 8.30 |
| CHEMBL4224859 | — | — | 1 | 8.15 |
| CHEMBL4228363 | — | — | 1 | 8.15 |
| CHEMBL2062563 | — | — | 1 | 8.00 |
| CHEMBL4227886 | — | — | 1 | 7.82 |
| CHEMBL4228394 | — | — | 1 | 7.58 |
| CHEMBL4224729 | — | — | 1 | 7.16 |
| CHEMBL4228242 | — | — | 1 | 7.00 |
| CHEMBL4227028 | — | — | 1 | 6.95 |
| CHEMBL4224959 | — | — | 1 | 6.89 |
| CHEMBL4225224 | — | — | 1 | 6.53 |
| CHEMBL4227791 | — | — | 1 | 6.51 |
| CHEMBL4226991 | — | — | 1 | 6.44 |
| CHEMBL4224693 | — | — | 1 | 6.44 |
| CHEMBL4225330 | — | — | 1 | 6.34 |
| CHEMBL4229169 | — | — | 1 | 6.25 |
| CHEMBL4224786 | — | — | 1 | 5.57 |
| CHEMBL4228074 | — | — | 1 | 5.34 |
| CHEMBL4227556 | — | — | 1 | 5.32 |
| CHEMBL4225896 | — | — | 1 | 4.89 |
| CHEMBL4225633 | — | — | 1 | 4.89 |
| CHEMBL4225206 | — | — | 1 | 4.70 |
| CHEMBL1230165 | SILMITASERTIB | 2.0 | 1 | - |
| CHEMBL2409175 | — | — | 1 | - |
| CHEMBL4229130 | — | — | 1 | - |
| CHEMBL2062585 | — | — | 1 | - |
| CHEMBL4228564 | — | — | 1 | - |
| CHEMBL4225046 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4225287 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4228654 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4227817 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4224859 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4228363 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL2062563 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4227886 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4228394 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4224729 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4228242 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4227028 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL4224959 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4225224 | — | IC50 | = | 297.0 | nM | 6.53 |
| CHEMBL4227791 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL4226991 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL4224693 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL4225330 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL4229169 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL4224786 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL4228074 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL4227556 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL4225896 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL4225633 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL4225206 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL1230165 | SILMITASERTIB | IC50 | < | 3.0 | nM | - |
| CHEMBL2409175 | — | IC50 | < | 3.0 | nM | - |
| CHEMBL4229130 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL2062585 | — | IC50 | < | 3.0 | nM | - |
| CHEMBL4228564 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4225046 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4225378 | — | IC50 | > | 30000.0 | nM | - |