Assay Detail
Binding
CHEMBL1663323
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Inhibition of human recombinant CK2 assessed as inhibition of [gamma33P]ATP incorporation into substrate by luminescence assay
68
Total Activities
68
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 68 | 7.28 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1652710 | — | — | 1 | 9.00 |
| CHEMBL1230165 | SILMITASERTIB | 2.0 | 1 | 9.00 |
| CHEMBL1652704 | — | — | 1 | 8.52 |
| CHEMBL1652738 | — | — | 1 | 8.52 |
| CHEMBL1652706 | — | — | 1 | 8.40 |
| CHEMBL1652707 | — | — | 1 | 8.40 |
| CHEMBL1652739 | — | — | 1 | 8.40 |
| CHEMBL1652708 | — | — | 1 | 8.30 |
| CHEMBL1652697 | — | — | 1 | 8.22 |
| CHEMBL1649763 | — | — | 1 | 8.22 |
| CHEMBL1652737 | — | — | 1 | 8.15 |
| CHEMBL1652700 | — | — | 1 | 8.10 |
| CHEMBL1652709 | — | — | 1 | 8.10 |
| CHEMBL1652703 | — | — | 1 | 8.05 |
| CHEMBL1652702 | — | — | 1 | 7.96 |
| CHEMBL1652705 | — | — | 1 | 7.80 |
| CHEMBL1652701 | — | — | 1 | 7.80 |
| CHEMBL1652741 | — | — | 1 | 7.72 |
| CHEMBL1652698 | — | — | 1 | 7.60 |
| CHEMBL1652699 | — | — | 1 | 7.57 |
| CHEMBL1652734 | — | — | 1 | 7.55 |
| CHEMBL1652732 | — | — | 1 | 7.50 |
| CHEMBL1652742 | — | — | 1 | 7.37 |
| CHEMBL1652730 | — | — | 1 | 7.17 |
| CHEMBL1649770 | — | — | 1 | 7.16 |
| CHEMBL1652740 | — | — | 1 | 7.16 |
| CHEMBL1649614 | — | — | 1 | 7.12 |
| CHEMBL1652733 | — | — | 1 | 7.11 |
| CHEMBL92361 | — | — | 1 | 7.10 |
| CHEMBL1652720 | — | — | 1 | 7.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1652710 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1230165 | SILMITASERTIB | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1652738 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1652704 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1652706 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1652707 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1652739 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1652708 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1652697 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL1649763 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL1652737 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1652700 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL1652709 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL1652703 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1652702 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1652705 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL1652701 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL1652741 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL1652698 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL1652699 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL1652734 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL1652732 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL1652742 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL1652730 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL1652740 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL1649770 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL1649614 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL1652733 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL92361 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL1652720 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL1652726 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL1652718 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL1652692 | — | IC50 | = | 129.0 | nM | 6.89 |
| CHEMBL1652736 | — | IC50 | = | 129.0 | nM | 6.89 |
| CHEMBL1652731 | — | IC50 | = | 178.0 | nM | 6.75 |
| CHEMBL1649769 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL1652729 | — | IC50 | = | 219.0 | nM | 6.66 |
| CHEMBL1649586 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL1652735 | — | IC50 | = | 395.0 | nM | 6.40 |
| CHEMBL1649761 | — | IC50 | = | 417.0 | nM | 6.38 |
| CHEMBL1652728 | — | IC50 | = | 516.0 | nM | 6.29 |
| CHEMBL1652716 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL1652722 | — | IC50 | = | 970.0 | nM | 6.01 |
| CHEMBL1652715 | — | IC50 | = | 990.0 | nM | 6.00 |
| CHEMBL1652721 | — | IC50 | = | 1070.0 | nM | 5.97 |
| CHEMBL1652717 | — | IC50 | = | 1260.0 | nM | 5.90 |
| CHEMBL1652714 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL1652719 | — | IC50 | = | 1780.0 | nM | 5.75 |
| CHEMBL1652711 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL1649764 | — | IC50 | > | 500.0 | nM | - |