Assay Detail
Binding
CHEMBL3381146
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Inhibition of human recombinant CK2a1/CK2b holoenzyme expressed in Escherichia coli BL21(DE3) pre-incubated for 10 mins before substrate addition by capillary electrophoresis based assay
20
Total Activities
20
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
Converting potent indeno[1,2-b]indole inhibitors of protein kinase CK2 into selective inhibitors of the breast cancer resistance protein ABCG2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 5.79 | 8.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1230165 | SILMITASERTIB | 2.0 | 1 | 8.43 |
| CHEMBL3353420 | — | — | 1 | 7.60 |
| CHEMBL6246 | ELLAGIC ACID | 2.0 | 1 | 7.40 |
| CHEMBL177820 | TETRABROMOBENZOTRIAZOLE | — | 1 | 7.22 |
| CHEMBL3353413 | — | — | 1 | 6.77 |
| CHEMBL1957190 | — | — | 1 | 6.44 |
| CHEMBL289277 | EMODIN | — | 1 | 6.24 |
| CHEMBL3353416 | — | — | 1 | 5.85 |
| CHEMBL3353414 | — | — | 1 | 5.60 |
| CHEMBL3353418 | — | — | 1 | 5.39 |
| CHEMBL3353417 | — | — | 1 | 5.29 |
| CHEMBL1957193 | — | — | 1 | 5.22 |
| CHEMBL1957192 | — | — | 1 | 5.16 |
| CHEMBL3353421 | — | — | 1 | 5.04 |
| CHEMBL3353422 | — | — | 1 | 4.96 |
| CHEMBL3353419 | — | — | 1 | 4.92 |
| CHEMBL1957191 | — | — | 1 | 4.82 |
| CHEMBL3353415 | — | — | 1 | 4.82 |
| CHEMBL1957203 | — | — | 1 | 4.46 |
| CHEMBL1957202 | — | — | 1 | 4.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1230165 | SILMITASERTIB | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL3353420 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL6246 | ELLAGIC ACID | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL177820 | TETRABROMOBENZOTRIAZOLE | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL3353413 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL1957190 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL289277 | EMODIN | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL3353416 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL3353414 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL3353418 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL3353417 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL1957193 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL1957192 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL3353421 | — | IC50 | = | 9200.0 | nM | 5.04 |
| CHEMBL3353422 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL3353419 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL1957191 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL3353415 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL1957203 | — | IC50 | = | 35000.0 | nM | 4.46 |
| CHEMBL1957202 | — | IC50 | = | 55000.0 | nM | 4.26 |