Assay Detail
Binding
CHEMBL3783584
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Inhibition of N-terminal His6 tagged full-length human recombinant active RSK2 using S6 peptide after 20 mins by fluorescence assay
25
Total Activities
25
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
Isoindole-1,3-dione derivatives as RSK2 inhibitors: synthesis, molecular docking simulation and SAR analysis
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 5.91 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6291 | BISINDOLYLMALEIMIDE IX | — | 1 | 8.00 |
| CHEMBL3781731 | — | — | 1 | 6.33 |
| CHEMBL3779994 | — | — | 1 | 6.28 |
| CHEMBL3780594 | — | — | 1 | 6.23 |
| CHEMBL3780949 | — | — | 1 | 6.23 |
| CHEMBL1775068 | — | — | 1 | 6.10 |
| CHEMBL3781117 | — | — | 1 | 6.07 |
| CHEMBL3781068 | — | — | 1 | 6.00 |
| CHEMBL3780363 | — | — | 1 | 6.00 |
| CHEMBL3781355 | — | — | 1 | 5.87 |
| CHEMBL3780464 | — | — | 1 | 5.67 |
| CHEMBL3780942 | — | — | 1 | 5.55 |
| CHEMBL3780055 | — | — | 1 | 5.46 |
| CHEMBL3780920 | — | — | 1 | 5.45 |
| CHEMBL3781064 | — | — | 1 | 5.37 |
| CHEMBL3781760 | — | — | 1 | 5.37 |
| CHEMBL3781690 | — | — | 1 | 5.34 |
| CHEMBL3780781 | — | — | 1 | 5.06 |
| CHEMBL3781291 | — | — | 1 | - |
| CHEMBL38326 | — | — | 1 | - |
| CHEMBL3780859 | — | — | 1 | - |
| CHEMBL3780433 | — | — | 1 | - |
| CHEMBL3781611 | — | — | 1 | - |
| CHEMBL3781591 | — | — | 1 | - |
| CHEMBL3780618 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6291 | BISINDOLYLMALEIMIDE IX | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3781731 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL3779994 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL3780594 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL3780949 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL1775068 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL3781117 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL3781068 | — | IC50 | = | 1010.0 | nM | 6.00 |
| CHEMBL3780363 | — | IC50 | = | 990.0 | nM | 6.00 |
| CHEMBL3781355 | — | IC50 | = | 1340.0 | nM | 5.87 |
| CHEMBL3780464 | — | IC50 | = | 2160.0 | nM | 5.67 |
| CHEMBL3780942 | — | IC50 | = | 2830.0 | nM | 5.55 |
| CHEMBL3780055 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL3780920 | — | IC50 | = | 3530.0 | nM | 5.45 |
| CHEMBL3781064 | — | IC50 | = | 4310.0 | nM | 5.37 |
| CHEMBL3781760 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL3781690 | — | IC50 | = | 4580.0 | nM | 5.34 |
| CHEMBL3780781 | — | IC50 | = | 8740.0 | nM | 5.06 |
| CHEMBL3781291 | — | IC50 | - | — | - | |
| CHEMBL38326 | — | IC50 | - | — | - | |
| CHEMBL3780859 | — | IC50 | - | — | - | |
| CHEMBL3780433 | — | IC50 | - | — | - | |
| CHEMBL3781611 | — | IC50 | - | — | - | |
| CHEMBL3781591 | — | IC50 | - | — | - | |
| CHEMBL3780618 | — | IC50 | - | — | - |