Assay Detail
Binding
CHEMBL1936698
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Inhibition of human RSK2-mediated CREB phosphorylation in HLR-CREB cells by cell based assay
21
Total Activities
21
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
Indole RSK inhibitors. Part 2: optimization of cell potency and kinase selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 6.76 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1933288 | — | — | 1 | 7.70 |
| CHEMBL1933280 | — | — | 1 | 7.40 |
| CHEMBL1933287 | — | — | 1 | 7.10 |
| CHEMBL1933278 | — | — | 1 | 7.05 |
| CHEMBL1933285 | — | — | 1 | 7.05 |
| CHEMBL1933289 | — | — | 1 | 7.00 |
| CHEMBL1933149 | — | — | 1 | 6.92 |
| CHEMBL1933147 | — | — | 1 | 6.89 |
| CHEMBL1933284 | — | — | 1 | 6.89 |
| CHEMBL1933286 | — | — | 1 | 6.80 |
| CHEMBL1933281 | — | — | 1 | 6.75 |
| CHEMBL1933143 | — | — | 1 | 6.70 |
| CHEMBL1933279 | — | — | 1 | 6.70 |
| CHEMBL1933283 | — | — | 1 | 6.70 |
| CHEMBL1933068 | — | — | 1 | 6.60 |
| CHEMBL1933290 | — | — | 1 | 6.54 |
| CHEMBL1933146 | — | — | 1 | 6.44 |
| CHEMBL1933277 | — | — | 1 | 6.34 |
| CHEMBL1933145 | — | — | 1 | 6.34 |
| CHEMBL1933148 | — | — | 1 | 6.10 |
| CHEMBL1933282 | — | — | 1 | 6.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1933288 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1933280 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL1933287 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL1933278 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL1933285 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL1933289 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL1933149 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL1933147 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL1933284 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL1933286 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL1933281 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL1933143 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL1933279 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL1933283 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL1933068 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL1933290 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL1933146 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL1933277 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL1933145 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL1933148 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL1933282 | — | IC50 | = | 1000.0 | nM | 6.00 |