Assay Detail
Binding
CHEMBL2328037
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Inhibition of recombinant RSK2 (unknown origin) expressed in baculovirus infected Sf9 cells assessed as decrease in substrate phosphorylation using GST-fusion protein containing ERalpha-Ser167 sequence-RLASTND as substrate by chemiluminescence analysis
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Improving the affinity of SL0101 for RSK using structure-based design.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 6.22 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2321925 | — | — | 1 | 7.70 |
| CHEMBL2326706 | — | — | 1 | 6.32 |
| CHEMBL2326708 | — | — | 1 | 6.21 |
| CHEMBL2326705 | — | — | 1 | 6.15 |
| CHEMBL240954 | — | — | 1 | 6.00 |
| CHEMBL2326707 | — | — | 1 | 5.82 |
| CHEMBL2326704 | — | — | 1 | 5.82 |
| CHEMBL2326709 | — | — | 1 | 5.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2321925 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2326706 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL2326708 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL2326705 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL240954 | — | IC50 | = | 990.0 | nM | 6.00 |
| CHEMBL2326707 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL2326704 | — | IC50 | = | 1510.0 | nM | 5.82 |
| CHEMBL2326709 | — | IC50 | = | 1770.0 | nM | 5.75 |