Assay Detail
Binding
CHEMBL4773120
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Inhibition of SYK (unknown origin) using poly(Glu, Tyr) 4:1 as substrate incubated in presence of [gamma33P]ATP by image analyser
6
Total Activities
6
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
Scaffold hopping of the SYK inhibitor entospletinib leads to broader targeting of the BCR signalosome.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 6.04 | 7.09 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3265032 | ENTOSPLETINIB | 3.0 | 1 | 7.09 |
| CHEMBL4785181 | — | — | 1 | 6.70 |
| CHEMBL4785298 | — | — | 1 | 6.52 |
| CHEMBL4784149 | — | — | 1 | 5.80 |
| CHEMBL4783559 | — | — | 1 | 5.09 |
| CHEMBL4781161 | — | — | 1 | 5.02 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3265032 | ENTOSPLETINIB | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL4785181 | — | IC50 | = | 201.0 | nM | 6.70 |
| CHEMBL4785298 | — | IC50 | = | 301.0 | nM | 6.52 |
| CHEMBL4784149 | — | IC50 | = | 1597.0 | nM | 5.80 |
| CHEMBL4783559 | — | IC50 | = | 8206.0 | nM | 5.09 |
| CHEMBL4781161 | — | IC50 | = | 9545.0 | nM | 5.02 |