Assay Detail
Binding
CHEMBL945314
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Inhibition of SYK-mediated FCepsilonRI signaling activity by mast cell degranulation assay
20
Total Activities
20
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Publication
Discovery and SAR of novel 4-thiazolyl-2-phenylaminopyrimidines as potent inhibitors of spleen tyrosine kinase (SYK).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 6.75 | 7.40 |
| Activity | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL511670 | — | — | 1 | 7.40 |
| CHEMBL511811 | — | — | 1 | 7.30 |
| CHEMBL512172 | — | — | 1 | 7.16 |
| CHEMBL472478 | — | — | 1 | 7.16 |
| CHEMBL485731 | — | — | 1 | 7.16 |
| CHEMBL471727 | — | — | 1 | 7.16 |
| CHEMBL475254 | — | — | 1 | 7.05 |
| CHEMBL485730 | — | — | 1 | 7.05 |
| CHEMBL471776 | — | — | 1 | 6.92 |
| CHEMBL471819 | — | — | 1 | 6.85 |
| CHEMBL475249 | — | — | 1 | 6.75 |
| CHEMBL486751 | — | — | 1 | 6.75 |
| CHEMBL470780 | — | — | 1 | 6.70 |
| CHEMBL451450 | — | — | 1 | 6.66 |
| CHEMBL470175 | — | — | 1 | 6.39 |
| CHEMBL512319 | — | — | 1 | 6.31 |
| CHEMBL509161 | — | — | 1 | 6.26 |
| CHEMBL453217 | — | — | 1 | 5.81 |
| CHEMBL473229 | — | — | 1 | 5.38 |
| CHEMBL475570 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL511670 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL511811 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL512172 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL472478 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL485731 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL471727 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL475254 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL485730 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL471776 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL471819 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL475249 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL486751 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL470780 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL451450 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL470175 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL512319 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL509161 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL453217 | — | IC50 | = | 1550.0 | nM | 5.81 |
| CHEMBL473229 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL475570 | — | Activity | - | — | - |