Assay Detail
Binding
CHEMBL992587
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Inhibition of human Syk expressed in Sf9 cells
19
Total Activities
19
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
Structure-activity relationship studies of imidazo[1,2-c]pyrimidine derivatives as potent and orally effective Syk family kinases inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 6.92 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL388978 | STAUROSPORINE | — | 1 | 8.52 |
| CHEMBL475575 | — | — | 1 | 8.40 |
| CHEMBL459146 | — | — | 1 | 8.22 |
| CHEMBL485204 | — | — | 1 | 8.22 |
| CHEMBL475609 | — | — | 1 | 8.05 |
| CHEMBL459147 | — | — | 1 | 7.55 |
| CHEMBL458973 | — | — | 1 | 7.52 |
| CHEMBL515054 | — | — | 1 | 7.52 |
| CHEMBL457519 | — | — | 1 | 7.04 |
| CHEMBL482175 | — | — | 1 | 6.64 |
| CHEMBL511977 | — | — | 1 | 6.42 |
| CHEMBL484350 | — | — | 1 | 6.14 |
| CHEMBL458806 | — | — | 1 | 6.08 |
| CHEMBL475180 | — | — | 1 | 6.00 |
| CHEMBL520842 | — | — | 1 | 5.92 |
| CHEMBL520669 | — | — | 1 | 5.82 |
| CHEMBL519131 | — | — | 1 | 5.37 |
| CHEMBL481973 | — | — | 1 | 5.15 |
| CHEMBL458788 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL388978 | STAUROSPORINE | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL475575 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL459146 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL485204 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL475609 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL459147 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL458973 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL515054 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL457519 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL482175 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL511977 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL484350 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL458806 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL475180 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL520842 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL520669 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL519131 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL481973 | — | IC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL458788 | — | IC50 | > | 10000.0 | nM | - |