Assay Detail
Binding
CHEMBL3865666
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Inhibition of GST-tagged full length human SYK (1 to 635 end residues) expressed in baculovirus expression system preincubated for 10 mins followed by Blk/Lyntide substrate and ATP addition measured after 45 mins TR-FRET assay
11
Total Activities
11
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
Carboxamide Spleen Tyrosine Kinase (Syk) Inhibitors: Leveraging Ground State Interactions To Accelerate Optimization.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 7.89 | 10.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3415583 | — | — | 1 | 10.22 |
| CHEMBL3414584 | — | — | 1 | 9.30 |
| CHEMBL3415610 | — | — | 1 | 9.15 |
| CHEMBL3951922 | — | — | 1 | 8.30 |
| CHEMBL3943181 | — | — | 1 | 8.15 |
| CHEMBL3961713 | — | — | 1 | 8.05 |
| CHEMBL3934210 | — | — | 1 | 7.62 |
| CHEMBL3972739 | — | — | 1 | 6.28 |
| CHEMBL3925317 | — | — | 1 | 6.00 |
| CHEMBL3935657 | — | — | 1 | 5.80 |
| CHEMBL3963092 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3415583 | — | IC50 | = | 0.06 | nM | 10.22 |
| CHEMBL3414584 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3415610 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL3951922 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3943181 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3961713 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3934210 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3972739 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL3925317 | — | IC50 | = | 990.0 | nM | 6.00 |
| CHEMBL3935657 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL3963092 | — | IC50 | > | 10000.0 | nM | - |