Assay Detail
Binding
CHEMBL3420413
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Inhibition of full-length GST-tagged human Syk preincubated for 10 mins followed by peptide substrate/ATP addition measured after 45 mins by TR-FRET assay
29
Total Activities
29
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
Overcoming mutagenicity and ion channel activity: optimization of selective spleen tyrosine kinase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 8.79 | 11.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3415598 | — | — | 1 | 11.00 |
| CHEMBL3415583 | — | — | 1 | 10.22 |
| CHEMBL3415606 | — | — | 1 | 10.00 |
| CHEMBL3415589 | — | — | 1 | 10.00 |
| CHEMBL3415594 | — | — | 1 | 10.00 |
| CHEMBL3415597 | — | — | 1 | 9.70 |
| CHEMBL3415604 | — | — | 1 | 9.40 |
| CHEMBL3414584 | — | — | 1 | 9.30 |
| CHEMBL3415587 | — | — | 1 | 9.30 |
| CHEMBL3415592 | — | — | 1 | 9.30 |
| CHEMBL3415599 | — | — | 1 | 9.22 |
| CHEMBL3415610 | — | — | 1 | 9.15 |
| CHEMBL3415588 | — | — | 1 | 9.10 |
| CHEMBL3415593 | — | — | 1 | 9.10 |
| CHEMBL3415595 | — | — | 1 | 9.05 |
| CHEMBL3415605 | — | — | 1 | 9.00 |
| CHEMBL3415607 | — | — | 1 | 8.70 |
| CHEMBL3415609 | — | — | 1 | 8.60 |
| CHEMBL3260318 | — | — | 1 | 8.55 |
| CHEMBL3415591 | — | — | 1 | 8.30 |
| CHEMBL3415585 | — | — | 1 | 8.15 |
| CHEMBL3415608 | — | — | 1 | 8.15 |
| CHEMBL3415584 | — | — | 1 | 8.06 |
| CHEMBL3415596 | — | — | 1 | 8.05 |
| CHEMBL3415582 | — | — | 1 | 7.72 |
| CHEMBL3415602 | — | — | 1 | 7.29 |
| CHEMBL3415603 | — | — | 1 | 7.22 |
| CHEMBL3415590 | — | — | 1 | 6.74 |
| CHEMBL3415586 | — | — | 1 | 6.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3415598 | — | IC50 | = | 0.01 | nM | 11.00 |
| CHEMBL3415583 | — | IC50 | = | 0.06 | nM | 10.22 |
| CHEMBL3415606 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL3415589 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL3415594 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL3415597 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL3415604 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL3414584 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3415587 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3415592 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3415599 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3415610 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL3415588 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL3415593 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL3415595 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL3415605 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3415607 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3415609 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL3260318 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL3415591 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3415585 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3415608 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3415584 | — | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL3415596 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3415582 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3415602 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL3415603 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL3415590 | — | IC50 | = | 184.0 | nM | 6.74 |
| CHEMBL3415586 | — | IC50 | = | 371.0 | nM | 6.43 |