Assay Detail
Binding
CHEMBL3592282
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Inhibition of SMYD2 (unknown origin) using biotinylated GSRAHSSHLKSKKGQSTSRH as substrate assessed as incorporation of tritium labeled methyl group from [3H]-SAM to biotinylated peptide substrate after 40 mins by scintillation proximity assay
11
Total Activities
11
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of A-893, A New Cell-Active Benzoxazinone Inhibitor of Lysine Methyltransferase SMYD2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 6.23 | 8.55 |
| Inhibition | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3590526 | — | — | 1 | 8.55 |
| CHEMBL3590527 | — | — | 1 | 8.25 |
| CHEMBL2169920 | — | — | 1 | 6.64 |
| CHEMBL3590519 | — | — | 1 | 6.36 |
| CHEMBL3590524 | — | — | 1 | 5.85 |
| CHEMBL3590520 | — | — | 1 | 5.66 |
| CHEMBL3590525 | — | — | 1 | 5.62 |
| CHEMBL3590518 | — | — | 1 | 5.51 |
| CHEMBL3590523 | — | — | 1 | 5.30 |
| CHEMBL3590521 | — | — | 1 | 4.58 |
| CHEMBL3590522 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3590526 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL3590527 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL2169920 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL3590519 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL3590524 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL3590520 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL3590525 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL3590518 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL3590523 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL3590521 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL3590522 | — | Inhibition | - | % | - |