Assay Detail
Binding
CHEMBL5628407
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of 3H-SAM from SUV39H1 (unknown origin) using biotinylated-histone H3 peptide as substrate incubated for 45 mins by SPA assay
12
Total Activities
12
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 |
Target
Histone-lysine N-methyltransferase SUV39H1 (CHEMBL1795118) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Development of selective class I protein arginine methyltransferase inhibitors through fragment-based drug design approach.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 4.71 | 5.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5633108 | — | — | 1 | 5.16 |
| CHEMBL5632617 | — | — | 1 | 4.85 |
| CHEMBL5633498 | — | — | 1 | 4.80 |
| CHEMBL5633177 | — | — | 1 | 4.80 |
| CHEMBL5633588 | — | — | 1 | 4.66 |
| CHEMBL5631669 | — | — | 1 | 4.64 |
| CHEMBL5632481 | — | — | 1 | 4.46 |
| CHEMBL5631576 | — | — | 1 | 4.33 |
| CHEMBL5633117 | — | — | 1 | - |
| CHEMBL5631984 | — | — | 1 | - |
| CHEMBL5632319 | — | — | 1 | - |
| CHEMBL5631287 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5633108 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL5632617 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL5633498 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL5633177 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL5633588 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL5631669 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL5632481 | — | IC50 | = | 35000.0 | nM | 4.46 |
| CHEMBL5631576 | — | IC50 | = | 47000.0 | nM | 4.33 |
| CHEMBL5633117 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL5631984 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5632319 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL5631287 | — | IC50 | > | 200000.0 | nM | - |