Assay Detail
Binding
CHEMBL5371707
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Inhibition of N-terminal polyhistidine-tagged recombinant human NSD1 (1538 to 2696 residues) expressed in baculovirus infected insect cell using SAM as substrate preincubated for 20 mins followed by substrate addition measured after 1 hrs by hotspot assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Insect cell |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Histone-lysine N-methyltransferase, H3 lysine-36 specific (CHEMBL3588738) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
NSD3: Advances in cancer therapeutic potential and inhibitors research.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 5.61 | 6.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL337173 | — | — | 1 | 6.96 |
| CHEMBL3137309 | VENETOCLAX | 4.0 | 1 | 5.62 |
| CHEMBL1215331 | PF-03882845 | 1.0 | 1 | 4.92 |
| CHEMBL2058156 | — | — | 1 | 4.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL337173 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3137309 | VENETOCLAX | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL1215331 | PF-03882845 | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL2058156 | — | IC50 | = | 12000.0 | nM | 4.92 |