Assay Detail
Binding
CHEMBL5617079
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human NSD2 (941 to 1240 residues) using unmethylated histone H3 as substrate incubated for 40 mins in the presence of SAM and nucleosomes by AlphaLISA method
38
Total Activities
38
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 NSD2 (CHEMBL3108645) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of a Highly Potent and Selective Inhibitor Targeting Protein Lysine Methyltransferase NSD2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 38 | 6.29 | 7.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5593832 | — | — | 1 | 7.77 |
| CHEMBL5589842 | — | — | 1 | 7.66 |
| CHEMBL5620247 | — | — | 1 | 7.54 |
| CHEMBL5618412 | — | — | 1 | 7.50 |
| CHEMBL5618451 | — | — | 1 | 7.42 |
| CHEMBL5619719 | — | — | 1 | 7.36 |
| CHEMBL5619815 | — | — | 1 | 7.35 |
| CHEMBL5619699 | — | — | 1 | 7.31 |
| CHEMBL5619576 | — | — | 1 | 7.22 |
| CHEMBL5620022 | — | — | 1 | 7.07 |
| CHEMBL5618171 | — | — | 1 | 6.69 |
| CHEMBL5422549 | — | — | 1 | 6.61 |
| CHEMBL5618212 | — | — | 1 | 6.57 |
| CHEMBL5619303 | — | — | 1 | 6.42 |
| CHEMBL5619878 | — | — | 1 | 6.25 |
| CHEMBL5619544 | — | — | 1 | 5.92 |
| CHEMBL5618533 | — | — | 1 | 5.85 |
| CHEMBL5619559 | — | — | 1 | 5.85 |
| CHEMBL596639 | — | — | 1 | 5.84 |
| CHEMBL5619512 | — | — | 1 | 5.82 |
| CHEMBL5619351 | — | — | 1 | 5.82 |
| CHEMBL5618866 | — | — | 1 | 5.82 |
| CHEMBL5619523 | — | — | 1 | 5.81 |
| CHEMBL569864 | — | — | 1 | 5.76 |
| CHEMBL5618415 | — | — | 1 | 5.61 |
| CHEMBL5618667 | — | — | 1 | 5.60 |
| CHEMBL5589782 | — | — | 1 | 5.58 |
| CHEMBL5618955 | — | — | 1 | 5.56 |
| CHEMBL5619072 | — | — | 1 | 5.50 |
| CHEMBL5618872 | — | — | 1 | 5.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5593832 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5589842 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL5620247 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL5618412 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL5618451 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL5619719 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL5619815 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL5619699 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL5619576 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL5620022 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL5618171 | — | IC50 | = | 204.0 | nM | 6.69 |
| CHEMBL5422549 | — | IC50 | = | 243.0 | nM | 6.61 |
| CHEMBL5618212 | — | IC50 | = | 271.0 | nM | 6.57 |
| CHEMBL5619303 | — | IC50 | = | 377.0 | nM | 6.42 |
| CHEMBL5619878 | — | IC50 | = | 569.0 | nM | 6.25 |
| CHEMBL5619544 | — | IC50 | = | 1199.0 | nM | 5.92 |
| CHEMBL5618533 | — | IC50 | = | 1408.0 | nM | 5.85 |
| CHEMBL5619559 | — | IC50 | = | 1411.0 | nM | 5.85 |
| CHEMBL596639 | — | IC50 | = | 1449.0 | nM | 5.84 |
| CHEMBL5619512 | — | IC50 | = | 1514.0 | nM | 5.82 |
| CHEMBL5618866 | — | IC50 | = | 1505.0 | nM | 5.82 |
| CHEMBL5619351 | — | IC50 | = | 1514.0 | nM | 5.82 |
| CHEMBL5619523 | — | IC50 | = | 1550.0 | nM | 5.81 |
| CHEMBL569864 | — | IC50 | = | 1731.0 | nM | 5.76 |
| CHEMBL5618415 | — | IC50 | = | 2431.0 | nM | 5.61 |
| CHEMBL5618667 | — | IC50 | = | 2521.0 | nM | 5.60 |
| CHEMBL5589782 | — | IC50 | = | 2647.0 | nM | 5.58 |
| CHEMBL5618955 | — | IC50 | = | 2777.0 | nM | 5.56 |
| CHEMBL5619072 | — | IC50 | = | 3153.0 | nM | 5.50 |
| CHEMBL5618872 | — | IC50 | = | 3326.0 | nM | 5.48 |
| CHEMBL5619142 | — | IC50 | = | 3762.0 | nM | 5.42 |
| CHEMBL5618106 | — | IC50 | = | 4296.0 | nM | 5.37 |
| CHEMBL5619962 | — | IC50 | = | 4565.0 | nM | 5.34 |
| CHEMBL5618534 | — | IC50 | = | 4899.0 | nM | 5.31 |
| CHEMBL5618724 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5618340 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL1873552 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL1902352 | — | IC50 | > | 5000.0 | nM | - |