Assay Detail
Binding
CHEMBL5318855
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human NSD2 (941 to 1240 residues) using SAM as substrate incubated for 3 hrs by AlphaLISA assay
39
Total Activities
39
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
Structural Modification and Pharmacological Evaluation of Substituted Quinoline-5,8-diones as Potent NSD2 Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 39 | 6.24 | 6.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5406268 | — | — | 1 | 6.70 |
| CHEMBL131199 | — | — | 1 | 6.68 |
| CHEMBL5422549 | — | — | 1 | 6.64 |
| CHEMBL337173 | — | — | 1 | 6.64 |
| CHEMBL5418169 | — | — | 1 | 6.62 |
| CHEMBL5412847 | — | — | 1 | 6.60 |
| CHEMBL5415704 | — | — | 1 | 6.60 |
| CHEMBL5402620 | — | — | 1 | 6.52 |
| CHEMBL5433538 | — | — | 1 | 6.52 |
| CHEMBL5401066 | — | — | 1 | 6.51 |
| CHEMBL5418912 | — | — | 1 | 6.48 |
| CHEMBL5419286 | — | — | 1 | 6.48 |
| CHEMBL5419919 | — | — | 1 | 6.44 |
| CHEMBL5402868 | — | — | 1 | 6.44 |
| CHEMBL5402955 | — | — | 1 | 6.42 |
| CHEMBL5436306 | — | — | 1 | 6.42 |
| CHEMBL5435504 | — | — | 1 | 6.39 |
| CHEMBL5440868 | — | — | 1 | 6.38 |
| CHEMBL5408020 | — | — | 1 | 6.35 |
| CHEMBL340219 | — | — | 1 | 6.35 |
| CHEMBL5422301 | — | — | 1 | 6.33 |
| CHEMBL337520 | — | — | 1 | 6.31 |
| CHEMBL5401031 | — | — | 1 | 6.31 |
| CHEMBL5435611 | — | — | 1 | 6.23 |
| CHEMBL5424751 | — | — | 1 | 6.12 |
| CHEMBL5397372 | — | — | 1 | 6.03 |
| CHEMBL5407373 | — | — | 1 | 6.00 |
| CHEMBL5412582 | — | — | 1 | 5.91 |
| CHEMBL5397204 | — | — | 1 | 5.89 |
| CHEMBL5407427 | — | — | 1 | 5.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5406268 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL131199 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL337173 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL5422549 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL5418169 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL5412847 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL5415704 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL5402620 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL5433538 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL5401066 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL5418912 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL5419286 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL5419919 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL5402868 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL5436306 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL5402955 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL5435504 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL5440868 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL340219 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL5408020 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL5422301 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL337520 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL5401031 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL5435611 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL5424751 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL5397372 | — | IC50 | = | 930.0 | nM | 6.03 |
| CHEMBL5407373 | — | IC50 | = | 990.0 | nM | 6.00 |
| CHEMBL5412582 | — | IC50 | = | 1220.0 | nM | 5.91 |
| CHEMBL5407427 | — | IC50 | = | 1290.0 | nM | 5.89 |
| CHEMBL5397204 | — | IC50 | = | 1280.0 | nM | 5.89 |
| CHEMBL5401919 | — | IC50 | = | 1310.0 | nM | 5.88 |
| CHEMBL5406546 | — | IC50 | = | 1350.0 | nM | 5.87 |
| CHEMBL5411172 | — | IC50 | = | 1460.0 | nM | 5.84 |
| CHEMBL5412710 | — | IC50 | = | 1710.0 | nM | 5.77 |
| CHEMBL5428630 | — | IC50 | = | 2290.0 | nM | 5.64 |
| CHEMBL5430389 | — | IC50 | = | 2340.0 | nM | 5.63 |
| CHEMBL5403046 | — | IC50 | = | 2480.0 | nM | 5.61 |
| CHEMBL5397613 | — | IC50 | = | 3050.0 | nM | 5.52 |
| CHEMBL5395206 | — | IC50 | > | 10000.0 | nM | - |