Assay Detail
Binding
CHEMBL5161737
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of MT2A in MTAP-null human HCT-116 cells after 72 hrs by LC-MS/MS analysis
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HCT116-MTAP null |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
S-adenosylmethionine synthase isoform type-2 (CHEMBL3313835) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Leveraging Structure-Based Drug Design to Identify Next-Generation MAT2A Inhibitors, Including Brain-Penetrant and Peripherally Efficacious Leads.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 7.53 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5185760 | — | — | 1 | 8.00 |
| CHEMBL5177250 | — | — | 1 | 7.96 |
| CHEMBL5187048 | — | — | 1 | 7.89 |
| CHEMBL5178902 | — | — | 1 | 7.85 |
| CHEMBL5207988 | — | — | 1 | 7.68 |
| CHEMBL5207874 | — | — | 1 | 7.64 |
| CHEMBL5185699 | — | — | 1 | 7.51 |
| CHEMBL5206988 | — | — | 1 | 7.50 |
| CHEMBL5170690 | — | — | 1 | 7.47 |
| CHEMBL5183776 | — | — | 1 | 7.34 |
| CHEMBL5205028 | — | — | 1 | 7.10 |
| CHEMBL5183514 | — | — | 1 | 7.00 |
| CHEMBL5208553 | — | — | 1 | 6.95 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5185760 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5177250 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5187048 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5178902 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5207988 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL5207874 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL5185699 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL5206988 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL5170690 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL5183776 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL5205028 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL5183514 | — | IC50 | = | 101.0 | nM | 7.00 |
| CHEMBL5208553 | — | IC50 | = | 113.0 | nM | 6.95 |