Assay Detail
Binding
CHEMBL5161735
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human MAT2A expressed in baculovirus infected Sf9 cells assessed as S-adenosyl methionine production using L-methionine as substrate preincubated for 60 mins followed by substrate addition and measured after 60 mins in presence of ATP
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| 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 | 16 | 6.38 | 7.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5170690 | — | — | 1 | 7.66 |
| CHEMBL5206904 | — | — | 1 | 7.47 |
| CHEMBL5176577 | — | — | 1 | 7.32 |
| CHEMBL5180626 | — | — | 1 | 7.27 |
| CHEMBL5188451 | — | — | 1 | 6.60 |
| CHEMBL5196666 | — | — | 1 | 6.50 |
| CHEMBL5175314 | — | — | 1 | 6.49 |
| CHEMBL5183201 | — | — | 1 | 6.39 |
| CHEMBL5183797 | — | — | 1 | 6.29 |
| CHEMBL5184221 | — | — | 1 | 6.28 |
| CHEMBL5201203 | — | — | 1 | 6.21 |
| CHEMBL5198564 | — | — | 1 | 6.16 |
| CHEMBL5177072 | — | — | 1 | 5.70 |
| CHEMBL5181922 | — | — | 1 | 5.48 |
| CHEMBL5185744 | — | — | 1 | 5.14 |
| CHEMBL5187600 | — | — | 1 | 5.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5170690 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL5206904 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL5176577 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL5180626 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL5188451 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL5196666 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL5175314 | — | IC50 | = | 325.0 | nM | 6.49 |
| CHEMBL5183201 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL5183797 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL5184221 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL5201203 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL5198564 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL5177072 | — | IC50 | = | 2010.0 | nM | 5.70 |
| CHEMBL5181922 | — | IC50 | = | 3310.0 | nM | 5.48 |
| CHEMBL5185744 | — | IC50 | = | 7200.0 | nM | 5.14 |
| CHEMBL5187600 | — | IC50 | = | 7830.0 | nM | 5.11 |