Assay Detail
Binding
CHEMBL4835540
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 incubated for 60 mins followed by substrate addition and measured after 60 mins
46
Total Activities
46
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
Discovery of AG-270, a First-in-Class Oral MAT2A Inhibitor for the Treatment of Tumors with Homozygous <i>MTAP</i> Deletion.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 46 | 6.73 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4521249 | — | — | 1 | 8.40 |
| CHEMBL4552959 | — | — | 1 | 8.40 |
| CHEMBL4558617 | — | — | 1 | 8.30 |
| CHEMBL4568226 | — | — | 1 | 8.15 |
| CHEMBL4582312 | — | — | 1 | 8.15 |
| CHEMBL4514699 | — | — | 1 | 8.15 |
| CHEMBL4870597 | — | — | 1 | 8.10 |
| CHEMBL4585665 | — | — | 1 | 8.00 |
| CHEMBL4584451 | — | — | 1 | 7.96 |
| CHEMBL4559088 | — | — | 1 | 7.89 |
| CHEMBL4573938 | — | — | 1 | 7.85 |
| CHEMBL4590059 | — | — | 1 | 7.60 |
| CHEMBL4529030 | — | — | 1 | 7.55 |
| CHEMBL4587880 | — | — | 1 | 7.48 |
| CHEMBL4549681 | — | — | 1 | 7.35 |
| CHEMBL4483464 | — | — | 1 | 7.28 |
| CHEMBL4560666 | — | — | 1 | 7.24 |
| CHEMBL4561247 | — | — | 1 | 7.18 |
| CHEMBL4582351 | — | — | 1 | 7.08 |
| CHEMBL4552037 | — | — | 1 | 7.01 |
| CHEMBL4856769 | — | — | 1 | 6.99 |
| CHEMBL4546944 | — | — | 1 | 6.92 |
| CHEMBL4525301 | — | — | 1 | 6.82 |
| CHEMBL4551583 | — | — | 1 | 6.80 |
| CHEMBL4531472 | — | — | 1 | 6.80 |
| CHEMBL4865263 | — | — | 1 | 6.58 |
| CHEMBL4877839 | — | — | 1 | 6.58 |
| CHEMBL4875209 | — | — | 1 | 6.57 |
| CHEMBL4875322 | — | — | 1 | 6.18 |
| CHEMBL4866271 | — | — | 1 | 6.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4521249 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4552959 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4558617 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4568226 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4582312 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4514699 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4870597 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4585665 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4584451 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4559088 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4573938 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4590059 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4529030 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4587880 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4549681 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL4483464 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL4560666 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL4561247 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL4582351 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL4552037 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL4856769 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL4546944 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4525301 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4551583 | — | IC50 | = | 159.0 | nM | 6.80 |
| CHEMBL4531472 | — | IC50 | = | 158.0 | nM | 6.80 |
| CHEMBL4865263 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL4877839 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL4875209 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4875322 | — | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL4866271 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL4878283 | — | IC50 | = | 1140.0 | nM | 5.94 |
| CHEMBL4541968 | — | IC50 | = | 1310.0 | nM | 5.88 |
| CHEMBL4522713 | — | IC50 | = | 1340.0 | nM | 5.87 |
| CHEMBL4859703 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4866030 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4854483 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL4865666 | — | IC50 | = | 3660.0 | nM | 5.44 |
| CHEMBL4539385 | — | IC50 | = | 3660.0 | nM | 5.44 |
| CHEMBL4872447 | — | IC50 | = | 4110.0 | nM | 5.39 |
| CHEMBL4862694 | — | IC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL4874436 | — | IC50 | = | 12200.0 | nM | 4.91 |
| CHEMBL4857178 | — | IC50 | = | 16600.0 | nM | 4.78 |
| CHEMBL4863546 | — | IC50 | = | 50100.0 | nM | 4.30 |
| CHEMBL4858279 | — | IC50 | = | 78800.0 | nM | 4.10 |
| CHEMBL4877600 | — | IC50 | - | — | - | |
| CHEMBL4877431 | — | IC50 | - | — | - |