Assay Detail
Functional
CHEMBL5383989
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against human HCT-116 cells expressing MTAP-/- assessed as inhibition of cell proliferation incubated for 4 days by fluorescence based assay
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HCT-116 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Design and Structural Optimization of Methionine Adenosyltransferase 2A (MAT2A) Inhibitors with High In Vivo Potency and Oral Bioavailability.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 6.79 | 7.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5399738 | — | — | 1 | 7.47 |
| CHEMBL5415073 | — | — | 1 | 7.38 |
| CHEMBL5432232 | — | — | 1 | 7.30 |
| CHEMBL5412125 | — | — | 1 | 7.28 |
| CHEMBL5401515 | — | — | 1 | 7.28 |
| CHEMBL5434352 | — | — | 1 | 7.25 |
| CHEMBL5405749 | — | — | 1 | 7.25 |
| CHEMBL5423083 | — | — | 1 | 7.17 |
| CHEMBL5398750 | — | — | 1 | 7.12 |
| CHEMBL5397124 | — | — | 1 | 7.10 |
| CHEMBL5400994 | — | — | 1 | 7.09 |
| CHEMBL5402991 | — | — | 1 | 7.08 |
| CHEMBL5440991 | — | — | 1 | 6.93 |
| CHEMBL5425823 | — | — | 1 | 6.92 |
| CHEMBL5178902 | — | — | 1 | 6.84 |
| CHEMBL5426003 | — | — | 1 | 6.80 |
| CHEMBL5427061 | — | — | 1 | 6.78 |
| CHEMBL4573938 | — | — | 1 | 6.61 |
| CHEMBL5412431 | — | — | 1 | 6.50 |
| CHEMBL5437430 | — | — | 1 | 6.45 |
| CHEMBL5432694 | — | — | 1 | 6.41 |
| CHEMBL5419227 | — | — | 1 | 6.35 |
| CHEMBL5393737 | — | — | 1 | 6.32 |
| CHEMBL5430139 | — | — | 1 | 6.10 |
| CHEMBL5418094 | — | — | 1 | 5.51 |
| CHEMBL5413811 | — | — | 1 | 5.21 |
| CHEMBL5433500 | — | — | 1 | - |
| CHEMBL5395838 | — | — | 1 | - |
| CHEMBL5408830 | — | — | 1 | - |
| CHEMBL5413008 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5399738 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL5415073 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL5432232 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL5412125 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL5401515 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL5434352 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL5405749 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL5423083 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL5398750 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL5397124 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL5400994 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL5402991 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL5440991 | — | IC50 | = | 118.0 | nM | 6.93 |
| CHEMBL5425823 | — | IC50 | = | 119.0 | nM | 6.92 |
| CHEMBL5178902 | — | IC50 | = | 145.0 | nM | 6.84 |
| CHEMBL5426003 | — | IC50 | = | 159.0 | nM | 6.80 |
| CHEMBL5427061 | — | IC50 | = | 166.0 | nM | 6.78 |
| CHEMBL4573938 | — | IC50 | = | 244.0 | nM | 6.61 |
| CHEMBL5412431 | — | IC50 | = | 315.0 | nM | 6.50 |
| CHEMBL5437430 | — | IC50 | = | 355.0 | nM | 6.45 |
| CHEMBL5432694 | — | IC50 | = | 387.0 | nM | 6.41 |
| CHEMBL5419227 | — | IC50 | = | 447.0 | nM | 6.35 |
| CHEMBL5393737 | — | IC50 | = | 484.0 | nM | 6.32 |
| CHEMBL5430139 | — | IC50 | = | 792.0 | nM | 6.10 |
| CHEMBL5418094 | — | IC50 | = | 3111.0 | nM | 5.51 |
| CHEMBL5413811 | — | IC50 | = | 6118.0 | nM | 5.21 |
| CHEMBL5433500 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5395838 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5408830 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5413008 | — | IC50 | > | 10000.0 | nM | - |