Assay Detail
ADMET
CHEMBL3377164
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of CYP2C9 (unknown origin)
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 5.65 | 5.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3330651 | — | — | 1 | 5.92 |
| CHEMBL2087461 | — | — | 1 | 5.89 |
| CHEMBL3330652 | — | — | 1 | 5.14 |
| CHEMBL3330650 | GDC-0623 | — | 1 | - |
| CHEMBL3330649 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3330651 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL2087461 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL3330652 | — | IC50 | = | 7300.0 | nM | 5.14 |
| CHEMBL3330650 | GDC-0623 | IC50 | > | 10000.0 | nM | - |
| CHEMBL3330649 | — | IC50 | > | 10000.0 | nM | - |