Assay Detail
Functional
CHEMBL3377161
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Antiproliferative activity against human HCT116 cells assessed as inhibition of cell proliferation after 72 hrs
8
Total Activities
8
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
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 |
|---|---|---|---|
| EC50 | 8 | 7.13 | 7.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3330652 | — | — | 1 | 7.46 |
| CHEMBL2087461 | — | — | 1 | 7.36 |
| CHEMBL3330650 | GDC-0623 | — | 1 | 7.29 |
| CHEMBL3330654 | — | — | 1 | 7.28 |
| CHEMBL3330655 | — | — | 1 | 6.97 |
| CHEMBL3330649 | — | — | 1 | 6.92 |
| CHEMBL3330653 | — | — | 1 | 6.92 |
| CHEMBL3330651 | — | — | 1 | 6.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3330652 | — | EC50 | = | 35.0 | nM | 7.46 |
| CHEMBL2087461 | — | EC50 | = | 44.0 | nM | 7.36 |
| CHEMBL3330650 | GDC-0623 | EC50 | = | 51.0 | nM | 7.29 |
| CHEMBL3330654 | — | EC50 | = | 52.0 | nM | 7.28 |
| CHEMBL3330655 | — | EC50 | = | 107.0 | nM | 6.97 |
| CHEMBL3330649 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3330653 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3330651 | — | EC50 | = | 140.0 | nM | 6.85 |