Assay Detail
Functional
CHEMBL3751461
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against human HepG2 cells harboring N-Ras mutation
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HepG2 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Optimization of allosteric MEK inhibitors. Part 2: Taming the sulfamide group balances compound distribution properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 8.20 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3746559 | — | — | 1 | 8.70 |
| CHEMBL3746640 | — | — | 1 | 8.30 |
| CHEMBL507361 | MIRDAMETINIB | 2.0 | 1 | 8.30 |
| CHEMBL1614701 | SELUMETINIB | 4.0 | 1 | 7.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3746559 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3746640 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL507361 | MIRDAMETINIB | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1614701 | SELUMETINIB | IC50 | = | 32.0 | nM | 7.50 |