Assay Detail
Binding
CHEMBL963131
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Inhibition of MEK-stimulated ERK phosphorylation in PDGF-stimulated mouse C26 cells treated as single oral dose before PDGF challenge by whole cell assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Cell Type | C26 |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
The discovery of the benzhydroxamate MEK inhibitors CI-1040 and PD 0325901.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 8.96 | 10.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL244488 | — | — | 1 | 10.15 |
| CHEMBL507361 | MIRDAMETINIB | 2.0 | 1 | 9.48 |
| CHEMBL450775 | — | — | 1 | 9.32 |
| CHEMBL507836 | — | — | 1 | 9.09 |
| CHEMBL508526 | — | — | 1 | 9.00 |
| CHEMBL105442 | CI-1040 | 2.0 | 1 | 8.46 |
| CHEMBL452600 | — | — | 1 | 8.46 |
| CHEMBL447345 | — | — | 1 | 7.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL244488 | — | IC50 | = | 0.07 | nM | 10.15 |
| CHEMBL507361 | MIRDAMETINIB | IC50 | = | 0.33 | nM | 9.48 |
| CHEMBL450775 | — | IC50 | = | 0.48 | nM | 9.32 |
| CHEMBL507836 | — | IC50 | = | 0.82 | nM | 9.09 |
| CHEMBL508526 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL105442 | CI-1040 | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL452600 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL447345 | — | IC50 | = | 19.0 | nM | 7.72 |