Assay Detail
Binding
CHEMBL963130
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Inhibition of MEK-mediated ERK phosphorylation in PDGF-stimulated mouse K-Balb cells treated as single oral dose preincubated for 24 hrs before PDGF challenge by whole cell assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| 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 | 14 | 6.70 | 7.45 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL105442 | CI-1040 | 2.0 | 1 | 7.45 |
| CHEMBL442641 | — | — | 1 | 7.33 |
| CHEMBL448323 | — | — | 1 | 7.30 |
| CHEMBL455472 | — | — | 1 | 7.07 |
| CHEMBL454114 | — | — | 1 | 6.95 |
| CHEMBL454880 | — | — | 1 | 6.87 |
| CHEMBL453890 | — | — | 1 | 6.76 |
| CHEMBL455470 | — | — | 1 | 6.63 |
| CHEMBL455471 | — | — | 1 | 6.59 |
| CHEMBL510625 | — | — | 1 | 6.49 |
| CHEMBL511056 | — | — | 1 | 6.21 |
| CHEMBL510244 | — | — | 1 | 6.19 |
| CHEMBL454115 | — | — | 1 | 6.18 |
| CHEMBL454116 | — | — | 1 | 5.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL105442 | CI-1040 | IC50 | = | 35.4 | nM | 7.45 |
| CHEMBL442641 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL448323 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL455472 | — | IC50 | = | 84.6 | nM | 7.07 |
| CHEMBL454114 | — | IC50 | = | 113.0 | nM | 6.95 |
| CHEMBL454880 | — | IC50 | = | 136.0 | nM | 6.87 |
| CHEMBL453890 | — | IC50 | = | 172.0 | nM | 6.76 |
| CHEMBL455470 | — | IC50 | = | 232.0 | nM | 6.63 |
| CHEMBL455471 | — | IC50 | = | 257.0 | nM | 6.59 |
| CHEMBL510625 | — | IC50 | = | 326.0 | nM | 6.49 |
| CHEMBL511056 | — | IC50 | = | 624.0 | nM | 6.21 |
| CHEMBL510244 | — | IC50 | = | 645.0 | nM | 6.19 |
| CHEMBL454115 | — | IC50 | = | 661.0 | nM | 6.18 |
| CHEMBL454116 | — | IC50 | = | 1780.0 | nM | 5.75 |