Assay Detail
Binding
CHEMBL963129
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Inhibition of MEK-mediated ERK phosphorylation in PDGF-stimulated mouse K-Balb cells treated as single oral dose preincubated for 1 hr 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 | 7.80 | 8.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL510244 | — | — | 1 | 8.80 |
| CHEMBL105442 | CI-1040 | 2.0 | 1 | 8.61 |
| CHEMBL511056 | — | — | 1 | 8.45 |
| CHEMBL442641 | — | — | 1 | 8.38 |
| CHEMBL454880 | — | — | 1 | 8.36 |
| CHEMBL453890 | — | — | 1 | 8.19 |
| CHEMBL455470 | — | — | 1 | 8.09 |
| CHEMBL448323 | — | — | 1 | 7.93 |
| CHEMBL455471 | — | — | 1 | 7.63 |
| CHEMBL454114 | — | — | 1 | 7.58 |
| CHEMBL455472 | — | — | 1 | 7.26 |
| CHEMBL510625 | — | — | 1 | 7.12 |
| CHEMBL454115 | — | — | 1 | 6.92 |
| CHEMBL454116 | — | — | 1 | 5.94 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL510244 | — | IC50 | = | 1.59 | nM | 8.80 |
| CHEMBL105442 | CI-1040 | IC50 | = | 2.45 | nM | 8.61 |
| CHEMBL511056 | — | IC50 | = | 3.55 | nM | 8.45 |
| CHEMBL442641 | — | IC50 | = | 4.18 | nM | 8.38 |
| CHEMBL454880 | — | IC50 | = | 4.42 | nM | 8.36 |
| CHEMBL453890 | — | IC50 | = | 6.48 | nM | 8.19 |
| CHEMBL455470 | — | IC50 | = | 8.18 | nM | 8.09 |
| CHEMBL448323 | — | IC50 | = | 11.8 | nM | 7.93 |
| CHEMBL455471 | — | IC50 | = | 23.5 | nM | 7.63 |
| CHEMBL454114 | — | IC50 | = | 26.4 | nM | 7.58 |
| CHEMBL455472 | — | IC50 | = | 54.9 | nM | 7.26 |
| CHEMBL510625 | — | IC50 | = | 75.8 | nM | 7.12 |
| CHEMBL454115 | — | IC50 | = | 119.0 | nM | 6.92 |
| CHEMBL454116 | — | IC50 | = | 1140.0 | nM | 5.94 |