Assay Detail
Binding
CHEMBL5049203
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Inhibition of ERK phosphorylation in human A-375 cells incubated for 3 hrs by DELFIA assay
13
Total Activities
13
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | A-375 |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Discovery of MAP855, an Efficacious and Selective MEK1/2 Inhibitor with an ATP-Competitive Mode of Action.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 10 | 5.10 | 6.40 |
| IC50 | 3 | 7.08 | 7.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3926171 | — | — | 1 | 7.22 |
| CHEMBL5089865 | — | — | 1 | 7.10 |
| CHEMBL5080471 | — | — | 1 | 6.92 |
| CHEMBL5090765 | — | — | 1 | 6.40 |
| CHEMBL5094993 | — | — | 1 | 5.52 |
| CHEMBL3904439 | — | — | 1 | 5.30 |
| CHEMBL5087942 | — | — | 1 | 5.24 |
| CHEMBL3951042 | — | — | 1 | 5.16 |
| CHEMBL3974369 | — | — | 1 | 4.72 |
| CHEMBL3936680 | — | — | 1 | 4.30 |
| CHEMBL3971755 | — | — | 1 | 4.19 |
| CHEMBL5085569 | — | — | 1 | - |
| CHEMBL3932078 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3926171 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL5089865 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL5080471 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL5090765 | — | EC50 | = | 400.0 | nM | 6.40 |
| CHEMBL5094993 | — | EC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL3904439 | — | EC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL5087942 | — | EC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL3951042 | — | EC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL3974369 | — | EC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL3936680 | — | EC50 | = | 50000.0 | nM | 4.30 |
| CHEMBL3971755 | — | EC50 | = | 64000.0 | nM | 4.19 |
| CHEMBL5085569 | — | EC50 | = | 340000.0 | nM | - |
| CHEMBL3932078 | — | EC50 | = | 109000.0 | nM | - |