Assay Detail
Binding
CHEMBL5046926
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human MEK-1 by Lanthascreen TR-FRET assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Dual specificity mitogen-activated protein kinase kinase 1 (CHEMBL3587) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Structural effects of morpholine replacement in ZSTK474 on Class I PI3K isoform inhibition: Development of novel MEK/PI3K bifunctional inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 7.28 | 8.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL244488 | — | — | 1 | 8.49 |
| CHEMBL5084156 | — | — | 1 | 6.91 |
| CHEMBL5089694 | — | — | 1 | 6.45 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL244488 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL5084156 | — | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL5089694 | — | IC50 | = | 352.0 | nM | 6.45 |