Assay Detail
Binding
CHEMBL3090923
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of MEK1 S218E/S222E mutant (unknown origin) using inactive MAP kinase 2/Erk2 and FAM-Erktide as substrate assessed as inhibition of FAM-Erktide phosphorylation preincubated with inactive MAP kinase 2/Erk2 for 30 mins followed by FAM-Erktide addition measured after 90 mins by IMAP fluorescence polarization assay
17
Total Activities
17
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
The sulfamide moiety affords higher inhibitory activity and oral bioavailability to a series of coumarin dual selective RAF/MEK inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 7.44 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3086072 | — | — | 1 | 8.30 |
| CHEMBL3086065 | — | — | 1 | 8.15 |
| CHEMBL3086078 | — | — | 1 | 8.05 |
| CHEMBL3086066 | — | — | 1 | 7.96 |
| CHEMBL3086069 | — | — | 1 | 7.68 |
| CHEMBL3086064 | — | — | 1 | 7.55 |
| CHEMBL3086068 | — | — | 1 | 7.54 |
| CHEMBL3086076 | — | — | 1 | 7.46 |
| CHEMBL3086073 | — | — | 1 | 7.44 |
| CHEMBL3086074 | — | — | 1 | 7.34 |
| CHEMBL3086075 | — | — | 1 | 7.33 |
| CHEMBL3086063 | — | — | 1 | 7.25 |
| CHEMBL3086070 | — | — | 1 | 7.24 |
| CHEMBL3086071 | — | — | 1 | 7.19 |
| CHEMBL81277 | — | — | 1 | 7.02 |
| CHEMBL3086062 | — | — | 1 | 6.68 |
| CHEMBL3086067 | — | — | 1 | 6.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3086072 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3086065 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3086078 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3086066 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3086069 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3086064 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL3086068 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL3086076 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL3086073 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL3086074 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL3086075 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL3086063 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL3086070 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL3086071 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL81277 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL3086062 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL3086067 | — | IC50 | = | 500.0 | nM | 6.30 |