Assay Detail
Binding
CHEMBL3090924
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of C-RAF (unknown origin)-mediated inactive MEK1 K97R mutant phosphorylation after 45 mins by TR-FRET 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
RAF proto-oncogene serine/threonine-protein kinase (CHEMBL1906) ↗| 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 | 7.57 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3086073 | — | — | 1 | 8.40 |
| CHEMBL3086075 | — | — | 1 | 8.40 |
| CHEMBL3086078 | — | — | 1 | 8.30 |
| CHEMBL3086066 | — | — | 1 | 8.30 |
| CHEMBL3086074 | — | — | 1 | 8.22 |
| CHEMBL3086065 | — | — | 1 | 8.10 |
| CHEMBL3086076 | — | — | 1 | 7.80 |
| CHEMBL3086064 | — | — | 1 | 7.58 |
| CHEMBL3086070 | — | — | 1 | 7.43 |
| CHEMBL3086072 | — | — | 1 | 7.40 |
| CHEMBL3086071 | — | — | 1 | 7.35 |
| CHEMBL3086069 | — | — | 1 | 7.30 |
| CHEMBL3086068 | — | — | 1 | 7.25 |
| CHEMBL3086062 | — | — | 1 | 7.00 |
| CHEMBL3086063 | — | — | 1 | 6.92 |
| CHEMBL81277 | — | — | 1 | 6.77 |
| CHEMBL3086067 | — | — | 1 | 6.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3086073 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3086075 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3086078 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3086066 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3086074 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3086065 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3086076 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3086064 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3086070 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL3086072 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3086071 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL3086069 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL3086068 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL3086062 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3086063 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL81277 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL3086067 | — | IC50 | = | 570.0 | nM | 6.24 |