Assay Detail
Binding
CHEMBL4738306
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of BRAF V600E mutant (unknown origin) using Ser/Thr 03 as substrate after 1 hr in presence of ATP by Z'-LYTE assay
12
Total Activities
12
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
Serine/threonine-protein kinase B-raf (CHEMBL5145) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design, synthesis, biological evaluation, and docking studies of novel (imidazol-5-yl)pyrimidine-based derivatives as dual BRAF/p38α inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.96 | 8.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4793723 | — | — | 1 | 8.60 |
| CHEMBL4797100 | — | — | 1 | 8.37 |
| CHEMBL4758203 | — | — | 1 | 8.25 |
| CHEMBL4741154 | — | — | 1 | 8.11 |
| CHEMBL4763666 | — | — | 1 | 8.10 |
| CHEMBL4779919 | — | — | 1 | 8.06 |
| CHEMBL4795144 | — | — | 1 | 7.83 |
| CHEMBL4756408 | — | — | 1 | 7.66 |
| CHEMBL4755378 | — | — | 1 | 7.58 |
| CHEMBL4794140 | — | — | 1 | 7.52 |
| CHEMBL388978 | STAUROSPORINE | — | 1 | 7.50 |
| CHEMBL406845 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4793723 | — | IC50 | = | 2.49 | nM | 8.60 |
| CHEMBL4797100 | — | IC50 | = | 4.25 | nM | 8.37 |
| CHEMBL4758203 | — | IC50 | = | 5.62 | nM | 8.25 |
| CHEMBL4741154 | — | IC50 | = | 7.81 | nM | 8.11 |
| CHEMBL4763666 | — | IC50 | = | 8.04 | nM | 8.10 |
| CHEMBL4779919 | — | IC50 | = | 8.68 | nM | 8.06 |
| CHEMBL4795144 | — | IC50 | = | 14.8 | nM | 7.83 |
| CHEMBL4756408 | — | IC50 | = | 21.8 | nM | 7.66 |
| CHEMBL4755378 | — | IC50 | = | 26.3 | nM | 7.58 |
| CHEMBL4794140 | — | IC50 | = | 30.3 | nM | 7.52 |
| CHEMBL388978 | STAUROSPORINE | IC50 | = | 31.6 | nM | 7.50 |
| CHEMBL406845 | — | IC50 | - | — | - |