Assay Detail
Binding
CHEMBL3807564
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of mouse full length GST-tagged BRAF V600E mutant assessed as reduction in human full length N-terminal His-tagged MEK1 phosphorylation pre-incubated for 1 hr before MEK1 addition and measured after 25 mins
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Design, biological evaluation and 3D QSAR studies of novel dioxin-containing triaryl pyrazoline derivatives as potential B-Raf inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 6.11 | 7.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1229517 | VEMURAFENIB | 4.0 | 1 | 7.52 |
| CHEMBL3805508 | — | — | 1 | 7.40 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 7.22 |
| CHEMBL3806108 | — | — | 1 | 7.16 |
| CHEMBL2146827 | — | — | 1 | 6.96 |
| CHEMBL3805893 | — | — | 1 | 6.96 |
| CHEMBL3805410 | — | — | 1 | 6.85 |
| CHEMBL3805409 | — | — | 1 | 6.82 |
| CHEMBL3805675 | — | — | 1 | 6.68 |
| CHEMBL3805849 | — | — | 1 | 6.57 |
| CHEMBL3805476 | — | — | 1 | 6.27 |
| CHEMBL3804945 | — | — | 1 | 6.21 |
| CHEMBL3805819 | — | — | 1 | 6.07 |
| CHEMBL3805248 | — | — | 1 | 5.94 |
| CHEMBL3805796 | — | — | 1 | 5.41 |
| CHEMBL3804881 | — | — | 1 | 5.37 |
| CHEMBL3805161 | — | — | 1 | 5.29 |
| CHEMBL3804914 | — | — | 1 | 5.16 |
| CHEMBL3805227 | — | — | 1 | 5.09 |
| CHEMBL3804840 | — | — | 1 | 4.97 |
| CHEMBL3805397 | — | — | 1 | 4.44 |
| CHEMBL3805052 | — | — | 1 | 4.08 |
| CHEMBL3805300 | — | — | 1 | - |
| CHEMBL3805803 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1229517 | VEMURAFENIB | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3805508 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL553 | ERLOTINIB | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL3806108 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL2146827 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3805893 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3805410 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL3805409 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL3805675 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL3805849 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL3805476 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL3804945 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL3805819 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL3805248 | — | IC50 | = | 1140.0 | nM | 5.94 |
| CHEMBL3805796 | — | IC50 | = | 3880.0 | nM | 5.41 |
| CHEMBL3804881 | — | IC50 | = | 4270.0 | nM | 5.37 |
| CHEMBL3805161 | — | IC50 | = | 5170.0 | nM | 5.29 |
| CHEMBL3804914 | — | IC50 | = | 6850.0 | nM | 5.16 |
| CHEMBL3805227 | — | IC50 | = | 8050.0 | nM | 5.09 |
| CHEMBL3804840 | — | IC50 | = | 10700.0 | nM | 4.97 |
| CHEMBL3805397 | — | IC50 | = | 36300.0 | nM | 4.44 |
| CHEMBL3805052 | — | IC50 | = | 83600.0 | nM | 4.08 |
| CHEMBL3805300 | — | IC50 | = | 118000.0 | nM | - |
| CHEMBL3805803 | — | IC50 | > | 300000.0 | nM | - |