Assay Detail
Binding
CHEMBL4196286
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of mouse full-length GST-tagged BRAF V600E mutant using recombinant human full length N-terminal His-tagged MEK1 as substrate preincubated for 60 mins followed by substrate addition and measured after 25 mins by ELISA
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Serine/threonine-protein kinase B-raf (CHEMBL2331061) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
Publication
Design, synthesis, mechanistic and histopathological studies of small-molecules of novel indole-2-carboxamides and pyrazino[1,2-a]indol-1(2H)-ones as potential anticancer agents effecting the reactive oxygen species production.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 6.15 | 7.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 7.22 |
| CHEMBL4208224 | — | — | 1 | 7.00 |
| CHEMBL4213146 | — | — | 1 | 6.05 |
| CHEMBL4207316 | — | — | 1 | 6.00 |
| CHEMBL4208745 | — | — | 1 | 6.00 |
| CHEMBL4209588 | — | — | 1 | 5.43 |
| CHEMBL4214496 | — | — | 1 | 5.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL553 | ERLOTINIB | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4208224 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4213146 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL4207316 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4208745 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4209588 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL4214496 | — | IC50 | = | 4800.0 | nM | 5.32 |