Assay Detail
Binding
CHEMBL1781334
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Inhibition of B-Raf V599E mutant assessed as phosphorylation of MEK1/2 by ELISA
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Serine/threonine-protein kinase B-raf (CHEMBL5145) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design and synthesis of 5,6-fused heterocyclic amides as Raf kinase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 7.38 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1778410 | — | — | 1 | 8.70 |
| CHEMBL1778401 | — | — | 1 | 8.40 |
| CHEMBL1778403 | — | — | 1 | 8.40 |
| CHEMBL1778394 | — | — | 1 | 8.30 |
| CHEMBL1778291 | — | — | 1 | 8.22 |
| CHEMBL1778395 | — | — | 1 | 8.22 |
| CHEMBL1778405 | — | — | 1 | 8.15 |
| CHEMBL1778396 | — | — | 1 | 7.96 |
| CHEMBL1778397 | — | — | 1 | 7.92 |
| CHEMBL1778404 | — | — | 1 | 7.82 |
| CHEMBL1778409 | — | — | 1 | 7.75 |
| CHEMBL1778408 | — | — | 1 | 7.72 |
| CHEMBL1162958 | — | — | 1 | 7.68 |
| CHEMBL1778393 | — | — | 1 | 7.60 |
| CHEMBL1778406 | — | — | 1 | 7.58 |
| CHEMBL1778407 | — | — | 1 | 7.19 |
| CHEMBL1778391 | — | — | 1 | 6.96 |
| CHEMBL470808 | — | — | 1 | 6.92 |
| CHEMBL1778399 | — | — | 1 | 6.89 |
| CHEMBL1778402 | — | — | 1 | 6.70 |
| CHEMBL1778411 | — | — | 1 | 6.62 |
| CHEMBL1778293 | — | — | 1 | 6.58 |
| CHEMBL1778294 | — | — | 1 | 6.47 |
| CHEMBL1778292 | — | — | 1 | 6.24 |
| CHEMBL1778398 | — | — | 1 | 6.17 |
| CHEMBL1778400 | — | — | 1 | 4.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1778410 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1778401 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1778403 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1778394 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1778291 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL1778395 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL1778405 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1778396 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1778397 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL1778404 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL1778409 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL1778408 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL1162958 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL1778393 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL1778406 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL1778407 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL1778391 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL470808 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL1778399 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL1778402 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL1778411 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL1778293 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL1778294 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL1778292 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL1778398 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL1778400 | — | IC50 | = | 17000.0 | nM | 4.77 |