Assay Detail
Binding
CHEMBL3755449
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Inhibition of B-Raf V600E mutant (unknown origin) by lantha screen assay
15
Total Activities
15
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
Discovery of EBI-907: A highly potent and orally active B-Raf(V600E) inhibitor for the treatment of melanoma and associated cancers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 8.06 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3752213 | — | — | 1 | 10.00 |
| CHEMBL3753260 | — | — | 1 | 9.22 |
| CHEMBL3754618 | — | — | 1 | 9.10 |
| CHEMBL3752762 | — | — | 1 | 9.10 |
| CHEMBL3752478 | — | — | 1 | 8.15 |
| CHEMBL3751896 | — | — | 1 | 8.15 |
| CHEMBL2023335 | — | — | 1 | 8.06 |
| CHEMBL3752457 | — | — | 1 | 7.96 |
| CHEMBL3753363 | — | — | 1 | 7.77 |
| CHEMBL3751892 | — | — | 1 | 7.70 |
| CHEMBL3753663 | — | — | 1 | 7.16 |
| CHEMBL3753972 | — | — | 1 | 7.10 |
| CHEMBL3753129 | — | — | 1 | 6.66 |
| CHEMBL1230020 | PLX-4720 | — | 1 | 6.66 |
| CHEMBL3754116 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3752213 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL3753260 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3754618 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL3752762 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL3752478 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3751896 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL2023335 | — | IC50 | = | 8.7 | nM | 8.06 |
| CHEMBL3752457 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3753363 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3751892 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3753663 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL3753972 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL3753129 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL1230020 | PLX-4720 | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL3754116 | — | IC50 | > | 30.0 | nM | - |