Assay Detail
Binding
CHEMBL3887349
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Kinase Activity: The compounds prepared in Examples were tested for inhibitory activity against three subtypes of RAF, i.e., RAF1 Y340D Y341D (C-RAF), B-RAF normal type and B-RAF.sup.V600E using Kinase Profiling Service (Invitrogen, U.S.) according to the manufacturer's instructions. The levels of enzymatic inhibition of the compounds were calculated as percent inhibition at various concentrations.
8
Total Activities
8
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
Thieno[3,2-D]pyrimidine derivatives having inhibitory activity for protein kinases
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 7.86 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3944137 | — | — | 1 | 8.30 |
| CHEMBL3982491 | — | — | 1 | 8.15 |
| CHEMBL3977543 | BELVARAFENIB | 2.0 | 1 | 8.15 |
| CHEMBL3954810 | — | — | 1 | 8.05 |
| CHEMBL3969260 | — | — | 1 | 7.66 |
| CHEMBL3965806 | — | — | 1 | 7.58 |
| CHEMBL3915720 | — | — | 1 | 7.51 |
| CHEMBL3894601 | — | — | 1 | 7.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3944137 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3982491 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3977543 | BELVARAFENIB | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3954810 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3969260 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3965806 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3915720 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL3894601 | — | IC50 | = | 32.0 | nM | 7.50 |