Assay Detail
Binding
CHEMBL5730037
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Kinase Activity: The compounds prepared in Examples were tested for inhibitory activity against FMS, DDR1 and DDR2 kinases using Kinase Screening and Profiling Service (Invitrogen, U.S.).
15
Total Activities
5
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Macrophage colony-stimulating factor 1 receptor (CHEMBL1844) ↗| 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 | 5 | 7.99 | 9.00 |
| kon | 5 | - | - |
| k_off | 5 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3969260 | — | — | 3 | 9.00 |
| CHEMBL3944137 | — | — | 3 | 8.40 |
| CHEMBL3977543 | BELVARAFENIB | 2.0 | 3 | 8.00 |
| CHEMBL3915720 | — | — | 3 | 7.30 |
| CHEMBL3954810 | — | — | 3 | 7.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3969260 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3944137 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3977543 | BELVARAFENIB | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3915720 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL3954810 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL3969260 | — | kon | = | - | — | - |
| CHEMBL3969260 | — | k_off | = | - | s-1 | - |
| CHEMBL3954810 | — | kon | = | - | — | - |
| CHEMBL3954810 | — | k_off | = | - | s-1 | - |
| CHEMBL3944137 | — | kon | = | - | — | - |
| CHEMBL3944137 | — | k_off | = | - | s-1 | - |
| CHEMBL3915720 | — | kon | = | - | — | - |
| CHEMBL3915720 | — | k_off | = | - | s-1 | - |
| CHEMBL3977543 | BELVARAFENIB | kon | = | - | — | - |
| CHEMBL3977543 | BELVARAFENIB | k_off | = | - | s-1 | - |