Assay Detail
Binding
CHEMBL3404063
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PDGFR-beta in human U251 cells compound pretreated for 60 min before PDGF-BB stimulation for 10 mins by phosphotyrosine ELISA cytoblot method
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | U-251 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Platelet-derived growth factor receptor beta (CHEMBL1913) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The design, synthesis and biological evaluation of conformationally restricted 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multi-targeted receptor tyrosine kinase and microtubule inhibitors as potential antitumor agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 7.21 | 7.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3297898 | — | — | 1 | 7.64 |
| CHEMBL3403513 | — | — | 1 | 7.61 |
| CHEMBL3403514 | — | — | 1 | 7.60 |
| CHEMBL3403509 | — | — | 1 | 7.39 |
| CHEMBL3403512 | — | — | 1 | 7.30 |
| CHEMBL3403517 | — | — | 1 | 7.24 |
| CHEMBL3403510 | — | — | 1 | 7.18 |
| CHEMBL3403515 | — | — | 1 | 7.13 |
| CHEMBL3403518 | — | — | 1 | 7.08 |
| CHEMBL3403519 | — | — | 1 | 6.88 |
| CHEMBL3403511 | — | — | 1 | 6.78 |
| CHEMBL3403516 | — | — | 1 | 6.70 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | - |
| CHEMBL276711 | SEMAXANIB | 3.0 | 1 | - |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3297898 | — | IC50 | = | 22.8 | nM | 7.64 |
| CHEMBL3403513 | — | IC50 | = | 24.6 | nM | 7.61 |
| CHEMBL3403514 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3403509 | — | IC50 | = | 40.4 | nM | 7.39 |
| CHEMBL3403512 | — | IC50 | = | 50.1 | nM | 7.30 |
| CHEMBL3403517 | — | IC50 | = | 58.2 | nM | 7.24 |
| CHEMBL3403510 | — | IC50 | = | 66.1 | nM | 7.18 |
| CHEMBL3403515 | — | IC50 | = | 73.2 | nM | 7.13 |
| CHEMBL3403518 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL3403519 | — | IC50 | = | 132.0 | nM | 6.88 |
| CHEMBL3403511 | — | IC50 | = | 166.3 | nM | 6.78 |
| CHEMBL3403516 | — | IC50 | = | 198.0 | nM | 6.70 |
| CHEMBL553 | ERLOTINIB | IC50 | - | — | - | |
| CHEMBL276711 | SEMAXANIB | IC50 | - | — | - | |
| CHEMBL535 | SUNITINIB | IC50 | = | 83.1 | nM | - |