Assay Detail
Binding
CHEMBL770476
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PDGF-stimulated Platelet-derived growth factor receptor autophosphorylation in rat aortic vascular smooth muscle cells (RAVSMCs) after 2 hr
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Expert |
Target
Platelet-derived growth factor receptor (PDGFr) (CHEMBL2111344) ↗| Type | PROTEIN FAMILY |
| Organism | Rattus norvegicus |
Publication
Synthesis and tyrosine kinase inhibitory activity of a series of 2-amino-8H-pyrido[2,3-d]pyrimidines: identification of potent, selective platelet-derived growth factor receptor tyrosine kinase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 8.16 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL134851 | — | — | 1 | 8.82 |
| CHEMBL434448 | — | — | 1 | 8.34 |
| CHEMBL49120 | PD-0166285 | 1.0 | 1 | 8.19 |
| CHEMBL136332 | — | — | 1 | 7.27 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL134851 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL434448 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL49120 | PD-0166285 | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL136332 | — | IC50 | = | 54.0 | nM | 7.27 |