Assay Detail
Binding
CHEMBL768949
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Platelet-derived growth factor receptor beta (PDGF-Rbeta)
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Platelet-derived growth factor receptor beta (CHEMBL1913) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosine kinase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 8.07 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL13976 | — | — | 1 | 9.30 |
| CHEMBL268731 | — | — | 1 | 9.00 |
| CHEMBL13608 | TOCERANIB | 2.0 | 1 | 9.00 |
| CHEMBL13354 | — | — | 1 | 8.70 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 8.70 |
| CHEMBL13485 | SU-11652 | — | 1 | 8.52 |
| CHEMBL13983 | — | — | 1 | 8.52 |
| CHEMBL13629 | — | — | 1 | 8.30 |
| CHEMBL267293 | — | — | 1 | 8.00 |
| CHEMBL275117 | — | — | 1 | 7.77 |
| CHEMBL274654 | ORANTINIB | 3.0 | 1 | 7.22 |
| CHEMBL430155 | — | — | 1 | 7.22 |
| CHEMBL276711 | SEMAXANIB | 3.0 | 1 | 4.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL13976 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL268731 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL13608 | TOCERANIB | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL13354 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL535 | SUNITINIB | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL13485 | SU-11652 | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL13983 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL13629 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL267293 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL275117 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL274654 | ORANTINIB | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL430155 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL276711 | SEMAXANIB | IC50 | = | 22900.0 | nM | 4.64 |