Assay Detail
Functional
CHEMBL768950
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Inhibition of Platelet-derived growth factor induced 3T3 cell proliferation
13
Total Activities
13
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | 3T3 |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Platelet-derived growth factor receptor (CHEMBL2096980) ↗| Type | PROTEIN COMPLEX |
| Organism | Mus musculus |
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 | 12 | 6.67 | 8.00 |
| NT | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 8.00 |
| CHEMBL13983 | — | — | 1 | 7.70 |
| CHEMBL268731 | — | — | 1 | 7.00 |
| CHEMBL13485 | SU-11652 | — | 1 | 7.00 |
| CHEMBL13629 | — | — | 1 | 7.00 |
| CHEMBL13608 | TOCERANIB | 2.0 | 1 | 7.00 |
| CHEMBL13976 | — | — | 1 | 7.00 |
| CHEMBL274654 | ORANTINIB | 3.0 | 1 | 6.00 |
| CHEMBL267293 | — | — | 1 | 6.00 |
| CHEMBL275117 | — | — | 1 | 6.00 |
| CHEMBL276711 | SEMAXANIB | 3.0 | 1 | 4.69 |
| CHEMBL430155 | — | — | 1 | - |
| CHEMBL13354 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL535 | SUNITINIB | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL13983 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL268731 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL13485 | SU-11652 | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL13629 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL13608 | TOCERANIB | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL13976 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL274654 | ORANTINIB | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL267293 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL275117 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL276711 | SEMAXANIB | IC50 | = | 20300.0 | nM | 4.69 |
| CHEMBL430155 | — | NT | - | — | - | |
| CHEMBL13354 | — | IC50 | = | - | nM | - |