Assay Detail
Binding
CHEMBL3855037
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PDGFRalpha kinase domain (unknown origin) assessed as reduction in probe peptide substrate phosphorylation by capillary electrophoresis
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Platelet-derived growth factor receptor alpha (CHEMBL2007) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Optimization of Platelet-Derived Growth Factor Receptor (PDGFR) Inhibitors for Duration of Action, as an Inhaled Therapy for Lung Remodeling in Pulmonary Arterial Hypertension.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 9.14 | 10.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3904768 | — | — | 1 | 10.05 |
| CHEMBL3979322 | — | — | 1 | 9.74 |
| CHEMBL3940697 | — | — | 1 | 9.72 |
| CHEMBL3915941 | — | — | 1 | 9.70 |
| CHEMBL3913766 | — | — | 1 | 9.49 |
| CHEMBL3975580 | — | — | 1 | 9.28 |
| CHEMBL3950278 | — | — | 1 | 9.12 |
| CHEMBL3985689 | — | — | 1 | 9.02 |
| CHEMBL3947262 | — | — | 1 | 8.92 |
| CHEMBL3955987 | — | — | 1 | 8.89 |
| CHEMBL3895824 | — | — | 1 | 8.89 |
| CHEMBL3902237 | — | — | 1 | 8.80 |
| CHEMBL3967097 | — | — | 1 | 8.49 |
| CHEMBL3971140 | — | — | 1 | 7.89 |
| CHEMBL3983564 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3904768 | — | IC50 | = | 0.09 | nM | 10.05 |
| CHEMBL3979322 | — | IC50 | = | 0.18 | nM | 9.74 |
| CHEMBL3940697 | — | IC50 | = | 0.19 | nM | 9.72 |
| CHEMBL3915941 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL3913766 | — | IC50 | = | 0.32 | nM | 9.49 |
| CHEMBL3975580 | — | IC50 | = | 0.53 | nM | 9.28 |
| CHEMBL3950278 | — | IC50 | = | 0.75 | nM | 9.12 |
| CHEMBL3985689 | — | IC50 | = | 0.96 | nM | 9.02 |
| CHEMBL3947262 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3955987 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3895824 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3902237 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3967097 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL3971140 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3983564 | — | IC50 | < | 0.1 | nM | - |