Assay Detail
Binding
CHEMBL4180809
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human N-terminal GST-His6 tagged PDGFRalpha (Q551 to L1089 residues) expressed in Sf9 insect cells using poly(Ala,Glu,Lys,Tyr)6:2:5:1 hydrobromide as substrate in presence of [gamma-33P]ATP
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Platelet-derived growth factor receptor alpha (CHEMBL2007) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Trisubstituted purine inhibitors of PDGFRα and their antileukemic activity in the human eosinophilic cell line EOL-1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 6.39 | 7.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4218356 | — | — | 1 | 7.23 |
| CHEMBL4209971 | — | — | 1 | 7.22 |
| CHEMBL4210919 | — | — | 1 | 7.18 |
| CHEMBL4205604 | — | — | 1 | 7.18 |
| CHEMBL4210474 | — | — | 1 | 7.02 |
| CHEMBL4214422 | — | — | 1 | 6.82 |
| CHEMBL4207053 | — | — | 1 | 6.81 |
| CHEMBL4214362 | — | — | 1 | 6.81 |
| CHEMBL4202703 | — | — | 1 | 6.80 |
| CHEMBL4207048 | — | — | 1 | 6.73 |
| CHEMBL4218779 | — | — | 1 | 6.71 |
| CHEMBL4211413 | — | — | 1 | 6.54 |
| CHEMBL4206527 | — | — | 1 | 6.34 |
| CHEMBL4216607 | — | — | 1 | 5.96 |
| CHEMBL4210897 | — | — | 1 | 5.91 |
| CHEMBL4209694 | — | — | 1 | 5.85 |
| CHEMBL4215315 | — | — | 1 | 5.83 |
| CHEMBL4207999 | — | — | 1 | 5.50 |
| CHEMBL4203120 | — | — | 1 | 5.32 |
| CHEMBL4218942 | — | — | 1 | 5.29 |
| CHEMBL4214781 | — | — | 1 | 5.12 |
| CHEMBL367625 | — | — | 1 | - |
| CHEMBL4205769 | — | — | 1 | - |
| CHEMBL4218867 | — | — | 1 | - |
| CHEMBL554 | LAPATINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4218356 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL4209971 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4210919 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL4205604 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL4210474 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL4214422 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4207053 | — | IC50 | = | 154.0 | nM | 6.81 |
| CHEMBL4214362 | — | IC50 | = | 156.0 | nM | 6.81 |
| CHEMBL4202703 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4207048 | — | IC50 | = | 187.0 | nM | 6.73 |
| CHEMBL4218779 | — | IC50 | = | 195.0 | nM | 6.71 |
| CHEMBL4211413 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL4206527 | — | IC50 | = | 452.0 | nM | 6.34 |
| CHEMBL4216607 | — | IC50 | = | 1090.0 | nM | 5.96 |
| CHEMBL4210897 | — | IC50 | = | 1233.0 | nM | 5.91 |
| CHEMBL4209694 | — | IC50 | = | 1412.0 | nM | 5.85 |
| CHEMBL4215315 | — | IC50 | = | 1496.0 | nM | 5.83 |
| CHEMBL4207999 | — | IC50 | = | 3197.0 | nM | 5.50 |
| CHEMBL4203120 | — | IC50 | = | 4739.0 | nM | 5.32 |
| CHEMBL4218942 | — | IC50 | = | 5099.0 | nM | 5.29 |
| CHEMBL4214781 | — | IC50 | = | 7655.0 | nM | 5.12 |
| CHEMBL367625 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4205769 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4218867 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL554 | LAPATINIB | IC50 | > | 20000.0 | nM | - |