Assay Detail
Binding
CHEMBL4012619
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PDGFRalpha (unknown origin) using FAM-labeled peptide as substrate preincubated for 10 mins followed by substrate addition in presence of ATP by mobility shift assay
60
Total Activities
60
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
Discovery of Potent, Selective Stem Cell Factor Receptor/Platelet Derived Growth Factor Receptor Alpha (c-KIT/PDGFRα) Dual Inhibitor for the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors (GISTs).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 60 | 6.58 | 8.34 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL941 | IMATINIB | 4.0 | 1 | 8.34 |
| CHEMBL4072731 | — | — | 1 | 8.14 |
| CHEMBL223360 | LINIFANIB | 3.0 | 1 | 7.82 |
| CHEMBL4091975 | — | — | 1 | 7.66 |
| CHEMBL4074518 | — | — | 1 | 7.66 |
| CHEMBL4101428 | — | — | 1 | 7.62 |
| CHEMBL4074755 | — | — | 1 | 7.57 |
| CHEMBL4059958 | — | — | 1 | 7.50 |
| CHEMBL4103605 | — | — | 1 | 7.40 |
| CHEMBL4088552 | — | — | 1 | 7.19 |
| CHEMBL4100492 | — | — | 1 | 7.09 |
| CHEMBL4063368 | — | — | 1 | 7.08 |
| CHEMBL4064941 | — | — | 1 | 7.08 |
| CHEMBL4074713 | — | — | 1 | 7.06 |
| CHEMBL4083050 | — | — | 1 | 7.06 |
| CHEMBL4099718 | — | — | 1 | 7.01 |
| CHEMBL4065800 | — | — | 1 | 6.97 |
| CHEMBL4071160 | — | — | 1 | 6.91 |
| CHEMBL4066302 | — | — | 1 | 6.90 |
| CHEMBL4074745 | — | — | 1 | 6.87 |
| CHEMBL4073536 | — | — | 1 | 6.87 |
| CHEMBL4079338 | — | — | 1 | 6.86 |
| CHEMBL4071997 | — | — | 1 | 6.80 |
| CHEMBL4063380 | — | — | 1 | 6.79 |
| CHEMBL4092638 | — | — | 1 | 6.75 |
| CHEMBL4096271 | — | — | 1 | 6.74 |
| CHEMBL4104034 | — | — | 1 | 6.67 |
| CHEMBL4069008 | — | — | 1 | 6.58 |
| CHEMBL4060326 | — | — | 1 | 6.52 |
| CHEMBL4084878 | — | — | 1 | 6.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL941 | IMATINIB | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL4072731 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL223360 | LINIFANIB | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4091975 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4074518 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4101428 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4074755 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4059958 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4103605 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4088552 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL4100492 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL4063368 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL4064941 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL4083050 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL4074713 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL4099718 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL4065800 | — | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL4071160 | — | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL4066302 | — | IC50 | = | 127.0 | nM | 6.90 |
| CHEMBL4074745 | — | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL4073536 | — | IC50 | = | 136.0 | nM | 6.87 |
| CHEMBL4079338 | — | IC50 | = | 137.0 | nM | 6.86 |
| CHEMBL4071997 | — | IC50 | = | 157.0 | nM | 6.80 |
| CHEMBL4063380 | — | IC50 | = | 164.0 | nM | 6.79 |
| CHEMBL4092638 | — | IC50 | = | 176.0 | nM | 6.75 |
| CHEMBL4096271 | — | IC50 | = | 182.0 | nM | 6.74 |
| CHEMBL4104034 | — | IC50 | = | 215.0 | nM | 6.67 |
| CHEMBL4069008 | — | IC50 | = | 262.0 | nM | 6.58 |
| CHEMBL4060326 | — | IC50 | = | 305.0 | nM | 6.52 |
| CHEMBL4084878 | — | IC50 | = | 309.0 | nM | 6.51 |
| CHEMBL4103890 | — | IC50 | = | 313.0 | nM | 6.50 |
| CHEMBL4078084 | — | IC50 | = | 387.0 | nM | 6.41 |
| CHEMBL4085962 | — | IC50 | = | 401.0 | nM | 6.40 |
| CHEMBL4085010 | — | IC50 | = | 411.0 | nM | 6.39 |
| CHEMBL4092765 | — | IC50 | = | 472.0 | nM | 6.33 |
| CHEMBL4100645 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL4085974 | — | IC50 | = | 576.0 | nM | 6.24 |
| CHEMBL4103897 | — | IC50 | = | 732.0 | nM | 6.13 |
| CHEMBL4062187 | — | IC50 | = | 928.0 | nM | 6.03 |
| CHEMBL4087221 | — | IC50 | = | 1081.0 | nM | 5.97 |
| CHEMBL4099624 | — | IC50 | = | 1101.0 | nM | 5.96 |
| CHEMBL4093721 | — | IC50 | = | 1133.0 | nM | 5.95 |
| CHEMBL4101438 | — | IC50 | = | 1123.0 | nM | 5.95 |
| CHEMBL4091741 | — | IC50 | = | 1179.0 | nM | 5.93 |
| CHEMBL4066145 | — | IC50 | = | 1465.0 | nM | 5.83 |
| CHEMBL4101778 | — | IC50 | = | 1572.0 | nM | 5.80 |
| CHEMBL4087656 | — | IC50 | = | 1779.0 | nM | 5.75 |
| CHEMBL4100372 | — | IC50 | = | 4077.0 | nM | 5.39 |
| CHEMBL4102831 | — | IC50 | = | 4608.0 | nM | 5.34 |
| CHEMBL4083910 | — | IC50 | = | 18925.0 | nM | 4.72 |