Assay Detail
Binding
CHEMBL4012622
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of cKIT (unknown origin) using FAM-labeled peptide as substrate preincubated for 10 mins followed by substrate addition in presence of ATP by mobility shift assay
50
Total Activities
50
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
Mast/stem cell growth factor receptor Kit (CHEMBL1936) ↗| 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 | 50 | 6.98 | 8.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4074755 | — | — | 1 | 8.85 |
| CHEMBL4101428 | — | — | 1 | 8.77 |
| CHEMBL4091975 | — | — | 1 | 8.72 |
| CHEMBL4103605 | — | — | 1 | 8.68 |
| CHEMBL4072731 | — | — | 1 | 8.62 |
| CHEMBL4083050 | — | — | 1 | 8.62 |
| CHEMBL4064941 | — | — | 1 | 8.59 |
| CHEMBL4063380 | — | — | 1 | 8.46 |
| CHEMBL4099718 | — | — | 1 | 8.44 |
| CHEMBL4100492 | — | — | 1 | 8.43 |
| CHEMBL4059958 | — | — | 1 | 8.43 |
| CHEMBL4074518 | — | — | 1 | 8.41 |
| CHEMBL4074745 | — | — | 1 | 8.21 |
| CHEMBL4066302 | — | — | 1 | 8.14 |
| CHEMBL4063368 | — | — | 1 | 8.06 |
| CHEMBL4084878 | — | — | 1 | 8.03 |
| CHEMBL4073536 | — | — | 1 | 7.92 |
| CHEMBL4092638 | — | — | 1 | 7.92 |
| CHEMBL4103890 | — | — | 1 | 7.85 |
| CHEMBL4104034 | — | — | 1 | 7.72 |
| CHEMBL4071160 | — | — | 1 | 7.70 |
| CHEMBL4085962 | — | — | 1 | 7.70 |
| CHEMBL4071997 | — | — | 1 | 7.58 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | 7.39 |
| CHEMBL4078084 | — | — | 1 | 7.29 |
| CHEMBL4092765 | — | — | 1 | 7.11 |
| CHEMBL4085010 | — | — | 1 | 6.92 |
| CHEMBL4085974 | — | — | 1 | 6.84 |
| CHEMBL4079775 | — | — | 1 | 6.70 |
| CHEMBL4101438 | — | — | 1 | 6.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4074755 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL4101428 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4091975 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL4103605 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL4072731 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL4083050 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL4064941 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL4063380 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL4099718 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL4100492 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL4059958 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL4074518 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL4074745 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL4066302 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL4063368 | — | IC50 | = | 8.7 | nM | 8.06 |
| CHEMBL4084878 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL4073536 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4092638 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4103890 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4104034 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4071160 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4085962 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4071997 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL941 | IMATINIB | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL4078084 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL4092765 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL4085010 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4085974 | — | IC50 | = | 144.0 | nM | 6.84 |
| CHEMBL4079775 | — | IC50 | = | 201.0 | nM | 6.70 |
| CHEMBL4101438 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL4103897 | — | IC50 | = | 318.0 | nM | 6.50 |
| CHEMBL4083910 | — | IC50 | = | 397.0 | nM | 6.40 |
| CHEMBL4093721 | — | IC50 | = | 553.0 | nM | 6.26 |
| CHEMBL4066145 | — | IC50 | = | 1416.0 | nM | 5.85 |
| CHEMBL4088552 | — | IC50 | = | 1831.0 | nM | 5.74 |
| CHEMBL4087656 | — | IC50 | = | 1949.0 | nM | 5.71 |
| CHEMBL4099624 | — | IC50 | = | 2225.0 | nM | 5.65 |
| CHEMBL4096271 | — | IC50 | = | 2402.0 | nM | 5.62 |
| CHEMBL4062187 | — | IC50 | = | 4581.0 | nM | 5.34 |
| CHEMBL4069008 | — | IC50 | = | 4794.0 | nM | 5.32 |
| CHEMBL4100372 | — | IC50 | = | 6438.0 | nM | 5.19 |
| CHEMBL4081793 | — | IC50 | = | 6768.0 | nM | 5.17 |
| CHEMBL4060326 | — | IC50 | = | 10890.0 | nM | 4.96 |
| CHEMBL4085020 | — | IC50 | = | 20556.0 | nM | 4.69 |
| CHEMBL4069773 | — | IC50 | = | 21432.0 | nM | 4.67 |
| CHEMBL4102831 | — | IC50 | = | 22056.0 | nM | 4.66 |
| CHEMBL4096971 | — | IC50 | = | 38667.0 | nM | 4.41 |
| CHEMBL4093186 | — | IC50 | = | 46064.0 | nM | 4.34 |
| CHEMBL4096138 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4102648 | — | IC50 | > | 50000.0 | nM | - |