Assay Detail
Binding
CHEMBL4020522
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of KIT V559D/V654A double mutant (unknown origin) using biotinylated poly-Glu-Tyr as substrate preincubated for 30 mins followed by substrate addition in presence of ATP by TR-FRET assay
28
Total Activities
28
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
Inhibitors to Overcome Secondary Mutations in the Stem Cell Factor Receptor KIT.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 6.39 | 6.90 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 6.90 |
| CHEMBL1171837 | PONATINIB | 4.0 | 1 | 6.87 |
| CHEMBL4101206 | — | — | 1 | 6.61 |
| CHEMBL4077510 | — | — | 1 | 6.60 |
| CHEMBL4100222 | — | — | 1 | 6.50 |
| CHEMBL4076193 | — | — | 1 | 6.11 |
| CHEMBL4103644 | — | — | 1 | 6.04 |
| CHEMBL4090058 | — | — | 1 | 5.96 |
| CHEMBL1784625 | — | — | 1 | 5.96 |
| CHEMBL4070641 | — | — | 1 | - |
| CHEMBL4071683 | — | — | 1 | - |
| CHEMBL4092478 | — | — | 1 | - |
| CHEMBL4082210 | — | — | 1 | - |
| CHEMBL4062017 | — | — | 1 | - |
| CHEMBL4085713 | — | — | 1 | - |
| CHEMBL1946170 | REGORAFENIB | 4.0 | 1 | - |
| CHEMBL4093459 | — | — | 1 | - |
| CHEMBL4097771 | — | — | 1 | - |
| CHEMBL4075321 | — | — | 1 | - |
| CHEMBL4092506 | — | — | 1 | - |
| CHEMBL4077028 | — | — | 1 | - |
| CHEMBL4074329 | — | — | 1 | - |
| CHEMBL4094827 | — | — | 1 | - |
| CHEMBL4065711 | — | — | 1 | - |
| CHEMBL4087133 | — | — | 1 | - |
| CHEMBL4103510 | — | — | 1 | - |
| CHEMBL4079252 | — | — | 1 | - |
| CHEMBL941 | IMATINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL535 | SUNITINIB | IC50 | = | 124.9 | nM | 6.90 |
| CHEMBL1171837 | PONATINIB | IC50 | = | 136.0 | nM | 6.87 |
| CHEMBL4101206 | — | IC50 | = | 246.6 | nM | 6.61 |
| CHEMBL4077510 | — | IC50 | = | 252.5 | nM | 6.60 |
| CHEMBL4100222 | — | IC50 | = | 313.5 | nM | 6.50 |
| CHEMBL4076193 | — | IC50 | = | 777.2 | nM | 6.11 |
| CHEMBL4103644 | — | IC50 | = | 908.3 | nM | 6.04 |
| CHEMBL4090058 | — | IC50 | = | 1084.7 | nM | 5.96 |
| CHEMBL1784625 | — | IC50 | = | 1101.6 | nM | 5.96 |
| CHEMBL4070641 | — | IC50 | - | — | - | |
| CHEMBL4071683 | — | IC50 | - | — | - | |
| CHEMBL4092478 | — | IC50 | - | — | - | |
| CHEMBL4082210 | — | IC50 | - | — | - | |
| CHEMBL4062017 | — | IC50 | - | — | - | |
| CHEMBL4085713 | — | IC50 | - | — | - | |
| CHEMBL1946170 | REGORAFENIB | IC50 | - | — | - | |
| CHEMBL4093459 | — | IC50 | - | — | - | |
| CHEMBL4097771 | — | IC50 | - | — | - | |
| CHEMBL4075321 | — | IC50 | - | — | - | |
| CHEMBL4092506 | — | IC50 | - | — | - | |
| CHEMBL4077028 | — | IC50 | - | — | - | |
| CHEMBL4074329 | — | IC50 | - | — | - | |
| CHEMBL4094827 | — | IC50 | - | — | - | |
| CHEMBL4065711 | — | IC50 | - | — | - | |
| CHEMBL4087133 | — | IC50 | - | — | - | |
| CHEMBL4103510 | — | IC50 | - | — | - | |
| CHEMBL4079252 | — | IC50 | - | — | - | |
| CHEMBL941 | IMATINIB | IC50 | - | — | - |