Assay Detail
Binding
CHEMBL2406229
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of ABL T315I mutant (unknown origin)-mediated phosphorylation of biotinylated poly-Glu-Tyr preincubated for 30 to 60 mins prior to substrate addition by TR-FRET assay
13
Total Activities
13
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 |
Publication
Targeting gain of function and resistance mutations in Abl and KIT by hybrid compound design.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 6.62 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1171837 | PONATINIB | 4.0 | 1 | 9.00 |
| CHEMBL2403815 | — | — | 1 | 7.09 |
| CHEMBL2403816 | — | — | 1 | 6.92 |
| CHEMBL510516 | — | — | 1 | 6.85 |
| CHEMBL2403820 | — | — | 1 | 6.75 |
| CHEMBL522892 | DOVITINIB | 3.0 | 1 | 6.64 |
| CHEMBL2403814 | — | — | 1 | 6.45 |
| CHEMBL2403818 | — | — | 1 | 6.36 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 6.30 |
| CHEMBL2403813 | — | — | 1 | 6.25 |
| CHEMBL2403821 | — | — | 1 | 6.09 |
| CHEMBL2403819 | — | — | 1 | 5.93 |
| CHEMBL2403817 | — | — | 1 | 5.44 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1171837 | PONATINIB | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL2403815 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL2403816 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL510516 | — | IC50 | = | 141.0 | nM | 6.85 |
| CHEMBL2403820 | — | IC50 | = | 176.0 | nM | 6.75 |
| CHEMBL522892 | DOVITINIB | IC50 | = | 228.0 | nM | 6.64 |
| CHEMBL2403814 | — | IC50 | = | 355.0 | nM | 6.45 |
| CHEMBL2403818 | — | IC50 | = | 441.0 | nM | 6.36 |
| CHEMBL535 | SUNITINIB | IC50 | = | 504.0 | nM | 6.30 |
| CHEMBL2403813 | — | IC50 | = | 561.0 | nM | 6.25 |
| CHEMBL2403821 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL2403819 | — | IC50 | = | 1170.0 | nM | 5.93 |
| CHEMBL2403817 | — | IC50 | = | 3620.0 | nM | 5.44 |