Assay Detail
Binding
CHEMBL2406232
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of cSRC T338M 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 | 0 — Uncurated / Unknown |
| 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 | 7.74 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2403820 | — | — | 1 | 9.05 |
| CHEMBL2403819 | — | — | 1 | 8.89 |
| CHEMBL2403818 | — | — | 1 | 8.77 |
| CHEMBL2403821 | — | — | 1 | 8.46 |
| CHEMBL2403815 | — | — | 1 | 8.23 |
| CHEMBL510516 | — | — | 1 | 7.64 |
| CHEMBL2403816 | — | — | 1 | 7.48 |
| CHEMBL2403814 | — | — | 1 | 7.48 |
| CHEMBL522892 | DOVITINIB | 3.0 | 1 | 7.30 |
| CHEMBL2403813 | — | — | 1 | 6.90 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 6.87 |
| CHEMBL1171837 | PONATINIB | 4.0 | 1 | 6.81 |
| CHEMBL2403817 | — | — | 1 | 6.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2403820 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL2403819 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL2403818 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL2403821 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL2403815 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL510516 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL2403816 | — | IC50 | = | 33.3 | nM | 7.48 |
| CHEMBL2403814 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL522892 | DOVITINIB | IC50 | = | 50.1 | nM | 7.30 |
| CHEMBL2403813 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL535 | SUNITINIB | IC50 | = | 134.0 | nM | 6.87 |
| CHEMBL1171837 | PONATINIB | IC50 | = | 156.0 | nM | 6.81 |
| CHEMBL2403817 | — | IC50 | = | 211.0 | nM | 6.68 |