Assay Detail
Binding
CHEMBL2406233
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of chicken wild-type cSRC (251 to 533)-mediated phosphorylation of biotinylated poly-Glu-Tyr expressed in Escherichia coli BL21(DE3) preincubated for 30 to 60 mins prior to substrate addition by TR-FRET assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Gallus gallus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Proto-oncogene tyrosine-protein kinase Src (CHEMBL3655) ↗| Type | SINGLE PROTEIN |
| Organism | Gallus gallus |
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 | 17 | 7.52 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1171837 | PONATINIB | 4.0 | 1 | 9.05 |
| CHEMBL2403819 | — | — | 1 | 8.96 |
| CHEMBL2403820 | — | — | 1 | 8.96 |
| CHEMBL2403818 | — | — | 1 | 8.92 |
| CHEMBL2403821 | — | — | 1 | 8.33 |
| CHEMBL2403815 | — | — | 1 | 7.92 |
| CHEMBL510516 | — | — | 1 | 7.85 |
| CHEMBL2403814 | — | — | 1 | 7.70 |
| CHEMBL2403813 | — | — | 1 | 7.47 |
| CHEMBL2403816 | — | — | 1 | 7.42 |
| CHEMBL2403874 | — | — | 1 | 7.41 |
| CHEMBL522892 | DOVITINIB | 3.0 | 1 | 7.09 |
| CHEMBL2403817 | — | — | 1 | 6.84 |
| CHEMBL2403875 | — | — | 1 | 6.52 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 6.26 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | 5.55 |
| CHEMBL2403879 | — | — | 1 | 5.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1171837 | PONATINIB | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL2403819 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL2403820 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL2403818 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL2403821 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL2403815 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL510516 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2403814 | — | IC50 | = | 19.9 | nM | 7.70 |
| CHEMBL2403813 | — | IC50 | = | 34.2 | nM | 7.47 |
| CHEMBL2403816 | — | IC50 | = | 37.9 | nM | 7.42 |
| CHEMBL2403874 | — | IC50 | = | 39.3 | nM | 7.41 |
| CHEMBL522892 | DOVITINIB | IC50 | = | 80.8 | nM | 7.09 |
| CHEMBL2403817 | — | IC50 | = | 145.0 | nM | 6.84 |
| CHEMBL2403875 | — | IC50 | = | 304.0 | nM | 6.52 |
| CHEMBL535 | SUNITINIB | IC50 | = | 555.0 | nM | 6.26 |
| CHEMBL941 | IMATINIB | IC50 | = | 2784.0 | nM | 5.55 |
| CHEMBL2403879 | — | IC50 | = | 3037.0 | nM | 5.52 |