Assay Detail
Binding
CHEMBL2411892
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Yes1 (unknown origin) by [gamma-33P]-ATP radiolabeled enzyme activity assay
10
Total Activities
10
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
Identification of potent Yes1 kinase inhibitors using a library screening approach.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 8.04 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL217092 | SARACATINIB | 3.0 | 1 | 9.15 |
| CHEMBL522892 | DOVITINIB | 3.0 | 1 | 8.85 |
| CHEMBL1738757 | REBASTINIB | 2.0 | 1 | 8.82 |
| CHEMBL457614 | — | — | 1 | 8.52 |
| CHEMBL587723 | AEE-788 | 2.0 | 1 | 7.88 |
| CHEMBL218632 | — | — | 1 | 7.66 |
| CHEMBL478629 | DORSOMORPHIN | — | 1 | 7.53 |
| CHEMBL2144069 | — | — | 1 | 7.29 |
| CHEMBL1952329 | SGI-1776 | 1.0 | 1 | 6.62 |
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL217092 | SARACATINIB | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL522892 | DOVITINIB | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL1738757 | REBASTINIB | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL457614 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL587723 | AEE-788 | IC50 | = | 13.1 | nM | 7.88 |
| CHEMBL218632 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL478629 | DORSOMORPHIN | IC50 | = | 29.8 | nM | 7.53 |
| CHEMBL2144069 | — | IC50 | = | 51.2 | nM | 7.29 |
| CHEMBL1952329 | SGI-1776 | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL5416410 | DASATINIB | IC50 | < | 1.0 | nM | - |