Assay Detail
Binding
CHEMBL1220002
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of mouse recombinant N-terminal His6-tagged Abl by radiometric kinase assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
The design, synthesis, and evaluation of 8 hybrid DFG-out allosteric kinase inhibitors: a structural analysis of the binding interactions of Gleevec, Nexavar, and BIRB-796.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 6.56 | 8.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1213973 | — | — | 1 | 8.07 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | 7.97 |
| CHEMBL1213974 | — | — | 1 | 7.20 |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | 6.65 |
| CHEMBL1213976 | — | — | 1 | 6.61 |
| CHEMBL1213975 | — | — | 1 | 6.24 |
| CHEMBL1213925 | — | — | 1 | 4.89 |
| CHEMBL103667 | DORAMAPIMOD | 2.0 | 1 | 4.84 |
| CHEMBL1213922 | — | — | 1 | - |
| CHEMBL1213923 | — | — | 1 | - |
| CHEMBL1213924 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1213973 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL941 | IMATINIB | IC50 | = | 10.8 | nM | 7.97 |
| CHEMBL1213974 | — | IC50 | = | 62.6 | nM | 7.20 |
| CHEMBL1336 | SORAFENIB | IC50 | = | 225.9 | nM | 6.65 |
| CHEMBL1213976 | — | IC50 | = | 244.0 | nM | 6.61 |
| CHEMBL1213975 | — | IC50 | = | 572.4 | nM | 6.24 |
| CHEMBL1213925 | — | IC50 | = | 12930.0 | nM | 4.89 |
| CHEMBL103667 | DORAMAPIMOD | IC50 | = | 14600.0 | nM | 4.84 |
| CHEMBL1213922 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL1213923 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL1213924 | — | IC50 | < | 1.0 | nM | - |