Assay Detail
Binding
CHEMBL4383512
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of active wild type His-tagged ABL T315I mutant (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells using ABLtide as substrate after 1 hr by ADP-Glo assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants including T315I for chronic myeloid leukemia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 9.70 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1289926 | AXITINIB | 4.0 | 1 | 9.70 |
| CHEMBL4439424 | — | — | 1 | 9.70 |
| CHEMBL4519289 | — | — | 1 | 9.70 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1289926 | AXITINIB | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4439424 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4519289 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL941 | IMATINIB | IC50 | > | 10000.0 | nM | - |