Assay Detail
Binding
CHEMBL5716090
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of GST tagged Abl E255K mutant (unknown origin) assessed as inhibition of phosphorylation using biotin-EAIYAAPFAKKK-amide as substrate preincubated for 5 mins followed by [gamma-32P]ATP addition
3
Total Activities
3
Compounds Tested
1
Activity Types
2
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
In vitro activity of Bcr-Abl inhibitors AMN107 and BMS-354825 against clinically relevant imatinib-resistant Abl kinase domain mutants.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 8.47 | 9.70 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| EFO_ID | EFO_ID | - | — | EFO:0000339 |
| EFO_TERM | EFO_TERM | - | — | chronic myelogenous leukemia |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1421 | DASATINIB ANHYDROUS | 4.0 | 1 | 9.70 |
| CHEMBL255863 | NILOTINIB | 4.0 | 1 | 7.23 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1421 | DASATINIB ANHYDROUS | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL255863 | NILOTINIB | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL941 | IMATINIB | IC50 | > | 5000.0 | nM | - |