Assay Detail
Binding
CHEMBL5716088
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Inhibition of GST tagged Abl Y253F 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 | 7.44 | 9.40 |
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 | 9.40 |
| CHEMBL255863 | NILOTINIB | 4.0 | 1 | 7.55 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | 5.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1421 | DASATINIB ANHYDROUS | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL255863 | NILOTINIB | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL941 | IMATINIB | IC50 | = | 4300.0 | nM | 5.37 |