Assay Detail
Binding
CHEMBL5716101
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of GST tagged Src (unknown origin) assessed as inhibition of phosphorylation using PTK biotinylated peptide substrate 2 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 |
Target
Proto-oncogene tyrosine-protein kinase Src (CHEMBL267) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 9.10 | 9.10 |
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 | 9.10 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | - |
| CHEMBL255863 | NILOTINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1421 | DASATINIB ANHYDROUS | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL941 | IMATINIB | IC50 | > | 5000.0 | nM | - |
| CHEMBL255863 | NILOTINIB | IC50 | > | 5000.0 | nM | - |