Assay Detail
Binding
CHEMBL5680951
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Inhibition of human N-terminal his tagged native ABL1 (229 to 499 residues) expressed in Sf9 cells using ABLtide as substrate preincubated for 2 hrs followed by ATP addition and measured every 2 mins for 2.5 hrs by spectrophotometric analysis
5
Total Activities
5
Compounds Tested
1
Activity Types
2
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Conformational control inhibition of the BCR-ABL1 tyrosine kinase, including the gatekeeper T315I mutant, by the switch-control inhibitor DCC-2036.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 7.66 | 9.10 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| EFO_ID | EFO_ID | - | — | MONDO:0004992 |
| EFO_TERM | EFO_TERM | - | — | cancer |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1738757 | REBASTINIB | 2.0 | 1 | 9.10 |
| CHEMBL5687006 | — | — | 1 | 8.05 |
| CHEMBL1738759 | — | — | 1 | 7.24 |
| CHEMBL5686996 | — | — | 1 | 7.06 |
| CHEMBL5687009 | — | — | 1 | 6.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1738757 | REBASTINIB | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL5687006 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1738759 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL5686996 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL5687009 | — | IC50 | = | 140.0 | nM | 6.85 |