Assay Detail
Binding
CHEMBL5108948
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Inhibition of Abl T315I mutant (unknown origin)
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
The progress of small-molecules and degraders against BCR-ABL for the treatment of CML.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 8.11 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL495727 | AT-9283 | 2.0 | 1 | 8.40 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 8.40 |
| CHEMBL1738757 | REBASTINIB | 2.0 | 1 | 8.30 |
| CHEMBL3545085 | XL-228 | 1.0 | 1 | 7.85 |
| CHEMBL384575 | — | — | 1 | 7.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL495727 | AT-9283 | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1908397 | KW-2449 | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1738757 | REBASTINIB | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3545085 | XL-228 | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL384575 | — | IC50 | = | 25.0 | nM | 7.60 |