Assay Detail
Functional
CHEMBL5681162
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Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 Q252H mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| Cell Type | BaF3 |
| Confidence | 1 — Organism |
| 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 | 7.70 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1421 | DASATINIB ANHYDROUS | 4.0 | 1 | 9.52 |
| CHEMBL255863 | NILOTINIB | 4.0 | 1 | 8.29 |
| CHEMBL1738757 | REBASTINIB | 2.0 | 1 | 7.62 |
| CHEMBL572878 | TOZASERTIB | 2.0 | 1 | 6.89 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | 6.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1421 | DASATINIB ANHYDROUS | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL255863 | NILOTINIB | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL1738757 | REBASTINIB | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL572878 | TOZASERTIB | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL941 | IMATINIB | IC50 | = | 700.0 | nM | 6.16 |