Assay Detail
Functional
CHEMBL5039655
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Cytotoxicity against mouse BAF3 cells expressing BCR-ABL T315I mutant assessed as inhibition of cell growth measured after 48 hrs by trypan blue assay
10
Total Activities
10
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
Discovery of a Candidate Containing an (<i>S</i>)-3,3-Difluoro-1-(4-methylpiperazin-1-yl)-2,3-dihydro-1<i>H</i>-inden Scaffold as a Highly Potent Pan-Inhibitor of the BCR-ABL Kinase Including the T315I-Resistant Mutant for the Treatment of Chronic Myeloid Leukemia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 7.92 | 8.33 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5093894 | — | — | 1 | 8.33 |
| CHEMBL1171837 | PONATINIB | 4.0 | 1 | 8.02 |
| CHEMBL5089813 | — | — | 1 | 7.96 |
| CHEMBL5089020 | — | — | 1 | 7.91 |
| CHEMBL5083651 | — | — | 1 | 7.40 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | - |
| CHEMBL255863 | NILOTINIB | 4.0 | 1 | - |
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | - |
| CHEMBL5081443 | — | — | 1 | - |
| CHEMBL5078722 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5093894 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL1171837 | PONATINIB | IC50 | = | 9.6 | nM | 8.02 |
| CHEMBL5089813 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5089020 | — | IC50 | = | 12.4 | nM | 7.91 |
| CHEMBL5083651 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL941 | IMATINIB | IC50 | > | 100.0 | nM | - |
| CHEMBL255863 | NILOTINIB | IC50 | > | 100.0 | nM | - |
| CHEMBL5416410 | DASATINIB | IC50 | > | 100.0 | nM | - |
| CHEMBL5081443 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL5078722 | — | IC50 | > | 100.0 | nM | - |