Assay Detail
Functional
CHEMBL5039652
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Cytotoxicity against mouse BAF3 cells expressing native BCR-ABL assessed as inhibition of cell growth measured after 72 hrs by MTT 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 | 8.29 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 9.15 |
| CHEMBL1171837 | PONATINIB | 4.0 | 1 | 9.05 |
| CHEMBL5093894 | — | — | 1 | 8.68 |
| CHEMBL5089813 | — | — | 1 | 8.57 |
| CHEMBL5089020 | — | — | 1 | 8.46 |
| CHEMBL5083651 | — | — | 1 | 8.03 |
| CHEMBL255863 | NILOTINIB | 4.0 | 1 | 7.93 |
| CHEMBL5081443 | — | — | 1 | 7.51 |
| CHEMBL5078722 | — | — | 1 | 7.20 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5416410 | DASATINIB | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL1171837 | PONATINIB | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL5093894 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL5089813 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL5089020 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL5083651 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL255863 | NILOTINIB | IC50 | = | 11.8 | nM | 7.93 |
| CHEMBL5081443 | — | IC50 | = | 31.2 | nM | 7.51 |
| CHEMBL5078722 | — | IC50 | = | 62.5 | nM | 7.20 |
| CHEMBL941 | IMATINIB | IC50 | > | 100.0 | nM | - |