Assay Detail
Functional
CHEMBL1787643
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Antiproliferative activity against mouse BA/F3 cells expressing ABL T315I mutant
19
Total Activities
19
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 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 7.49 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1784635 | — | — | 1 | 8.40 |
| CHEMBL1784641 | — | — | 1 | 8.26 |
| CHEMBL1236871 | — | — | 1 | 8.24 |
| CHEMBL1784634 | — | — | 1 | 8.12 |
| CHEMBL1784637 | — | — | 1 | 8.08 |
| CHEMBL1171837 | PONATINIB | 4.0 | 1 | 8.06 |
| CHEMBL1784627 | — | — | 1 | 8.02 |
| CHEMBL1784638 | — | — | 1 | 7.97 |
| CHEMBL1784628 | — | — | 1 | 7.87 |
| CHEMBL1784640 | — | — | 1 | 7.76 |
| CHEMBL1784629 | — | — | 1 | 7.75 |
| CHEMBL1784625 | — | — | 1 | 7.34 |
| CHEMBL1784636 | — | — | 1 | 7.19 |
| CHEMBL1784639 | — | — | 1 | 7.19 |
| CHEMBL1784626 | — | — | 1 | 7.19 |
| CHEMBL1784633 | — | — | 1 | 7.16 |
| CHEMBL1784630 | — | — | 1 | 6.29 |
| CHEMBL1784632 | — | — | 1 | 6.15 |
| CHEMBL1784631 | — | — | 1 | 5.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1784635 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1784641 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL1236871 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL1784634 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL1784637 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL1171837 | PONATINIB | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL1784627 | — | IC50 | = | 9.6 | nM | 8.02 |
| CHEMBL1784638 | — | IC50 | = | 10.8 | nM | 7.97 |
| CHEMBL1784628 | — | IC50 | = | 13.4 | nM | 7.87 |
| CHEMBL1784640 | — | IC50 | = | 17.5 | nM | 7.76 |
| CHEMBL1784629 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL1784625 | — | IC50 | = | 45.5 | nM | 7.34 |
| CHEMBL1784636 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL1784639 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL1784626 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL1784633 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL1784630 | — | IC50 | = | 519.0 | nM | 6.29 |
| CHEMBL1784632 | — | IC50 | = | 709.0 | nM | 6.15 |
| CHEMBL1784631 | — | IC50 | = | 5738.0 | nM | 5.24 |