Assay Detail
Binding
CHEMBL3810823
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human BCR-ABL T315I mutant expressed in mouse BAF3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | BaF3 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 8 | 9.13 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1171837 | PONATINIB | 4.0 | 1 | 9.52 |
| CHEMBL3808884 | — | — | 1 | 8.74 |
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | - |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | - |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | - |
| CHEMBL941 | IMATINIB | 4.0 | 1 | - |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | - |
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1171837 | PONATINIB | EC50 | = | 0.3 | nM | 9.52 |
| CHEMBL3808884 | — | EC50 | = | 1.8 | nM | 8.74 |
| CHEMBL5416410 | DASATINIB | EC50 | > | 1000.0 | nM | - |
| CHEMBL553 | ERLOTINIB | EC50 | - | — | - | |
| CHEMBL535 | SUNITINIB | EC50 | > | 1000.0 | nM | - |
| CHEMBL941 | IMATINIB | EC50 | > | 1000.0 | nM | - |
| CHEMBL1336 | SORAFENIB | EC50 | - | — | - | |
| CHEMBL1173655 | AFATINIB | EC50 | - | — | - |