Assay Detail
Binding
CHEMBL3810822
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Inhibition of human wild type BCR-ABL 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 | 9.64 | 10.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3808884 | — | — | 1 | 10.40 |
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 10.40 |
| CHEMBL1171837 | PONATINIB | 4.0 | 1 | 10.30 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | 7.47 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | - |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | - |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | - |
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3808884 | — | EC50 | = | 0.04 | nM | 10.40 |
| CHEMBL5416410 | DASATINIB | EC50 | = | 0.04 | nM | 10.40 |
| CHEMBL1171837 | PONATINIB | EC50 | = | 0.05 | nM | 10.30 |
| CHEMBL941 | IMATINIB | EC50 | = | 34.0 | nM | 7.47 |
| CHEMBL553 | ERLOTINIB | EC50 | - | — | - | |
| CHEMBL535 | SUNITINIB | EC50 | - | — | - | |
| CHEMBL1336 | SORAFENIB | EC50 | - | — | - | |
| CHEMBL1173655 | AFATINIB | EC50 | - | — | - |