Assay Detail
Functional
CHEMBL2318560
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Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL M351T mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
4
Total Activities
4
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
Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 8.64 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 9.70 |
| CHEMBL2316582 | OLVEREMBATINIB | 3.0 | 1 | 9.70 |
| CHEMBL255863 | NILOTINIB | 4.0 | 1 | 8.52 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | 6.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5416410 | DASATINIB | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL2316582 | OLVEREMBATINIB | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL255863 | NILOTINIB | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL941 | IMATINIB | IC50 | = | 240.0 | nM | 6.62 |