Assay Detail
Functional
CHEMBL2318554
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Cytotoxicity against human KU812 cells expressing BCR-ABL assessed as growth inhibition after 72 hrs by CCK-8 assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | KU812 |
| 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 | 2 | 9.09 | 9.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2316582 | OLVEREMBATINIB | 3.0 | 1 | 9.89 |
| CHEMBL428647 | PACLITAXEL | 4.0 | 1 | 8.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2316582 | OLVEREMBATINIB | IC50 | = | 0.13 | nM | 9.89 |
| CHEMBL428647 | PACLITAXEL | IC50 | = | 5.3 | nM | 8.28 |