Assay Detail
Functional
CHEMBL5039657
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Cytotoxicity against human KU812 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
10
Total Activities
10
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
Discovery of a Candidate Containing an (<i>S</i>)-3,3-Difluoro-1-(4-methylpiperazin-1-yl)-2,3-dihydro-1<i>H</i>-inden Scaffold as a Highly Potent Pan-Inhibitor of the BCR-ABL Kinase Including the T315I-Resistant Mutant for the Treatment of Chronic Myeloid Leukemia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 9.17 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 10.00 |
| CHEMBL1171837 | PONATINIB | 4.0 | 1 | 10.00 |
| CHEMBL5093894 | — | — | 1 | 10.00 |
| CHEMBL5089813 | — | — | 1 | 9.70 |
| CHEMBL5089020 | — | — | 1 | 9.70 |
| CHEMBL5083651 | — | — | 1 | 9.40 |
| CHEMBL255863 | NILOTINIB | 4.0 | 1 | 8.74 |
| CHEMBL5081443 | — | — | 1 | 8.57 |
| CHEMBL5078722 | — | — | 1 | 8.28 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | 7.29 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5416410 | DASATINIB | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL1171837 | PONATINIB | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL5093894 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL5089813 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL5089020 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL5083651 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL255863 | NILOTINIB | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL5081443 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL5078722 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL941 | IMATINIB | IC50 | = | 51.3 | nM | 7.29 |