Assay Detail
Functional
CHEMBL3776565
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Cytotoxicity against human K562 cells assessed as cell viability after 72 hrs by MTT assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | K562 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Structure-Activity Relationship Study of Rakicidins: Overcoming Chronic Myeloid Leukemia Resistance to Imatinib with 4-Methylester-Rakicidin A.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 6.45 | 9.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 9.60 |
| CHEMBL1171837 | PONATINIB | 4.0 | 1 | 9.47 |
| CHEMBL255863 | NILOTINIB | 4.0 | 1 | 8.41 |
| CHEMBL288441 | BOSUTINIB | 4.0 | 1 | 8.37 |
| CHEMBL3775684 | — | — | 1 | 7.18 |
| CHEMBL3774592 | — | — | 1 | 6.58 |
| CHEMBL3775955 | — | — | 1 | 6.55 |
| CHEMBL3774991 | — | — | 1 | 6.48 |
| CHEMBL3775624 | — | — | 1 | 6.41 |
| CHEMBL3775355 | — | — | 1 | 6.37 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | 6.29 |
| CHEMBL3774614 | — | — | 1 | 5.86 |
| CHEMBL3774666 | — | — | 1 | 5.78 |
| CHEMBL3775644 | — | — | 1 | 5.71 |
| CHEMBL3775820 | — | — | 1 | 5.28 |
| CHEMBL3774958 | — | — | 1 | 5.12 |
| CHEMBL3775034 | — | — | 1 | 5.06 |
| CHEMBL3774976 | — | — | 1 | 5.04 |
| CHEMBL3775146 | — | — | 1 | 4.84 |
| CHEMBL3775914 | — | — | 1 | 4.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5416410 | DASATINIB | IC50 | = | 0.25 | nM | 9.60 |
| CHEMBL1171837 | PONATINIB | IC50 | = | 0.34 | nM | 9.47 |
| CHEMBL255863 | NILOTINIB | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL288441 | BOSUTINIB | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL3775684 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL3774592 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL3775955 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL3774991 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL3775624 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL3775355 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL941 | IMATINIB | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL3774614 | — | IC50 | = | 1370.0 | nM | 5.86 |
| CHEMBL3774666 | — | IC50 | = | 1650.0 | nM | 5.78 |
| CHEMBL3775644 | — | IC50 | = | 1930.0 | nM | 5.71 |
| CHEMBL3775820 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL3774958 | — | IC50 | = | 7600.0 | nM | 5.12 |
| CHEMBL3775034 | — | IC50 | = | 8700.0 | nM | 5.06 |
| CHEMBL3774976 | — | IC50 | = | 9130.0 | nM | 5.04 |
| CHEMBL3775146 | — | IC50 | = | 14500.0 | nM | 4.84 |
| CHEMBL3775914 | — | IC50 | = | 30900.0 | nM | 4.51 |