Assay Detail
Functional
CHEMBL4724281
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against human AU565 cells assessed as reduction in cell viability incubated for 72 hrs by WST8 assay
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | AU565 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
HER2 Kinase-Targeted Breast Cancer Therapy: Design, Synthesis, and In Vitro and In Vivo Evaluation of Novel Lapatinib Congeners as Selective and Potent HER2 Inhibitors with Favorable Metabolic Stability.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 6.55 | 7.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL554 | LAPATINIB | 4.0 | 1 | 7.19 |
| CHEMBL4793731 | — | — | 1 | 7.00 |
| CHEMBL3637894 | — | — | 1 | 6.89 |
| CHEMBL4796265 | — | — | 1 | 6.87 |
| CHEMBL4763836 | — | — | 1 | 6.87 |
| CHEMBL4786479 | — | — | 1 | 6.83 |
| CHEMBL4797630 | — | — | 1 | 6.82 |
| CHEMBL4798493 | — | — | 1 | 6.81 |
| CHEMBL4782561 | — | — | 1 | 6.69 |
| CHEMBL4783947 | — | — | 1 | 6.66 |
| CHEMBL4785584 | — | — | 1 | 6.66 |
| CHEMBL4753277 | — | — | 1 | 6.65 |
| CHEMBL4762151 | — | — | 1 | 6.54 |
| CHEMBL4753194 | — | — | 1 | 6.52 |
| CHEMBL4779497 | — | — | 1 | 6.51 |
| CHEMBL4760002 | — | — | 1 | 6.46 |
| CHEMBL4777529 | — | — | 1 | 6.44 |
| CHEMBL4786203 | — | — | 1 | 6.39 |
| CHEMBL4776952 | — | — | 1 | 6.38 |
| CHEMBL4776990 | — | — | 1 | 6.36 |
| CHEMBL4749477 | — | — | 1 | 6.35 |
| CHEMBL4793130 | — | — | 1 | 6.34 |
| CHEMBL4754866 | — | — | 1 | 6.31 |
| CHEMBL4757576 | — | — | 1 | 6.26 |
| CHEMBL4781812 | — | — | 1 | 6.18 |
| CHEMBL4793314 | — | — | 1 | 6.17 |
| CHEMBL4789816 | — | — | 1 | 6.12 |
| CHEMBL4777297 | — | — | 1 | 6.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL554 | LAPATINIB | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL4793731 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL3637894 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4796265 | — | IC50 | = | 134.0 | nM | 6.87 |
| CHEMBL4763836 | — | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL4786479 | — | IC50 | = | 149.0 | nM | 6.83 |
| CHEMBL4797630 | — | IC50 | = | 152.0 | nM | 6.82 |
| CHEMBL4798493 | — | IC50 | = | 154.0 | nM | 6.81 |
| CHEMBL4782561 | — | IC50 | = | 205.0 | nM | 6.69 |
| CHEMBL4783947 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL4785584 | — | IC50 | = | 219.0 | nM | 6.66 |
| CHEMBL4753277 | — | IC50 | = | 225.0 | nM | 6.65 |
| CHEMBL4762151 | — | IC50 | = | 289.0 | nM | 6.54 |
| CHEMBL4753194 | — | IC50 | = | 304.0 | nM | 6.52 |
| CHEMBL4779497 | — | IC50 | = | 311.0 | nM | 6.51 |
| CHEMBL4760002 | — | IC50 | = | 348.0 | nM | 6.46 |
| CHEMBL4777529 | — | IC50 | = | 364.0 | nM | 6.44 |
| CHEMBL4786203 | — | IC50 | = | 408.0 | nM | 6.39 |
| CHEMBL4776952 | — | IC50 | = | 419.0 | nM | 6.38 |
| CHEMBL4776990 | — | IC50 | = | 441.0 | nM | 6.36 |
| CHEMBL4749477 | — | IC50 | = | 447.0 | nM | 6.35 |
| CHEMBL4793130 | — | IC50 | = | 456.0 | nM | 6.34 |
| CHEMBL4754866 | — | IC50 | = | 491.0 | nM | 6.31 |
| CHEMBL4757576 | — | IC50 | = | 545.0 | nM | 6.26 |
| CHEMBL4781812 | — | IC50 | = | 663.0 | nM | 6.18 |
| CHEMBL4793314 | — | IC50 | = | 684.0 | nM | 6.17 |
| CHEMBL4789816 | — | IC50 | = | 767.0 | nM | 6.12 |
| CHEMBL4777297 | — | IC50 | = | 923.0 | nM | 6.04 |