Assay Detail
Functional
CHEMBL4724249
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against human MDA-MB-231 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 | MDA-MB-231 |
| 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 | 5.34 | 6.13 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4793731 | — | — | 1 | 6.13 |
| CHEMBL4749477 | — | — | 1 | 5.97 |
| CHEMBL4796265 | — | — | 1 | 5.87 |
| CHEMBL4762151 | — | — | 1 | 5.86 |
| CHEMBL4776952 | — | — | 1 | 5.77 |
| CHEMBL4789816 | — | — | 1 | 5.72 |
| CHEMBL4793130 | — | — | 1 | 5.71 |
| CHEMBL4776990 | — | — | 1 | 5.59 |
| CHEMBL4786203 | — | — | 1 | 5.58 |
| CHEMBL4785584 | — | — | 1 | 5.55 |
| CHEMBL4793314 | — | — | 1 | 5.41 |
| CHEMBL4798493 | — | — | 1 | 5.35 |
| CHEMBL4763836 | — | — | 1 | 5.35 |
| CHEMBL4753277 | — | — | 1 | 5.30 |
| CHEMBL4782561 | — | — | 1 | 5.28 |
| CHEMBL4754866 | — | — | 1 | 5.26 |
| CHEMBL4781812 | — | — | 1 | 5.18 |
| CHEMBL4760002 | — | — | 1 | 5.17 |
| CHEMBL4786479 | — | — | 1 | 5.14 |
| CHEMBL4753194 | — | — | 1 | 5.11 |
| CHEMBL4783947 | — | — | 1 | 5.06 |
| CHEMBL4777529 | — | — | 1 | 5.05 |
| CHEMBL4779497 | — | — | 1 | 4.99 |
| CHEMBL554 | LAPATINIB | 4.0 | 1 | 4.98 |
| CHEMBL4777297 | — | — | 1 | 4.94 |
| CHEMBL3637894 | — | — | 1 | 4.94 |
| CHEMBL4797630 | — | — | 1 | 4.86 |
| CHEMBL4757576 | — | — | 1 | 4.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4793731 | — | IC50 | = | 737.0 | nM | 6.13 |
| CHEMBL4749477 | — | IC50 | = | 1063.0 | nM | 5.97 |
| CHEMBL4796265 | — | IC50 | = | 1360.0 | nM | 5.87 |
| CHEMBL4762151 | — | IC50 | = | 1371.0 | nM | 5.86 |
| CHEMBL4776952 | — | IC50 | = | 1699.0 | nM | 5.77 |
| CHEMBL4789816 | — | IC50 | = | 1902.0 | nM | 5.72 |
| CHEMBL4793130 | — | IC50 | = | 1948.0 | nM | 5.71 |
| CHEMBL4776990 | — | IC50 | = | 2559.0 | nM | 5.59 |
| CHEMBL4786203 | — | IC50 | = | 2659.0 | nM | 5.58 |
| CHEMBL4785584 | — | IC50 | = | 2828.0 | nM | 5.55 |
| CHEMBL4793314 | — | IC50 | = | 3924.0 | nM | 5.41 |
| CHEMBL4798493 | — | IC50 | = | 4513.0 | nM | 5.35 |
| CHEMBL4763836 | — | IC50 | = | 4503.0 | nM | 5.35 |
| CHEMBL4753277 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL4782561 | — | IC50 | = | 5233.0 | nM | 5.28 |
| CHEMBL4754866 | — | IC50 | = | 5447.0 | nM | 5.26 |
| CHEMBL4781812 | — | IC50 | = | 6555.0 | nM | 5.18 |
| CHEMBL4760002 | — | IC50 | = | 6732.0 | nM | 5.17 |
| CHEMBL4786479 | — | IC50 | = | 7316.0 | nM | 5.14 |
| CHEMBL4753194 | — | IC50 | = | 7833.0 | nM | 5.11 |
| CHEMBL4783947 | — | IC50 | = | 8776.0 | nM | 5.06 |
| CHEMBL4777529 | — | IC50 | = | 8846.0 | nM | 5.05 |
| CHEMBL4779497 | — | IC50 | = | 10160.0 | nM | 4.99 |
| CHEMBL554 | LAPATINIB | IC50 | = | 10373.0 | nM | 4.98 |
| CHEMBL4777297 | — | IC50 | = | 11509.0 | nM | 4.94 |
| CHEMBL3637894 | — | IC50 | = | 11600.0 | nM | 4.94 |
| CHEMBL4797630 | — | IC50 | = | 13783.0 | nM | 4.86 |
| CHEMBL4757576 | — | IC50 | = | 30162.0 | nM | 4.52 |