Assay Detail
Functional
CHEMBL911373
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Her2 sheddase activity in BT474 cell line
16
Total Activities
16
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | BT-474 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Receptor tyrosine-protein kinase erbB-2 (CHEMBL1824) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of a potent, selective, and orally active human epidermal growth factor receptor-2 sheddase inhibitor for the treatment of cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 6.84 | 7.89 |
| Activity | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL375418 | — | — | 1 | 7.89 |
| CHEMBL373532 | — | — | 1 | 7.75 |
| CHEMBL221857 | — | — | 1 | 7.28 |
| CHEMBL434567 | — | — | 1 | 7.17 |
| CHEMBL221698 | — | — | 1 | 7.04 |
| CHEMBL219104 | — | — | 1 | 6.85 |
| CHEMBL219105 | — | — | 1 | 6.80 |
| CHEMBL221120 | — | — | 1 | 6.80 |
| CHEMBL387202 | — | — | 1 | 6.64 |
| CHEMBL426388 | — | — | 1 | 6.55 |
| CHEMBL373853 | — | — | 1 | 6.52 |
| CHEMBL221537 | — | — | 1 | 6.25 |
| CHEMBL140575 | — | — | 1 | 6.17 |
| CHEMBL218586 | — | — | 1 | 6.00 |
| CHEMBL220975 | — | — | 1 | - |
| CHEMBL220501 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL375418 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL373532 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL221857 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL434567 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL221698 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL219104 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL219105 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL221120 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL387202 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL426388 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL373853 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL221537 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL140575 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL218586 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL220975 | — | Activity | - | — | - | |
| CHEMBL220501 | — | Activity | - | — | - |