Assay Detail
Binding
CHEMBL927683
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of HER2 sheddase in BT474 cells by extracellular domain shedding assay
31
Total Activities
31
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | BT-474 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
Disintegrin and metalloproteinase domain-containing protein 10 (CHEMBL5028) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design and identification of selective HER-2 sheddase inhibitors via P1' manipulation and unconventional P2' perturbations to induce a molecular metamorphosis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 6.97 | 7.89 |
| Activity | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL375418 | — | — | 1 | 7.89 |
| CHEMBL373532 | — | — | 1 | 7.75 |
| CHEMBL253920 | — | — | 1 | 7.62 |
| CHEMBL429669 | — | — | 1 | 7.58 |
| CHEMBL252442 | — | — | 1 | 7.47 |
| CHEMBL251884 | — | — | 1 | 7.38 |
| CHEMBL251847 | — | — | 1 | 7.38 |
| CHEMBL446457 | — | — | 1 | 7.35 |
| CHEMBL221857 | — | — | 1 | 7.28 |
| CHEMBL251865 | — | — | 1 | 7.17 |
| CHEMBL252877 | — | — | 1 | 7.14 |
| CHEMBL252278 | — | — | 1 | 7.07 |
| CHEMBL252246 | — | — | 1 | 7.04 |
| CHEMBL401870 | — | — | 1 | 7.03 |
| CHEMBL403380 | — | — | 1 | 6.89 |
| CHEMBL219104 | — | — | 1 | 6.86 |
| CHEMBL253460 | — | — | 1 | 6.86 |
| CHEMBL403185 | — | — | 1 | 6.82 |
| CHEMBL403161 | — | — | 1 | 6.79 |
| CHEMBL442443 | — | — | 1 | 6.77 |
| CHEMBL404132 | — | — | 1 | 6.74 |
| CHEMBL252079 | — | — | 1 | 6.71 |
| CHEMBL252081 | — | — | 1 | 6.64 |
| CHEMBL402954 | — | — | 1 | 6.62 |
| CHEMBL404093 | — | — | 1 | 6.54 |
| CHEMBL252678 | — | — | 1 | 6.37 |
| CHEMBL252912 | — | — | 1 | 6.23 |
| CHEMBL253256 | — | — | 1 | 6.16 |
| CHEMBL404170 | — | — | 1 | 6.04 |
| CHEMBL251848 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL375418 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL373532 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL253920 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL429669 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL252442 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL251884 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL251847 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL446457 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL221857 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL251865 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL252877 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL252278 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL252246 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL401870 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL403380 | — | IC50 | = | 129.0 | nM | 6.89 |
| CHEMBL219104 | — | IC50 | = | 137.0 | nM | 6.86 |
| CHEMBL253460 | — | IC50 | = | 139.0 | nM | 6.86 |
| CHEMBL403185 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL403161 | — | IC50 | = | 162.0 | nM | 6.79 |
| CHEMBL442443 | — | IC50 | = | 169.0 | nM | 6.77 |
| CHEMBL404132 | — | IC50 | = | 184.0 | nM | 6.74 |
| CHEMBL252079 | — | IC50 | = | 194.0 | nM | 6.71 |
| CHEMBL252081 | — | IC50 | = | 229.0 | nM | 6.64 |
| CHEMBL402954 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL404093 | — | IC50 | = | 289.0 | nM | 6.54 |
| CHEMBL252678 | — | IC50 | = | 431.0 | nM | 6.37 |
| CHEMBL252912 | — | IC50 | = | 594.0 | nM | 6.23 |
| CHEMBL253256 | — | IC50 | = | 689.0 | nM | 6.16 |
| CHEMBL404170 | — | IC50 | = | 902.0 | nM | 6.04 |
| CHEMBL251848 | — | Activity | - | — | - | |
| CHEMBL403022 | — | Activity | - | — | - |