Assay Detail
Binding
CHEMBL923200
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Inhibition of human recombinant HER2 expressed in insect Sf9 cells
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Receptor tyrosine-protein kinase erbB-2 (CHEMBL1824) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
5-((4-Aminopiperidin-1-yl)methyl)pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 7.24 | 7.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL248114 | — | — | 1 | 7.89 |
| CHEMBL248322 | — | — | 1 | 7.75 |
| CHEMBL248116 | — | — | 1 | 7.66 |
| CHEMBL248108 | — | — | 1 | 7.64 |
| CHEMBL248321 | — | — | 1 | 7.58 |
| CHEMBL392273 | — | — | 1 | 7.57 |
| CHEMBL247104 | — | — | 1 | 7.51 |
| CHEMBL247710 | — | — | 1 | 7.50 |
| CHEMBL247915 | — | — | 1 | 7.47 |
| CHEMBL247914 | — | — | 1 | 7.46 |
| CHEMBL391387 | — | — | 1 | 7.44 |
| CHEMBL391778 | — | — | 1 | 7.42 |
| CHEMBL247709 | — | — | 1 | 7.39 |
| CHEMBL393264 | — | — | 1 | 7.37 |
| CHEMBL391181 | — | — | 1 | 7.37 |
| CHEMBL246687 | — | — | 1 | 7.28 |
| CHEMBL391779 | — | — | 1 | 7.27 |
| CHEMBL246284 | — | — | 1 | 7.26 |
| CHEMBL248115 | — | — | 1 | 7.22 |
| CHEMBL393848 | — | — | 1 | 7.16 |
| CHEMBL392664 | — | — | 1 | 7.12 |
| CHEMBL247309 | — | — | 1 | 6.96 |
| CHEMBL247513 | — | — | 1 | 6.92 |
| CHEMBL247711 | — | — | 1 | 6.77 |
| CHEMBL247512 | — | — | 1 | 6.75 |
| CHEMBL246898 | — | — | 1 | 6.72 |
| CHEMBL247916 | — | — | 1 | 6.72 |
| CHEMBL395883 | — | — | 1 | 6.60 |
| CHEMBL246493 | — | — | 1 | 6.25 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL248114 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL248322 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL248116 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL248108 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL248321 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL392273 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL247104 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL247710 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL247915 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL247914 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL391387 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL391778 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL247709 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL393264 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL391181 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL246687 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL391779 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL246284 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL248115 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL393848 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL392664 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL247309 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL247513 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL247711 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL247512 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL246898 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL247916 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL395883 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL246493 | — | IC50 | = | 560.0 | nM | 6.25 |