Assay Detail
Binding
CHEMBL903493
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Inhibition of human recombinant cytoplasmic HER2 kinase expressed in Sf9 cells
32
Total Activities
32
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
New C-5 substituted pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 32 | 6.75 | 7.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL394057 | — | — | 1 | 7.75 |
| CHEMBL245278 | — | — | 1 | 7.39 |
| CHEMBL246284 | — | — | 1 | 7.26 |
| CHEMBL245667 | — | — | 1 | 7.22 |
| CHEMBL428046 | — | — | 1 | 7.22 |
| CHEMBL245869 | — | — | 1 | 7.16 |
| CHEMBL427671 | — | — | 1 | 7.06 |
| CHEMBL394333 | — | — | 1 | 7.05 |
| CHEMBL429827 | — | — | 1 | 6.96 |
| CHEMBL246694 | — | — | 1 | 6.96 |
| CHEMBL246276 | — | — | 1 | 6.96 |
| CHEMBL246072 | — | — | 1 | 6.92 |
| CHEMBL245867 | — | — | 1 | 6.89 |
| CHEMBL394495 | — | — | 1 | 6.89 |
| CHEMBL395591 | — | — | 1 | 6.85 |
| CHEMBL246073 | — | — | 1 | 6.77 |
| CHEMBL395883 | — | — | 1 | 6.60 |
| CHEMBL394463 | — | — | 1 | 6.60 |
| CHEMBL246491 | — | — | 1 | 6.55 |
| CHEMBL394462 | — | — | 1 | 6.51 |
| CHEMBL396079 | — | — | 1 | 6.42 |
| CHEMBL247127 | — | — | 1 | 6.39 |
| CHEMBL394056 | — | — | 1 | 6.38 |
| CHEMBL246489 | — | — | 1 | 6.38 |
| CHEMBL247101 | — | — | 1 | 6.37 |
| CHEMBL397122 | — | — | 1 | 6.29 |
| CHEMBL246493 | — | — | 1 | 6.25 |
| CHEMBL245868 | — | — | 1 | 6.25 |
| CHEMBL246492 | — | — | 1 | 6.23 |
| CHEMBL245277 | — | — | 1 | 6.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL394057 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL245278 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL246284 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL245667 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL428046 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL245869 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL427671 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL394333 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL429827 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL246694 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL246276 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL246072 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL245867 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL394495 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL395591 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL246073 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL395883 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL394463 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL246491 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL394462 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL396079 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL247127 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL394056 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL246489 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL247101 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL397122 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL246493 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL245868 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL246492 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL245277 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL247100 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL188304 | — | IC50 | > | 1000.0 | nM | - |