Assay Detail
Binding
CHEMBL991255
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Inhibition of ErbB2
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
Receptor tyrosine-protein kinase erbB-2 (CHEMBL1824) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Thienopyrimidine-based dual EGFR/ErbB-2 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 7.03 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL480349 | — | — | 1 | 8.22 |
| CHEMBL1201179 | LAPATINIB DITOSYLATE | 4.0 | 1 | 8.05 |
| CHEMBL514938 | GSK-969786A | — | 1 | 7.85 |
| CHEMBL474431 | — | — | 1 | 7.51 |
| CHEMBL506414 | GW684626B | — | 1 | 7.37 |
| CHEMBL473429 | — | — | 1 | 7.17 |
| CHEMBL473438 | — | — | 1 | 7.17 |
| CHEMBL475768 | — | — | 1 | 7.15 |
| CHEMBL473437 | — | — | 1 | 7.12 |
| CHEMBL475769 | — | — | 1 | 7.07 |
| CHEMBL481324 | — | — | 1 | 7.02 |
| CHEMBL480348 | — | — | 1 | 6.96 |
| CHEMBL473427 | — | — | 1 | 6.95 |
| CHEMBL475446 | — | — | 1 | 6.95 |
| CHEMBL473436 | — | — | 1 | 6.92 |
| CHEMBL473428 | — | — | 1 | 6.91 |
| CHEMBL475594 | — | — | 1 | 6.84 |
| CHEMBL481331 | — | — | 1 | 6.82 |
| CHEMBL475600 | — | — | 1 | 6.69 |
| CHEMBL475767 | — | — | 1 | 6.61 |
| CHEMBL475761 | GW784684X | — | 1 | 6.60 |
| CHEMBL475599 | GSK-300014A | — | 1 | 6.52 |
| CHEMBL479800 | — | — | 1 | 6.15 |
| CHEMBL519757 | — | — | 1 | 6.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL480349 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL1201179 | LAPATINIB DITOSYLATE | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL514938 | GSK-969786A | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL474431 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL506414 | GW684626B | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL473429 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL473438 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL475768 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL473437 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL475769 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL481324 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL480348 | — | IC50 | = | 111.0 | nM | 6.96 |
| CHEMBL473427 | — | IC50 | = | 113.0 | nM | 6.95 |
| CHEMBL475446 | — | IC50 | = | 113.0 | nM | 6.95 |
| CHEMBL473436 | — | IC50 | = | 121.0 | nM | 6.92 |
| CHEMBL473428 | — | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL475594 | — | IC50 | = | 146.0 | nM | 6.84 |
| CHEMBL481331 | — | IC50 | = | 153.0 | nM | 6.82 |
| CHEMBL475600 | — | IC50 | = | 203.0 | nM | 6.69 |
| CHEMBL475767 | — | IC50 | = | 246.0 | nM | 6.61 |
| CHEMBL475761 | GW784684X | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL475599 | GSK-300014A | IC50 | = | 299.0 | nM | 6.52 |
| CHEMBL479800 | — | IC50 | = | 709.0 | nM | 6.15 |
| CHEMBL519757 | — | IC50 | = | 898.0 | nM | 6.05 |