Assay Detail
Binding
CHEMBL953992
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Inhibition of HER2
25
Total Activities
25
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
Discovery of novel small-molecule inhibitors of human epidermal growth factor receptor-2: combined ligand and target-based approach.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 6.95 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL490062 | — | — | 1 | 9.00 |
| CHEMBL483332 | — | — | 1 | 9.00 |
| CHEMBL518750 | — | — | 1 | 8.70 |
| CHEMBL479171 | — | — | 1 | 8.40 |
| CHEMBL458098 | — | — | 1 | 8.10 |
| CHEMBL179363 | — | — | 1 | 8.10 |
| CHEMBL554 | LAPATINIB | 4.0 | 1 | 8.05 |
| CHEMBL93049 | — | — | 1 | 8.05 |
| CHEMBL453376 | — | — | 1 | 8.00 |
| CHEMBL483321 | CP-724714 | 2.0 | 1 | 7.92 |
| CHEMBL367492 | — | — | 1 | 7.89 |
| CHEMBL488350 | — | — | 1 | 7.89 |
| CHEMBL477078 | — | — | 1 | 7.72 |
| CHEMBL483082 | — | — | 1 | 6.70 |
| CHEMBL521284 | — | — | 1 | 6.13 |
| CHEMBL175558 | — | — | 1 | 6.00 |
| CHEMBL488564 | — | — | 1 | 5.77 |
| CHEMBL518983 | — | — | 1 | 5.28 |
| CHEMBL116857 | — | — | 1 | 5.03 |
| CHEMBL483085 | — | — | 1 | 4.80 |
| CHEMBL71884 | — | — | 1 | 4.68 |
| CHEMBL55994 | — | — | 1 | 4.46 |
| CHEMBL89505 | — | — | 1 | 4.19 |
| CHEMBL364272 | — | — | 1 | - |
| CHEMBL190654 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL490062 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL483332 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL518750 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL479171 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL458098 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL179363 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL554 | LAPATINIB | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL93049 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL453376 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL483321 | CP-724714 | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL367492 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL488350 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL477078 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL483082 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL521284 | — | IC50 | = | 733.0 | nM | 6.13 |
| CHEMBL175558 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL488564 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL518983 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL116857 | — | IC50 | = | 9300.0 | nM | 5.03 |
| CHEMBL483085 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL71884 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL55994 | — | IC50 | = | 35000.0 | nM | 4.46 |
| CHEMBL89505 | — | IC50 | = | 65000.0 | nM | 4.19 |
| CHEMBL364272 | — | IC50 | = | 120000.0 | nM | - |
| CHEMBL190654 | — | IC50 | = | 310000.0 | nM | - |