Assay Detail
Binding
CHEMBL673948
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In vitro inhibition of ERBB2 receptor kinase autophosphorylation.
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Receptor tyrosine-protein kinase erbB-2 (CHEMBL1824) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Tyrphostins. 2. Heterocyclic and alpha-substituted benzylidenemalononitrile tyrphostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine kinases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 4.72 | 5.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL56879 | — | — | 1 | 5.52 |
| CHEMBL56542 | — | — | 1 | 5.31 |
| CHEMBL296407 | — | — | 1 | 5.19 |
| CHEMBL54471 | — | — | 1 | 5.00 |
| CHEMBL59145 | — | — | 1 | 4.92 |
| CHEMBL56543 | — | — | 1 | 4.87 |
| CHEMBL55204 | — | — | 1 | 4.87 |
| CHEMBL417941 | — | — | 1 | 4.77 |
| CHEMBL56132 | — | — | 1 | 4.75 |
| CHEMBL56393 | — | — | 1 | 4.75 |
| CHEMBL293749 | — | — | 1 | 4.64 |
| CHEMBL55360 | — | — | 1 | 4.47 |
| CHEMBL53898 | — | — | 1 | 4.46 |
| CHEMBL55994 | — | — | 1 | 4.46 |
| CHEMBL55979 | — | — | 1 | 4.43 |
| CHEMBL56731 | — | — | 1 | 4.38 |
| CHEMBL291986 | — | — | 1 | 4.31 |
| CHEMBL55993 | — | — | 1 | 4.30 |
| CHEMBL56219 | — | — | 1 | 4.24 |
| CHEMBL57251 | — | — | 1 | - |
| CHEMBL440298 | — | — | 1 | - |
| CHEMBL56319 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL56879 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL56542 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL296407 | — | IC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL54471 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL59145 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL56543 | — | IC50 | = | 13500.0 | nM | 4.87 |
| CHEMBL55204 | — | IC50 | = | 13600.0 | nM | 4.87 |
| CHEMBL417941 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL56132 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL56393 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL293749 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL55360 | — | IC50 | = | 34000.0 | nM | 4.47 |
| CHEMBL53898 | — | IC50 | = | 35000.0 | nM | 4.46 |
| CHEMBL55994 | — | IC50 | = | 35000.0 | nM | 4.46 |
| CHEMBL55979 | — | IC50 | = | 37000.0 | nM | 4.43 |
| CHEMBL56731 | — | IC50 | = | 42000.0 | nM | 4.38 |
| CHEMBL291986 | — | IC50 | = | 49000.0 | nM | 4.31 |
| CHEMBL55993 | — | IC50 | = | 50000.0 | nM | 4.30 |
| CHEMBL56219 | — | IC50 | = | 57000.0 | nM | 4.24 |
| CHEMBL57251 | — | IC50 | > | 166000.0 | nM | - |
| CHEMBL440298 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL56319 | — | IC50 | > | 333000.0 | nM | - |