Assay Detail
Binding
CHEMBL676156
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Inhibition of autophosphorylation of epidermal growth factor receptor prepared from human A431 carcinoma cells.
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | A-431 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Tyrosine kinase inhibitors. 11. Soluble analogues of pyrrolo- and pyrazoloquinazolines as epidermal growth factor receptor inhibitors: synthesis, biological evaluation, and modeling of the mode of binding.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 7.12 | 8.02 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL39715 | — | — | 1 | 8.02 |
| CHEMBL36967 | — | — | 1 | 8.02 |
| CHEMBL287007 | — | — | 1 | 8.01 |
| CHEMBL39320 | — | — | 1 | 7.89 |
| CHEMBL40130 | — | — | 1 | 7.80 |
| CHEMBL39337 | — | — | 1 | 7.70 |
| CHEMBL36727 | — | — | 1 | 7.66 |
| CHEMBL40734 | — | — | 1 | 7.66 |
| CHEMBL416611 | — | — | 1 | 7.31 |
| CHEMBL39355 | — | — | 1 | 7.11 |
| CHEMBL39811 | — | — | 1 | 7.09 |
| CHEMBL36164 | — | — | 1 | 6.87 |
| CHEMBL37373 | — | — | 1 | 6.84 |
| CHEMBL38199 | — | — | 1 | 6.72 |
| CHEMBL287289 | — | — | 1 | 6.64 |
| CHEMBL287832 | — | — | 1 | 6.58 |
| CHEMBL37543 | — | — | 1 | 6.50 |
| CHEMBL289213 | — | — | 1 | 6.23 |
| CHEMBL36819 | — | — | 1 | 5.92 |
| CHEMBL289162 | — | — | 1 | 5.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL39715 | — | IC50 | = | 9.6 | nM | 8.02 |
| CHEMBL36967 | — | IC50 | = | 9.6 | nM | 8.02 |
| CHEMBL287007 | — | IC50 | = | 9.7 | nM | 8.01 |
| CHEMBL39320 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL40130 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL39337 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL36727 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL40734 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL416611 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL39355 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL39811 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL36164 | — | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL37373 | — | IC50 | = | 145.0 | nM | 6.84 |
| CHEMBL38199 | — | IC50 | = | 192.0 | nM | 6.72 |
| CHEMBL287289 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL287832 | — | IC50 | = | 262.0 | nM | 6.58 |
| CHEMBL37543 | — | IC50 | = | 318.0 | nM | 6.50 |
| CHEMBL289213 | — | IC50 | = | 584.0 | nM | 6.23 |
| CHEMBL36819 | — | IC50 | = | 1196.0 | nM | 5.92 |
| CHEMBL289162 | — | IC50 | = | 1780.0 | nM | 5.75 |