Assay Detail
Binding
CHEMBL677215
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Inhibition of Epidermal growth factor receptor autophosphorylation in A431 human epidermoid carcinoma cells
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | A-431 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Tyrosine kinase inhibitors. 10. Isomeric 4-[(3-bromophenyl)amino]pyrido[d]-pyrimidines are potent ATP binding site inhibitors of the tyrosine kinase function of the epidermal growth factor receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 7.22 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL53062 | — | — | 1 | 7.92 |
| CHEMBL53428 | — | — | 1 | 7.85 |
| CHEMBL53753 | — | — | 1 | 7.82 |
| CHEMBL54400 | — | — | 1 | 7.80 |
| CHEMBL51853 | — | — | 1 | 7.80 |
| CHEMBL53156 | — | — | 1 | 7.70 |
| CHEMBL53711 | — | — | 1 | 7.68 |
| CHEMBL53796 | — | — | 1 | 7.50 |
| CHEMBL300217 | — | — | 1 | 7.28 |
| CHEMBL52076 | — | — | 1 | 6.96 |
| CHEMBL298637 | — | — | 1 | 6.26 |
| CHEMBL300083 | — | — | 1 | 5.68 |
| CHEMBL50245 | — | — | 1 | 5.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL53062 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL53428 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL53753 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL54400 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL51853 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL53156 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL53711 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL53796 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL300217 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL52076 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL298637 | — | IC50 | = | 552.0 | nM | 6.26 |
| CHEMBL300083 | — | IC50 | = | 2085.0 | nM | 5.68 |
| CHEMBL50245 | — | IC50 | = | 2300.0 | nM | 5.64 |