Assay Detail
Functional
CHEMBL621852
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Inhibition of EGF-dependent autophosphorylation of EGF-R in A431 cells
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | A-431 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Tyrosine kinase inhibitors. 14. Structure-activity relationships for methylamino-substituted derivatives of 4-[(3-bromophenyl)amino]-6-(methylamino)-pyrido[3,4-d]pyrimidine (PD 158780), a potent and specific inhibitor of the tyrosine kinase activity of receptors for the EGF family of growth factors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 4.73 | 5.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL162622 | — | — | 1 | 5.10 |
| CHEMBL53753 | — | — | 1 | 4.89 |
| CHEMBL433520 | — | — | 1 | 4.55 |
| CHEMBL162034 | — | — | 1 | 4.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL162622 | — | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL53753 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL433520 | — | IC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL162034 | — | IC50 | = | 43000.0 | nM | 4.37 |