Assay Detail
Functional
CHEMBL621853
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Inhibition of autophosphorylation of epidermal growth factor receptor in A431 cells in culture
22
Total Activities
22
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 | 22 | 7.63 | 8.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL165574 | — | — | 1 | 8.23 |
| CHEMBL162142 | — | — | 1 | 8.20 |
| CHEMBL162622 | — | — | 1 | 8.10 |
| CHEMBL162223 | — | — | 1 | 8.09 |
| CHEMBL166307 | — | — | 1 | 8.05 |
| CHEMBL162981 | — | — | 1 | 8.04 |
| CHEMBL53753 | — | — | 1 | 7.89 |
| CHEMBL165508 | — | — | 1 | 7.89 |
| CHEMBL51853 | — | — | 1 | 7.80 |
| CHEMBL166358 | — | — | 1 | 7.80 |
| CHEMBL349070 | — | — | 1 | 7.72 |
| CHEMBL165731 | — | — | 1 | 7.70 |
| CHEMBL53711 | — | — | 1 | 7.68 |
| CHEMBL162821 | — | — | 1 | 7.64 |
| CHEMBL166255 | — | — | 1 | 7.57 |
| CHEMBL433520 | — | — | 1 | 7.55 |
| CHEMBL162034 | — | — | 1 | 7.37 |
| CHEMBL162053 | — | — | 1 | 7.34 |
| CHEMBL165630 | — | — | 1 | 7.15 |
| CHEMBL162719 | — | — | 1 | 6.99 |
| CHEMBL163369 | — | — | 1 | 6.64 |
| CHEMBL163168 | — | — | 1 | 6.35 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL165574 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL162142 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL162622 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL162223 | — | IC50 | = | 8.1 | nM | 8.09 |
| CHEMBL166307 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL162981 | — | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL53753 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL165508 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL51853 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL166358 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL349070 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL165731 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL53711 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL162821 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL166255 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL433520 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL162034 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL162053 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL165630 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL162719 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL163369 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL163168 | — | IC50 | = | 449.0 | nM | 6.35 |