Assay Detail
Functional
CHEMBL680030
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Tested for inhibition of PLC gamma-derived substrate in Epidermal growth factor receptor stimulated A431 cells
12
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | A-431 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Tyrosine kinase inhibitors. 12. Synthesis and structure-activity relationships for 6-substituted 4-(phenylamino)pyrimido[5,4-d]pyrimidines designed as inhibitors of the epidermal growth factor receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 8.32 | 9.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL51853 | — | — | 1 | 9.89 |
| CHEMBL52765 | — | — | 1 | 9.11 |
| CHEMBL53711 | — | — | 2 | 8.59 |
| CHEMBL53156 | — | — | 1 | 8.51 |
| CHEMBL50519 | — | — | 1 | 8.37 |
| CHEMBL300217 | — | — | 1 | 8.12 |
| CHEMBL53796 | — | — | 1 | 8.02 |
| CHEMBL50344 | — | — | 1 | 7.96 |
| CHEMBL52197 | — | — | 1 | 7.52 |
| CHEMBL52015 | — | — | 1 | 7.08 |
| CHEMBL53753 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL51853 | — | IC50 | = | 0.13 | nM | 9.89 |
| CHEMBL52765 | — | IC50 | = | 0.78 | nM | 9.11 |
| CHEMBL53711 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL53156 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL50519 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL300217 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL53796 | — | IC50 | = | 9.6 | nM | 8.02 |
| CHEMBL50344 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL52197 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL52015 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL53711 | — | IC50 | = | 0.006 | nM | - |
| CHEMBL53753 | — | IC50 | = | 0.008 | nM | - |