Assay Detail
Binding
CHEMBL679548
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Inhibition of tyrosine kinase activity of Epidermal growth factor receptor from human A431 cells
10
Total Activities
10
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. 9. Synthesis and evaluation of fused tricyclic quinazoline analogues as ATP site inhibitors of the tyrosine kinase activity of the epidermal growth factor receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 8.30 | 10.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL29197 | — | — | 1 | 10.60 |
| CHEMBL366580 | — | — | 1 | 9.47 |
| CHEMBL39337 | — | — | 1 | 9.36 |
| CHEMBL176891 | — | — | 1 | 8.88 |
| CHEMBL172652 | — | — | 1 | 8.39 |
| CHEMBL93051 | — | — | 1 | 7.82 |
| CHEMBL175101 | — | — | 1 | 7.66 |
| CHEMBL427298 | — | — | 1 | 6.69 |
| CHEMBL96627 | — | — | 1 | 5.86 |
| CHEMBL93346 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL29197 | — | IC50 | = | 0.025 | nM | 10.60 |
| CHEMBL366580 | — | IC50 | = | 0.34 | nM | 9.47 |
| CHEMBL39337 | — | IC50 | = | 0.44 | nM | 9.36 |
| CHEMBL176891 | — | IC50 | = | 1.32 | nM | 8.88 |
| CHEMBL172652 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL93051 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL175101 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL427298 | — | IC50 | = | 203.0 | nM | 6.69 |
| CHEMBL96627 | — | IC50 | = | 1370.0 | nM | 5.86 |
| CHEMBL93346 | — | IC50 | > | 10000.0 | nM | - |