Assay Detail
Binding
CHEMBL683040
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Inhibition of tyrosine kinase activity of Epidermal growth factor receptor from human A431 carcinoma cells
14
Total Activities
14
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 | 14 | 8.91 | 11.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL176582 | — | — | 1 | 11.00 |
| CHEMBL174426 | — | — | 1 | 10.60 |
| CHEMBL328216 | — | — | 1 | 9.92 |
| CHEMBL93032 | — | — | 1 | 9.77 |
| CHEMBL426580 | — | — | 1 | 9.54 |
| CHEMBL40734 | — | — | 1 | 9.36 |
| CHEMBL153525 | — | — | 1 | 8.91 |
| CHEMBL173498 | — | — | 1 | 8.77 |
| CHEMBL290096 | — | — | 1 | 7.57 |
| CHEMBL153170 | — | — | 1 | 7.54 |
| CHEMBL177053 | — | — | 1 | 7.36 |
| CHEMBL155100 | — | — | 1 | 6.57 |
| CHEMBL63786 | — | — | 1 | - |
| CHEMBL66031 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL176582 | — | IC50 | = | 0.01 | nM | 11.00 |
| CHEMBL174426 | — | IC50 | = | 0.025 | nM | 10.60 |
| CHEMBL328216 | — | IC50 | = | 0.12 | nM | 9.92 |
| CHEMBL93032 | — | IC50 | = | 0.17 | nM | 9.77 |
| CHEMBL426580 | — | IC50 | = | 0.29 | nM | 9.54 |
| CHEMBL40734 | — | IC50 | = | 0.44 | nM | 9.36 |
| CHEMBL153525 | — | IC50 | = | 1.24 | nM | 8.91 |
| CHEMBL173498 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL290096 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL153170 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL177053 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL155100 | — | IC50 | = | 272.0 | nM | 6.57 |
| CHEMBL63786 | — | IC50 | = | 0.003 | nM | - |
| CHEMBL66031 | — | IC50 | = | 0.008 | nM | - |