Assay Detail
Binding
CHEMBL677204
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Evaluation of inhibitory activity against phospholipase C-gamma1 phosphorylation by Epidermal growth factor receptor enzyme isolated from A431 cells.
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | A-431 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Tyrosine kinase inhibitors. 5. Synthesis and structure-activity relationships for 4-[(phenylmethyl)amino]- and 4-(phenylamino)quinazolines as potent adenosine 5'-triphosphate binding site inhibitors of the tyrosine kinase domain of the epidermal growth factor receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 43 | 6.60 | 10.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL29197 | — | — | 1 | 10.54 |
| CHEMBL328216 | — | — | 1 | 9.92 |
| CHEMBL52765 | — | — | 1 | 9.10 |
| CHEMBL325245 | — | — | 1 | 8.00 |
| CHEMBL93181 | — | — | 1 | 8.00 |
| CHEMBL329672 | — | — | 1 | 7.64 |
| CHEMBL290096 | — | — | 1 | 7.57 |
| CHEMBL115745 | — | — | 1 | 7.25 |
| CHEMBL326596 | — | — | 1 | 7.24 |
| CHEMBL92825 | — | — | 1 | 7.10 |
| CHEMBL333082 | — | — | 1 | 6.98 |
| CHEMBL119033 | — | — | 1 | 6.86 |
| CHEMBL332938 | — | — | 1 | 6.70 |
| CHEMBL289959 | — | — | 1 | 6.46 |
| CHEMBL52197 | — | — | 1 | 6.46 |
| CHEMBL333418 | — | — | 1 | 6.36 |
| CHEMBL92824 | — | — | 1 | 6.24 |
| CHEMBL333851 | — | — | 1 | 6.23 |
| CHEMBL117710 | — | — | 1 | 6.12 |
| CHEMBL117697 | — | — | 1 | 6.08 |
| CHEMBL329161 | — | — | 1 | 6.05 |
| CHEMBL441083 | — | — | 1 | 6.04 |
| CHEMBL94275 | — | — | 1 | 6.00 |
| CHEMBL332096 | — | — | 1 | 5.85 |
| CHEMBL117804 | — | — | 1 | 5.39 |
| CHEMBL330882 | — | — | 1 | 5.31 |
| CHEMBL37346 | — | — | 1 | 5.26 |
| CHEMBL116748 | — | — | 1 | 5.23 |
| CHEMBL117554 | — | — | 1 | 5.16 |
| CHEMBL119708 | — | — | 1 | 5.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL29197 | — | IC50 | = | 0.029 | nM | 10.54 |
| CHEMBL328216 | — | IC50 | = | 0.12 | nM | 9.92 |
| CHEMBL52765 | — | IC50 | = | 0.79 | nM | 9.10 |
| CHEMBL325245 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL93181 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL329672 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL290096 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL115745 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL326596 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL92825 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL333082 | — | IC50 | = | 105.0 | nM | 6.98 |
| CHEMBL119033 | — | IC50 | = | 139.0 | nM | 6.86 |
| CHEMBL332938 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL289959 | — | IC50 | = | 344.0 | nM | 6.46 |
| CHEMBL52197 | — | IC50 | = | 348.0 | nM | 6.46 |
| CHEMBL333418 | — | IC50 | = | 439.0 | nM | 6.36 |
| CHEMBL92824 | — | IC50 | = | 577.0 | nM | 6.24 |
| CHEMBL333851 | — | IC50 | = | 588.0 | nM | 6.23 |
| CHEMBL117710 | — | IC50 | = | 756.0 | nM | 6.12 |
| CHEMBL117697 | — | IC50 | = | 842.0 | nM | 6.08 |
| CHEMBL329161 | — | IC50 | = | 897.0 | nM | 6.05 |
| CHEMBL441083 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL94275 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL332096 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL117804 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL330882 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL37346 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL116748 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL117554 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL119708 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL116919 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL324371 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL119000 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL331417 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL119432 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL39563 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL119758 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL118482 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL117711 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL326095 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL119242 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL330946 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL424255 | — | IC50 | > | 10000.0 | nM | - |