Assay Detail
Binding
CHEMBL2020642
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human EGFR expressed in human A431 cells using poly(Glu4/Tyr) and [gamma32P]ATP as substrate after 1 hr by scintillation counting
65
Total Activities
65
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 | Autocuration |
Publication
Synthesis and structure-activity relationships of (aryloxy)quinazoline ureas as novel, potent, and selective vascular endothelial growth factor receptor-2 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 65 | 5.45 | 6.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL301018 | — | — | 1 | 6.42 |
| CHEMBL2018749 | — | — | 1 | 6.10 |
| CHEMBL2018760 | — | — | 1 | 6.05 |
| CHEMBL2018757 | — | — | 1 | 6.05 |
| CHEMBL2018756 | — | — | 1 | 6.05 |
| CHEMBL2018752 | — | — | 1 | 6.00 |
| CHEMBL2018753 | — | — | 1 | 6.00 |
| CHEMBL328106 | — | — | 1 | 5.44 |
| CHEMBL2018755 | — | — | 1 | 5.40 |
| CHEMBL94191 | — | — | 1 | 5.37 |
| CHEMBL2018750 | — | — | 1 | 5.32 |
| CHEMBL2018762 | — | — | 1 | 5.30 |
| CHEMBL1277620 | — | — | 1 | 5.24 |
| CHEMBL2018759 | — | — | 1 | 5.24 |
| CHEMBL1278149 | — | — | 1 | 5.23 |
| CHEMBL2018751 | — | — | 1 | 5.21 |
| CHEMBL2018754 | — | — | 1 | 5.19 |
| CHEMBL1761929 | — | — | 1 | 5.16 |
| CHEMBL2018748 | — | — | 1 | 5.15 |
| CHEMBL2018761 | — | — | 1 | 5.14 |
| CHEMBL2018758 | — | — | 1 | 5.12 |
| CHEMBL2018777 | — | — | 1 | 5.04 |
| CHEMBL2018773 | — | — | 1 | 5.04 |
| CHEMBL2018767 | — | — | 1 | 5.03 |
| CHEMBL2018765 | — | — | 1 | 5.00 |
| CHEMBL179603 | — | — | 1 | - |
| CHEMBL2018886 | — | — | 1 | - |
| CHEMBL2018880 | — | — | 1 | - |
| CHEMBL2018883 | — | — | 1 | - |
| CHEMBL1761930 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL301018 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL2018749 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL2018757 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL2018756 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL2018760 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL2018752 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL2018753 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL328106 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL2018755 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL94191 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL2018750 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL2018762 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL1277620 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL2018759 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL1278149 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL2018751 | — | IC50 | = | 6150.0 | nM | 5.21 |
| CHEMBL2018754 | — | IC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL1761929 | — | IC50 | = | 6900.0 | nM | 5.16 |
| CHEMBL2018748 | — | IC50 | = | 7050.0 | nM | 5.15 |
| CHEMBL2018761 | — | IC50 | = | 7200.0 | nM | 5.14 |
| CHEMBL2018758 | — | IC50 | = | 7600.0 | nM | 5.12 |
| CHEMBL2018777 | — | IC50 | = | 9150.0 | nM | 5.04 |
| CHEMBL2018773 | — | IC50 | = | 9100.0 | nM | 5.04 |
| CHEMBL2018767 | — | IC50 | = | 9450.0 | nM | 5.03 |
| CHEMBL2018765 | — | IC50 | = | 9900.0 | nM | 5.00 |
| CHEMBL2018885 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1761937 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2018882 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1761942 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1277253 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1277254 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2018768 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2018745 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2018746 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2018747 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1761931 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2016600 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1761938 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1761939 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2018881 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1277162 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL205089 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2018884 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1761936 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1761932 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1761930 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2018883 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2018880 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2018886 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL179603 | — | IC50 | > | 10000.0 | nM | - |