Assay Detail
Binding
CHEMBL3636784
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Inhibition of EGFR (unknown origin) after 120 mins by HotSpot assay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Targeting EGFR/HER2 tyrosine kinases with a new potent series of 6-substituted 4-anilinoquinazoline hybrids: Design, synthesis, kinase assay, cell-based assay, and molecular docking.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 7.16 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1614725 | TAK-285 | 1.0 | 1 | 9.00 |
| CHEMBL3633929 | — | — | 1 | 8.52 |
| CHEMBL3633774 | — | — | 1 | 8.40 |
| CHEMBL3633940 | — | — | 1 | 8.05 |
| CHEMBL554 | LAPATINIB | 4.0 | 1 | 8.00 |
| CHEMBL3633934 | — | — | 1 | 7.64 |
| CHEMBL3633930 | — | — | 1 | 7.54 |
| CHEMBL3633941 | — | — | 1 | 7.51 |
| CHEMBL3633932 | — | — | 1 | 7.46 |
| CHEMBL180022 | NERATINIB | 4.0 | 1 | 7.04 |
| CHEMBL3633928 | — | — | 1 | 7.00 |
| CHEMBL3633933 | — | — | 1 | 6.64 |
| CHEMBL3633938 | — | — | 1 | 6.35 |
| CHEMBL3633775 | — | — | 1 | 6.26 |
| CHEMBL3633936 | — | — | 1 | 6.09 |
| CHEMBL3632637 | — | — | 1 | 5.99 |
| CHEMBL3633942 | — | — | 1 | 5.84 |
| CHEMBL3633939 | — | — | 1 | 5.52 |
| CHEMBL3633935 | — | — | 1 | - |
| CHEMBL3633931 | — | — | 1 | - |
| CHEMBL3633937 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1614725 | TAK-285 | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3633929 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3633774 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3633940 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL554 | LAPATINIB | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3633934 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3633930 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL3633941 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL3633932 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL180022 | NERATINIB | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL3633928 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL3633933 | — | IC50 | = | 227.0 | nM | 6.64 |
| CHEMBL3633938 | — | IC50 | = | 445.0 | nM | 6.35 |
| CHEMBL3633775 | — | IC50 | = | 543.0 | nM | 6.26 |
| CHEMBL3633936 | — | IC50 | = | 812.0 | nM | 6.09 |
| CHEMBL3632637 | — | IC50 | = | 1020.0 | nM | 5.99 |
| CHEMBL3633942 | — | IC50 | = | 1460.0 | nM | 5.84 |
| CHEMBL3633939 | — | IC50 | = | 3050.0 | nM | 5.52 |
| CHEMBL3633935 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3633931 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3633937 | — | IC50 | > | 10000.0 | nM | - |