Assay Detail
Binding
CHEMBL4628612
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Inhibition of EGFR in human KB cells assessed as reduction in EGF-stimulated EGFR phosphorylation preincubated for 1 hr followed by EGF stimulation and measured after 6 mins by ELISA
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | KB |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design and synthesis of a novel class EGFR/HER2 dual inhibitors containing tricyclic oxazine fused quinazolines scaffold.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 6.68 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2441563 | — | — | 1 | 7.92 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 7.72 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 7.60 |
| CHEMBL4643111 | — | — | 1 | 7.35 |
| CHEMBL554 | LAPATINIB | 4.0 | 1 | 7.21 |
| CHEMBL4636996 | — | — | 1 | 7.10 |
| CHEMBL4642158 | — | — | 1 | 6.94 |
| CHEMBL4634499 | — | — | 1 | 6.92 |
| CHEMBL4635100 | — | — | 1 | 6.92 |
| CHEMBL2441567 | — | — | 1 | 6.90 |
| CHEMBL4648271 | — | — | 1 | 6.79 |
| CHEMBL4648924 | — | — | 1 | 6.75 |
| CHEMBL4634817 | — | — | 1 | 6.35 |
| CHEMBL4634127 | — | — | 1 | 6.25 |
| CHEMBL4643903 | — | — | 1 | 6.24 |
| CHEMBL4638194 | — | — | 1 | 6.07 |
| CHEMBL4639556 | — | — | 1 | 5.31 |
| CHEMBL4641942 | — | — | 1 | 5.31 |
| CHEMBL4646638 | — | — | 1 | 5.23 |
| CHEMBL4632500 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2441563 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL553 | ERLOTINIB | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL939 | GEFITINIB | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4643111 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL554 | LAPATINIB | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL4636996 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL4642158 | — | IC50 | = | 116.0 | nM | 6.94 |
| CHEMBL4634499 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4635100 | — | IC50 | = | 121.0 | nM | 6.92 |
| CHEMBL2441567 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL4648271 | — | IC50 | = | 163.0 | nM | 6.79 |
| CHEMBL4648924 | — | IC50 | = | 179.0 | nM | 6.75 |
| CHEMBL4634817 | — | IC50 | = | 446.0 | nM | 6.35 |
| CHEMBL4634127 | — | IC50 | = | 569.0 | nM | 6.25 |
| CHEMBL4643903 | — | IC50 | = | 578.0 | nM | 6.24 |
| CHEMBL4638194 | — | IC50 | = | 844.0 | nM | 6.07 |
| CHEMBL4639556 | — | IC50 | = | 4870.0 | nM | 5.31 |
| CHEMBL4641942 | — | IC50 | = | 4870.0 | nM | 5.31 |
| CHEMBL4646638 | — | IC50 | = | 5830.0 | nM | 5.23 |
| CHEMBL4632500 | — | IC50 | > | 10000.0 | nM | - |