Assay Detail
Binding
CHEMBL5327355
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Inhibition of wild type EGFR (unknown origin) using TK as substrate incubated for 120 mins in presence of ATP by HTRF assay
9
Total Activities
9
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
Design, synthesis and biological evaluation of phosphoroxy quinazoline derivatives as potential EGFR<sup>T790M/C797S</sup> inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 6.42 | 7.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3545311 | BRIGATINIB | 4.0 | 1 | 7.28 |
| CHEMBL5397801 | — | — | 1 | 6.34 |
| CHEMBL5422588 | — | — | 1 | 6.30 |
| CHEMBL5435775 | — | — | 1 | 6.23 |
| CHEMBL5179357 | — | — | 1 | 6.19 |
| CHEMBL5425947 | — | — | 1 | 6.17 |
| CHEMBL5416489 | — | — | 1 | - |
| CHEMBL5415311 | — | — | 1 | - |
| CHEMBL5415418 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3545311 | BRIGATINIB | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL5397801 | — | IC50 | = | 460.7 | nM | 6.34 |
| CHEMBL5422588 | — | IC50 | = | 499.7 | nM | 6.30 |
| CHEMBL5435775 | — | IC50 | = | 589.7 | nM | 6.23 |
| CHEMBL5179357 | — | IC50 | = | 651.7 | nM | 6.19 |
| CHEMBL5425947 | — | IC50 | = | 682.3 | nM | 6.17 |
| CHEMBL5416489 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL5415311 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL5415418 | — | IC50 | > | 500.0 | nM | - |