Assay Detail
Binding
CHEMBL5327353
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EGFR L858R/T790M/C797S triple mutant (unknown origin) using TK as substrate incubated for 120 mins in presence of ATP by HTRF assay
19
Total Activities
19
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 | 19 | 9.74 | 10.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5432965 | — | — | 1 | 10.30 |
| CHEMBL5434495 | — | — | 1 | 10.22 |
| CHEMBL5180388 | — | — | 1 | 10.10 |
| CHEMBL5186680 | — | — | 1 | 10.05 |
| CHEMBL5415311 | — | — | 1 | 10.00 |
| CHEMBL5422588 | — | — | 1 | 9.92 |
| CHEMBL5418539 | — | — | 1 | 9.92 |
| CHEMBL5396086 | — | — | 1 | 9.92 |
| CHEMBL5397801 | — | — | 1 | 9.92 |
| CHEMBL5431909 | — | — | 1 | 9.89 |
| CHEMBL5399653 | — | — | 1 | 9.82 |
| CHEMBL5393923 | — | — | 1 | 9.82 |
| CHEMBL5436031 | — | — | 1 | 9.82 |
| CHEMBL5425947 | — | — | 1 | 9.54 |
| CHEMBL5435775 | — | — | 1 | 9.47 |
| CHEMBL5415418 | — | — | 1 | 9.40 |
| CHEMBL5179357 | — | — | 1 | 9.37 |
| CHEMBL5416489 | — | — | 1 | 9.09 |
| CHEMBL3545311 | BRIGATINIB | 4.0 | 1 | 8.47 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5432965 | — | IC50 | = | 0.05 | nM | 10.30 |
| CHEMBL5434495 | — | IC50 | = | 0.06 | nM | 10.22 |
| CHEMBL5180388 | — | IC50 | = | 0.08 | nM | 10.10 |
| CHEMBL5186680 | — | IC50 | = | 0.09 | nM | 10.05 |
| CHEMBL5415311 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL5422588 | — | IC50 | = | 0.12 | nM | 9.92 |
| CHEMBL5418539 | — | IC50 | = | 0.12 | nM | 9.92 |
| CHEMBL5396086 | — | IC50 | = | 0.12 | nM | 9.92 |
| CHEMBL5397801 | — | IC50 | = | 0.12 | nM | 9.92 |
| CHEMBL5431909 | — | IC50 | = | 0.13 | nM | 9.89 |
| CHEMBL5399653 | — | IC50 | = | 0.15 | nM | 9.82 |
| CHEMBL5393923 | — | IC50 | = | 0.15 | nM | 9.82 |
| CHEMBL5436031 | — | IC50 | = | 0.15 | nM | 9.82 |
| CHEMBL5425947 | — | IC50 | = | 0.29 | nM | 9.54 |
| CHEMBL5435775 | — | IC50 | = | 0.34 | nM | 9.47 |
| CHEMBL5415418 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL5179357 | — | IC50 | = | 0.43 | nM | 9.37 |
| CHEMBL5416489 | — | IC50 | = | 0.81 | nM | 9.09 |
| CHEMBL3545311 | BRIGATINIB | IC50 | = | 3.38 | nM | 8.47 |