Assay Detail
Binding
CHEMBL5117930
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 the presence of ATP by HTRF 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
Novel anilinopyrimidine derivatives as potential EGFR<sup>T790M/C797S</sup> Inhibitors: Design, Synthesis, biological activity study.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 9.60 | 10.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5195904 | — | — | 1 | 10.15 |
| CHEMBL5188940 | — | — | 1 | 10.10 |
| CHEMBL5180388 | — | — | 1 | 10.10 |
| CHEMBL5188373 | — | — | 1 | 10.05 |
| CHEMBL5186680 | — | — | 1 | 10.05 |
| CHEMBL5193123 | — | — | 1 | 10.00 |
| CHEMBL5197545 | — | — | 1 | 9.92 |
| CHEMBL5203220 | — | — | 1 | 9.82 |
| CHEMBL5193149 | — | — | 1 | 9.82 |
| CHEMBL5192223 | — | — | 1 | 9.72 |
| CHEMBL5206164 | — | — | 1 | 9.66 |
| CHEMBL5180894 | — | — | 1 | 9.57 |
| CHEMBL5178971 | — | — | 1 | 9.55 |
| CHEMBL5204749 | — | — | 1 | 9.39 |
| CHEMBL5203385 | — | — | 1 | 9.39 |
| CHEMBL5179357 | — | — | 1 | 9.37 |
| CHEMBL5203041 | — | — | 1 | 9.17 |
| CHEMBL5209094 | — | — | 1 | 9.17 |
| CHEMBL5199678 | — | — | 1 | 9.08 |
| CHEMBL5195137 | — | — | 1 | 9.03 |
| CHEMBL3545311 | BRIGATINIB | 4.0 | 1 | 8.47 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5195904 | — | IC50 | = | 0.07 | nM | 10.15 |
| CHEMBL5188940 | — | IC50 | = | 0.08 | nM | 10.10 |
| CHEMBL5180388 | — | IC50 | = | 0.08 | nM | 10.10 |
| CHEMBL5188373 | — | IC50 | = | 0.09 | nM | 10.05 |
| CHEMBL5186680 | — | IC50 | = | 0.09 | nM | 10.05 |
| CHEMBL5193123 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL5197545 | — | IC50 | = | 0.12 | nM | 9.92 |
| CHEMBL5203220 | — | IC50 | = | 0.15 | nM | 9.82 |
| CHEMBL5193149 | — | IC50 | = | 0.15 | nM | 9.82 |
| CHEMBL5192223 | — | IC50 | = | 0.19 | nM | 9.72 |
| CHEMBL5206164 | — | IC50 | = | 0.22 | nM | 9.66 |
| CHEMBL5180894 | — | IC50 | = | 0.27 | nM | 9.57 |
| CHEMBL5178971 | — | IC50 | = | 0.28 | nM | 9.55 |
| CHEMBL5204749 | — | IC50 | = | 0.41 | nM | 9.39 |
| CHEMBL5203385 | — | IC50 | = | 0.41 | nM | 9.39 |
| CHEMBL5179357 | — | IC50 | = | 0.43 | nM | 9.37 |
| CHEMBL5203041 | — | IC50 | = | 0.67 | nM | 9.17 |
| CHEMBL5209094 | — | IC50 | = | 0.67 | nM | 9.17 |
| CHEMBL5199678 | — | IC50 | = | 0.84 | nM | 9.08 |
| CHEMBL5195137 | — | IC50 | = | 0.93 | nM | 9.03 |
| CHEMBL3545311 | BRIGATINIB | IC50 | = | 3.38 | nM | 8.47 |