Assay Detail
Binding
CHEMBL5120428
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EGFR L858R/T790M/C797S mutant (unknown origin) phosphorylation expressed in mouse BaF3 cells measured after 4 hrs by HTRF assay
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | BaF3 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of Novel Allosteric EGFR L858R Inhibitors for the Treatment of Non-Small-Cell Lung Cancer as a Single Agent or in Combination with Osimertinib.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 7.97 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5177023 | — | — | 1 | 8.70 |
| CHEMBL5184760 | — | — | 1 | 8.52 |
| CHEMBL5189574 | — | — | 1 | 8.52 |
| CHEMBL5183324 | — | — | 1 | 8.40 |
| CHEMBL5184539 | — | — | 1 | 8.40 |
| CHEMBL5173979 | — | — | 1 | 8.40 |
| CHEMBL5202945 | — | — | 1 | 8.40 |
| CHEMBL5180839 | — | — | 1 | 8.30 |
| CHEMBL5207479 | — | — | 1 | 8.30 |
| CHEMBL4214567 | — | — | 1 | 8.22 |
| CHEMBL5208056 | — | — | 1 | 8.22 |
| CHEMBL5193772 | — | — | 1 | 8.22 |
| CHEMBL5193594 | — | — | 1 | 8.15 |
| CHEMBL5180289 | — | — | 1 | 8.15 |
| CHEMBL5189114 | — | — | 1 | 8.15 |
| CHEMBL5187250 | — | — | 1 | 8.15 |
| CHEMBL5172668 | — | — | 1 | 8.15 |
| CHEMBL5170519 | — | — | 1 | 8.00 |
| CHEMBL4443062 | — | — | 1 | 8.00 |
| CHEMBL5203543 | — | — | 1 | 7.96 |
| CHEMBL5198433 | — | — | 1 | 7.80 |
| CHEMBL5203388 | — | — | 1 | 7.80 |
| CHEMBL5207152 | — | — | 1 | 7.77 |
| CHEMBL5173986 | — | — | 1 | 7.70 |
| CHEMBL5201725 | — | — | 1 | 7.66 |
| CHEMBL5195669 | — | — | 1 | 7.64 |
| CHEMBL5170278 | — | — | 1 | 6.94 |
| CHEMBL5171139 | — | — | 1 | 6.34 |
| CHEMBL5208369 | — | — | 1 | 6.03 |
| CHEMBL5205834 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5177023 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5184760 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5189574 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5183324 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5184539 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5173979 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5202945 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5180839 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5207479 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4214567 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5208056 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5193772 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5193594 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5180289 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5189114 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5187250 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5172668 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5170519 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4443062 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5203543 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5198433 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5203388 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5207152 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5173986 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5201725 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL5195669 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL5170278 | — | IC50 | = | 116.0 | nM | 6.94 |
| CHEMBL5171139 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL5208369 | — | IC50 | = | 938.0 | nM | 6.03 |
| CHEMBL5205834 | — | IC50 | > | 10000.0 | nM | - |