Assay Detail
Binding
CHEMBL5120429
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Inhibition of EGFR L858R/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 | 7.14 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5193594 | — | — | 1 | 8.10 |
| CHEMBL5180839 | — | — | 1 | 7.92 |
| CHEMBL5183324 | — | — | 1 | 7.92 |
| CHEMBL5184539 | — | — | 1 | 7.89 |
| CHEMBL5202945 | — | — | 1 | 7.82 |
| CHEMBL5208056 | — | — | 1 | 7.77 |
| CHEMBL5170519 | — | — | 1 | 7.70 |
| CHEMBL5177023 | — | — | 1 | 7.70 |
| CHEMBL5203543 | — | — | 1 | 7.66 |
| CHEMBL5184760 | — | — | 1 | 7.64 |
| CHEMBL5189574 | — | — | 1 | 7.58 |
| CHEMBL5207152 | — | — | 1 | 7.52 |
| CHEMBL5201725 | — | — | 1 | 7.48 |
| CHEMBL5207479 | — | — | 1 | 7.48 |
| CHEMBL5172668 | — | — | 1 | 7.27 |
| CHEMBL5180289 | — | — | 1 | 7.04 |
| CHEMBL4443062 | — | — | 1 | 7.00 |
| CHEMBL5193772 | — | — | 1 | 6.97 |
| CHEMBL5189114 | — | — | 1 | 6.89 |
| CHEMBL5173979 | — | — | 1 | 6.74 |
| CHEMBL5187250 | — | — | 1 | 6.53 |
| CHEMBL5198433 | — | — | 1 | 6.47 |
| CHEMBL4214567 | — | — | 1 | 6.34 |
| CHEMBL5173986 | — | — | 1 | 6.07 |
| CHEMBL5170278 | — | — | 1 | 5.96 |
| CHEMBL5203388 | — | — | 1 | 5.77 |
| CHEMBL5195669 | — | — | 1 | 5.50 |
| CHEMBL5171139 | — | — | 1 | - |
| CHEMBL5205834 | — | — | 1 | - |
| CHEMBL5208369 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5193594 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL5180839 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5183324 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5184539 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5202945 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5208056 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5170519 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5177023 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5203543 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL5184760 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL5189574 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL5207152 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL5201725 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL5207479 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL5172668 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL5180289 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL4443062 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL5193772 | — | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL5189114 | — | IC50 | = | 129.0 | nM | 6.89 |
| CHEMBL5173979 | — | IC50 | = | 183.0 | nM | 6.74 |
| CHEMBL5187250 | — | IC50 | = | 297.0 | nM | 6.53 |
| CHEMBL5198433 | — | IC50 | = | 342.0 | nM | 6.47 |
| CHEMBL4214567 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL5173986 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL5170278 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL5203388 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL5195669 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL5171139 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5205834 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5208369 | — | IC50 | > | 10000.0 | nM | - |