Assay Detail
Binding
CHEMBL4730214
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EGFR T790M/L858R mutant (unknown origin) using FAM-labelled peptide as substrate incubated for 10 mins in presence of ATP by Kinase Glo luminescence assay
8
Total Activities
8
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
Discovery of thiapyran-pyrimidine derivatives as potential EGFR inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 6.99 | 7.90 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3786343 | OLMUTINIB | 4.0 | 1 | 7.90 |
| CHEMBL4780534 | — | — | 1 | 6.88 |
| CHEMBL4776833 | — | — | 1 | 6.20 |
| CHEMBL4740516 | — | — | 1 | - |
| CHEMBL4754688 | — | — | 1 | - |
| CHEMBL4754481 | — | — | 1 | - |
| CHEMBL4795151 | — | — | 1 | - |
| CHEMBL573339 | PI-103 | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3786343 | OLMUTINIB | IC50 | = | 12.7 | nM | 7.90 |
| CHEMBL4780534 | — | IC50 | = | 132.1 | nM | 6.88 |
| CHEMBL4776833 | — | IC50 | = | 638.4 | nM | 6.20 |
| CHEMBL4740516 | — | IC50 | - | — | - | |
| CHEMBL4754688 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4754481 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4795151 | — | IC50 | - | — | - | |
| CHEMBL573339 | PI-103 | IC50 | - | — | - |