Assay Detail
Binding
CHEMBL4708520
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EGFR T790M mutant (unknown origin) using FAM-labelled peptide as substrate incubated for 10 mins in presence of ATP measured by mobility shift assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Design, synthesis and antitumor activity of novel thiophene-pyrimidine derivatives as EGFR inhibitors overcoming T790M and L858R/T790M mutations.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 7.21 | 7.32 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3786343 | OLMUTINIB | 4.0 | 1 | 7.32 |
| CHEMBL4789286 | — | — | 1 | 7.19 |
| CHEMBL4787616 | — | — | 1 | 7.12 |
| CHEMBL4762165 | — | — | 1 | - |
| CHEMBL4779676 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3786343 | OLMUTINIB | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL4789286 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL4787616 | — | IC50 | = | 76.6 | nM | 7.12 |
| CHEMBL4762165 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4779676 | — | IC50 | > | 1000.0 | nM | - |