Assay Detail
Binding
CHEMBL4736786
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EGFR L858R/T790M (unknown origin) by mobility shift assay
11
Total Activities
11
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
Design, synthesis and evaluation of novel ErbB/HDAC multitargeted inhibitors with selectivity in EGFR mutant cell lines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 8.33 | 9.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 9.37 |
| CHEMBL4759072 | — | — | 1 | 8.82 |
| CHEMBL4744985 | — | — | 1 | 8.74 |
| CHEMBL4793338 | — | — | 1 | 8.64 |
| CHEMBL4759112 | — | — | 1 | 8.52 |
| CHEMBL4794998 | — | — | 1 | 8.27 |
| CHEMBL4759697 | — | — | 1 | 8.08 |
| CHEMBL4758761 | — | — | 1 | 7.85 |
| CHEMBL4794670 | — | — | 1 | 7.82 |
| CHEMBL4758842 | — | — | 1 | 7.80 |
| CHEMBL4783641 | — | — | 1 | 7.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 0.43 | nM | 9.37 |
| CHEMBL4759072 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4744985 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4793338 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL4759112 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4794998 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL4759697 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL4758761 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4794670 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4758842 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4783641 | — | IC50 | = | 17.0 | nM | 7.77 |