Assay Detail
Binding
CHEMBL3389028
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ERG
13
Total Activities
13
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 |
Target
Voltage-gated inwardly rectifying potassium channel KCNH2 (CHEMBL240) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 5.09 | 5.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3353405 | — | — | 1 | 5.40 |
| CHEMBL2426288 | — | — | 1 | 5.38 |
| CHEMBL3353406 | — | — | 1 | 5.37 |
| CHEMBL3353403 | — | — | 1 | 5.25 |
| CHEMBL3353404 | — | — | 1 | 5.17 |
| CHEMBL2426277 | — | — | 1 | 5.15 |
| CHEMBL3353407 | — | — | 1 | 5.13 |
| CHEMBL2426279 | — | — | 1 | 5.04 |
| CHEMBL3353408 | — | — | 1 | 4.83 |
| CHEMBL3353409 | — | — | 1 | 4.81 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 4.79 |
| CHEMBL3353411 | — | — | 1 | 4.76 |
| CHEMBL3353412 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3353405 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL2426288 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL3353406 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL3353403 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL3353404 | — | IC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL2426277 | — | IC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL3353407 | — | IC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL2426279 | — | IC50 | = | 9100.0 | nM | 5.04 |
| CHEMBL3353408 | — | IC50 | = | 14800.0 | nM | 4.83 |
| CHEMBL3353409 | — | IC50 | = | 15600.0 | nM | 4.81 |
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 16200.0 | nM | 4.79 |
| CHEMBL3353411 | — | IC50 | = | 17500.0 | nM | 4.76 |
| CHEMBL3353412 | — | IC50 | > | 33000.0 | nM | - |