Assay Detail
Toxicity
CHEMBL5378342
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ERG stably expressed in HEK293 cells by whole cell voltage clamp method
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Toxicity |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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 First-in-Class GPR183 Antagonist for the Potential Treatment of Rheumatoid Arthritis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 5.26 | 5.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3262896 | — | — | 1 | 5.80 |
| CHEMBL5395781 | — | — | 1 | 5.64 |
| CHEMBL5424378 | — | — | 1 | 5.62 |
| CHEMBL5399120 | — | — | 1 | 5.31 |
| CHEMBL5394700 | — | — | 1 | 5.10 |
| CHEMBL5414588 | — | — | 1 | 4.74 |
| CHEMBL5406913 | — | — | 1 | 4.61 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3262896 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL5395781 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL5424378 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL5399120 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL5394700 | — | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL5414588 | — | IC50 | = | 18300.0 | nM | 4.74 |
| CHEMBL5406913 | — | IC50 | = | 24600.0 | nM | 4.61 |