Assay Detail
Binding
CHEMBL2390223
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ERG expressed in HEK293 cells by electrophysiology assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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
Synthesis and biological investigation of coumarin piperazine (piperidine) derivatives as potential multireceptor atypical antipsychotics.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 6.50 | 7.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2387253 | — | — | 1 | 7.51 |
| CHEMBL2387260 | — | — | 1 | 6.80 |
| CHEMBL2385102 | — | — | 1 | 6.71 |
| CHEMBL2387230 | — | — | 1 | 6.65 |
| CHEMBL85 | RISPERIDONE | 4.0 | 1 | 6.24 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 6.19 |
| CHEMBL2387265 | — | — | 1 | 6.09 |
| CHEMBL2387229 | — | — | 1 | 5.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2387253 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL2387260 | — | IC50 | = | 159.0 | nM | 6.80 |
| CHEMBL2385102 | — | IC50 | = | 195.0 | nM | 6.71 |
| CHEMBL2387230 | — | IC50 | = | 226.0 | nM | 6.65 |
| CHEMBL85 | RISPERIDONE | IC50 | = | 581.0 | nM | 6.24 |
| CHEMBL42 | CLOZAPINE | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL2387265 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL2387229 | — | IC50 | = | 1591.0 | nM | 5.80 |