Assay Detail
Binding
CHEMBL1176236
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to human ERG expressed in HEK293 cells
17
Total Activities
17
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
Discovery of bishomo(hetero)arylpiperazines as novel multifunctional ligands targeting dopamine D(3) and serotonin 5-HT(1A) and 5-HT(2A) receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 5.47 | 6.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1171823 | — | — | 1 | 6.52 |
| CHEMBL1173142 | — | — | 1 | 6.05 |
| CHEMBL496739 | — | — | 1 | 6.03 |
| CHEMBL1112 | ARIPIPRAZOLE | 4.0 | 1 | 5.99 |
| CHEMBL1173143 | — | — | 1 | 5.92 |
| CHEMBL1172204 | — | — | 1 | 5.66 |
| CHEMBL1172206 | — | — | 1 | 5.62 |
| CHEMBL1173017 | — | — | 1 | 5.42 |
| CHEMBL1172734 | — | — | 1 | 5.42 |
| CHEMBL1173077 | — | — | 1 | 5.39 |
| CHEMBL1171824 | — | — | 1 | 5.19 |
| CHEMBL1172205 | — | — | 1 | 5.10 |
| CHEMBL1173018 | — | — | 1 | 5.06 |
| CHEMBL1171646 | — | — | 1 | 4.89 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 4.77 |
| CHEMBL715 | OLANZAPINE | 4.0 | 1 | 4.44 |
| CHEMBL1171644 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1171823 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL1173142 | — | Ki | = | 900.0 | nM | 6.05 |
| CHEMBL496739 | — | Ki | = | 930.0 | nM | 6.03 |
| CHEMBL1112 | ARIPIPRAZOLE | Ki | = | 1020.0 | nM | 5.99 |
| CHEMBL1173143 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL1172204 | — | Ki | = | 2200.0 | nM | 5.66 |
| CHEMBL1172206 | — | Ki | = | 2400.0 | nM | 5.62 |
| CHEMBL1173017 | — | Ki | = | 3800.0 | nM | 5.42 |
| CHEMBL1172734 | — | Ki | = | 3800.0 | nM | 5.42 |
| CHEMBL1173077 | — | Ki | = | 4100.0 | nM | 5.39 |
| CHEMBL1171824 | — | Ki | = | 6400.0 | nM | 5.19 |
| CHEMBL1172205 | — | Ki | = | 8000.0 | nM | 5.10 |
| CHEMBL1173018 | — | Ki | = | 8700.0 | nM | 5.06 |
| CHEMBL1171646 | — | Ki | = | 13000.0 | nM | 4.89 |
| CHEMBL42 | CLOZAPINE | Ki | = | 17000.0 | nM | 4.77 |
| CHEMBL715 | OLANZAPINE | Ki | = | 36000.0 | nM | 4.44 |
| CHEMBL1171644 | — | Ki | > | 10000.0 | nM | - |