Assay Detail
Binding
CHEMBL954169
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to human ERG expressed in HEK293 cells by whole cell patch clamp method
18
Total Activities
18
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 a new class of potential multifunctional atypical antipsychotic agents targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors: design, synthesis, and effects on behavior.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 6.17 | 6.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 6.92 |
| CHEMBL522044 | — | — | 1 | 6.80 |
| CHEMBL462508 | — | — | 1 | 6.70 |
| CHEMBL496531 | — | — | 1 | 6.70 |
| CHEMBL495572 | — | — | 1 | 6.68 |
| CHEMBL495573 | — | — | 1 | 6.58 |
| CHEMBL461236 | — | — | 1 | 6.52 |
| CHEMBL497604 | — | — | 1 | 6.41 |
| CHEMBL85 | RISPERIDONE | 4.0 | 1 | 6.04 |
| CHEMBL496739 | — | — | 1 | 6.03 |
| CHEMBL1112 | ARIPIPRAZOLE | 4.0 | 1 | 5.99 |
| CHEMBL461023 | — | — | 1 | 5.74 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 4.77 |
| CHEMBL715 | OLANZAPINE | 4.0 | 1 | 4.44 |
| CHEMBL497574 | — | — | 1 | - |
| CHEMBL497573 | — | — | 1 | - |
| CHEMBL517730 | — | — | 1 | - |
| CHEMBL497988 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL522044 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL462508 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL496531 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL495572 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL495573 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL461236 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL497604 | — | Ki | = | 390.0 | nM | 6.41 |
| CHEMBL85 | RISPERIDONE | Ki | = | 920.0 | nM | 6.04 |
| CHEMBL496739 | — | Ki | = | 930.0 | nM | 6.03 |
| CHEMBL1112 | ARIPIPRAZOLE | Ki | = | 1020.0 | nM | 5.99 |
| CHEMBL461023 | — | Ki | = | 1840.0 | nM | 5.74 |
| CHEMBL42 | CLOZAPINE | Ki | = | 17000.0 | nM | 4.77 |
| CHEMBL715 | OLANZAPINE | Ki | = | 36000.0 | nM | 4.44 |
| CHEMBL497574 | — | Ki | - | — | - | |
| CHEMBL497573 | — | Ki | - | — | - | |
| CHEMBL517730 | — | Ki | - | — | - | |
| CHEMBL497988 | — | Ki | - | — | - |