Assay Detail
Binding
CHEMBL4149876
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ERG expressed in HEK293 cells assessed as reduction in peak tail current after 2 to 5 mins by patch clamp based 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
BMS-986163, a Negative Allosteric Modulator of GluN2B with Potential Utility in Major Depressive Disorder.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 5.57 | 6.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4115628 | — | — | 1 | 6.40 |
| CHEMBL4111330 | — | — | 1 | 6.21 |
| CHEMBL4170867 | — | — | 1 | 5.11 |
| CHEMBL3892956 | — | — | 1 | 4.55 |
| CHEMBL4161899 | — | — | 1 | - |
| CHEMBL4115649 | — | — | 1 | - |
| CHEMBL4168402 | — | — | 1 | - |
| CHEMBL3911371 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4115628 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL4111330 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL4170867 | — | IC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL3892956 | — | IC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL4161899 | — | IC50 | - | — | - | |
| CHEMBL4115649 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4168402 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3911371 | — | IC50 | > | 5000.0 | nM | - |