Assay Detail
Binding
CHEMBL820996
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro displacement of [35S]-MK- 499 from HEK 293 cells stably transfected with hERG voltage-gated potassium channel subunit Kv11.1
15
Total Activities
12
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 | Expert |
Target
Voltage-gated inwardly rectifying potassium channel KCNH2 (CHEMBL240) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Optimization of a tertiary alcohol series of phosphodiesterase-4 (PDE4) inhibitors: structure-activity relationship related to PDE4 inhibition and human ether-a-go-go related gene potassium channel binding affinity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 4.55 | 5.93 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL61191 | — | — | 1 | 5.93 |
| CHEMBL2112296 | — | — | 1 | 4.68 |
| CHEMBL2112294 | — | — | 1 | 4.65 |
| CHEMBL417776 | — | — | 2 | 4.64 |
| CHEMBL78806 | — | — | 1 | 4.60 |
| CHEMBL276559 | — | — | 2 | 4.58 |
| CHEMBL2112295 | — | — | 1 | 4.42 |
| CHEMBL383762 | — | — | 1 | 4.41 |
| CHEMBL78439 | — | — | 2 | 4.38 |
| CHEMBL81491 | — | — | 1 | 4.25 |
| CHEMBL310303 | — | — | 1 | 4.23 |
| CHEMBL199015 | — | — | 1 | 4.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL61191 | — | Ki | = | 1180.0 | nM | 5.93 |
| CHEMBL2112296 | — | Ki | = | 21000.0 | nM | 4.68 |
| CHEMBL2112294 | — | Ki | = | 22400.0 | nM | 4.65 |
| CHEMBL417776 | — | Ki | = | 22700.0 | nM | 4.64 |
| CHEMBL78806 | — | Ki | = | 25000.0 | nM | 4.60 |
| CHEMBL417776 | — | Ki | = | 25400.0 | nM | 4.59 |
| CHEMBL276559 | — | Ki | = | 26400.0 | nM | 4.58 |
| CHEMBL2112295 | — | Ki | = | 38100.0 | nM | 4.42 |
| CHEMBL383762 | — | Ki | = | 39000.0 | nM | 4.41 |
| CHEMBL78439 | — | Ki | = | 42200.0 | nM | 4.38 |
| CHEMBL276559 | — | Ki | = | 41500.0 | nM | 4.38 |
| CHEMBL78439 | — | Ki | = | 44700.0 | nM | 4.35 |
| CHEMBL81491 | — | Ki | = | 55900.0 | nM | 4.25 |
| CHEMBL310303 | — | Ki | = | 58400.0 | nM | 4.23 |
| CHEMBL199015 | — | Ki | = | 61400.0 | nM | 4.21 |