Assay Detail
Binding
CHEMBL1021966
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [35S]N-[(4R)-1'-[(2R)-6-cyano-1,2,3,4-tetrahydro-2-naphthyl]-3,4-dihydro-4-hydroxyspiro[2H-1-benzopyran-2,4'-piperidin]6-yl]methanesulfonamide from human ERG expressed in HEK293 cells
26
Total Activities
26
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 tetrasubstituted imidazolines as potent and selective neuropeptide Y Y5 receptor antagonists: reduced human ether-a-go-go related gene potassium channel binding affinity and potent antiobesity effect.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 5.64 | 7.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL522456 | — | — | 1 | 7.00 |
| CHEMBL522793 | — | — | 1 | 6.31 |
| CHEMBL490949 | — | — | 1 | 6.31 |
| CHEMBL523134 | — | — | 1 | 5.76 |
| CHEMBL490937 | — | — | 1 | 5.47 |
| CHEMBL521947 | — | — | 1 | 5.36 |
| CHEMBL523305 | — | — | 1 | 5.21 |
| CHEMBL506163 | — | — | 1 | 5.20 |
| CHEMBL490902 | — | — | 1 | 5.20 |
| CHEMBL523821 | — | — | 1 | 5.16 |
| CHEMBL490903 | — | — | 1 | 5.11 |
| CHEMBL491119 | — | — | 1 | - |
| CHEMBL491288 | — | — | 1 | - |
| CHEMBL490123 | — | — | 1 | - |
| CHEMBL521932 | — | — | 1 | - |
| CHEMBL490901 | — | — | 1 | - |
| CHEMBL491107 | — | — | 1 | - |
| CHEMBL491894 | — | — | 1 | - |
| CHEMBL491895 | — | — | 1 | - |
| CHEMBL490561 | — | — | 1 | - |
| CHEMBL491567 | — | — | 1 | - |
| CHEMBL489725 | — | — | 1 | - |
| CHEMBL523776 | — | — | 1 | - |
| CHEMBL489726 | — | — | 1 | - |
| CHEMBL523945 | — | — | 1 | - |
| CHEMBL489732 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL522456 | — | IC50 | = | 101.0 | nM | 7.00 |
| CHEMBL522793 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL490949 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL523134 | — | IC50 | = | 1730.0 | nM | 5.76 |
| CHEMBL490937 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL521947 | — | IC50 | = | 4330.0 | nM | 5.36 |
| CHEMBL523305 | — | IC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL506163 | — | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL490902 | — | IC50 | = | 6330.0 | nM | 5.20 |
| CHEMBL523821 | — | IC50 | = | 6930.0 | nM | 5.16 |
| CHEMBL490903 | — | IC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL491119 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL491288 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL490123 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL521932 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL490901 | — | IC50 | - | — | - | |
| CHEMBL491107 | — | IC50 | - | — | - | |
| CHEMBL491894 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL491895 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL490561 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL491567 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL489725 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL523776 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL489726 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL523945 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL489732 | — | IC50 | > | 10000.0 | nM | - |