Assay Detail
Binding
CHEMBL2044873
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human KV1.5 ion channel expressed in mouse L929 cells by whole cell patch clamp assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | L929 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Potassium voltage-gated channel subfamily A member 5 (CHEMBL4306) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of ((S)-5-(methoxymethyl)-7-(1-methyl-1H-indol-2-yl)-2-(trifluoromethyl)-4,7-dihydropyrazolo[1,5-a]pyrimidin-6-yl)((S)-2-(3-methylisoxazol-5-yl)pyrrolidin-1-yl)methanone as a potent and selective I(Kur) inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 6.84 | 7.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2042152 | — | — | 1 | 7.16 |
| CHEMBL2042162 | — | — | 1 | 7.14 |
| CHEMBL2042156 | — | — | 1 | 7.08 |
| CHEMBL2042154 | — | — | 1 | 7.00 |
| CHEMBL2042158 | — | — | 1 | 7.00 |
| CHEMBL2042147 | — | — | 1 | 6.91 |
| CHEMBL2042148 | — | — | 1 | 6.83 |
| CHEMBL2042163 | — | — | 1 | 6.82 |
| CHEMBL2042157 | — | — | 1 | 6.78 |
| CHEMBL2042151 | — | — | 1 | 6.68 |
| CHEMBL2042159 | — | — | 1 | 6.64 |
| CHEMBL2042160 | — | — | 1 | 6.55 |
| CHEMBL2042149 | — | — | 1 | 6.38 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2042152 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL2042162 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL2042156 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL2042154 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL2042158 | — | IC50 | = | 101.0 | nM | 7.00 |
| CHEMBL2042147 | — | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL2042148 | — | IC50 | = | 149.0 | nM | 6.83 |
| CHEMBL2042163 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL2042157 | — | IC50 | = | 165.0 | nM | 6.78 |
| CHEMBL2042151 | — | IC50 | = | 209.0 | nM | 6.68 |
| CHEMBL2042159 | — | IC50 | = | 227.0 | nM | 6.64 |
| CHEMBL2042160 | — | IC50 | = | 281.0 | nM | 6.55 |
| CHEMBL2042149 | — | IC50 | = | 419.0 | nM | 6.38 |