Assay Detail
Binding
CHEMBL810541
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Inhibition of [3H]glibenclamide binding to HEK293 cells co-expressing human Sulfonylurea receptor SUR1 and Inward rectifier K+ channel Kir6.2 at high affinity state with 2 mM MgATP
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
6-Chloro-3-alkylamino-4H-thieno[3,2-e]-1,2,4-thiadiazine 1,1-dioxide derivatives potently and selectively activate ATP sensitive potassium channels of pancreatic beta-cells.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 6.66 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL134168 | — | — | 1 | 8.52 |
| CHEMBL133663 | — | — | 1 | 6.92 |
| CHEMBL135091 | — | — | 1 | 6.75 |
| CHEMBL336586 | — | — | 1 | 6.64 |
| CHEMBL135191 | TIFENAZOXIDE | 2.0 | 1 | 6.50 |
| CHEMBL131971 | — | — | 1 | 6.47 |
| CHEMBL3350270 | — | — | 1 | 6.34 |
| CHEMBL2111887 | — | — | 1 | 6.19 |
| CHEMBL133596 | — | — | 1 | 5.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL134168 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL133663 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL135091 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL336586 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL135191 | TIFENAZOXIDE | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL131971 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL3350270 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL2111887 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL133596 | — | IC50 | = | 2270.0 | nM | 5.64 |