Potency data for probe A-1596586 and control A-1596584
No in vitro potency data available.
In cell potency
| Target name | Target information | Species | Assay description | A-1596586 | A-1596584 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| CFTR | primary human bronchial epithelial (HBE) cells from F508del CF patients | Homo sapiens | HBE-TECC (Human Bronchial Epithelial- Trans-Epithelial Current Clamp) assay | EC50 = 28 nM | EC50 > 3 µM | PMID: 29251932 |
| CFTR | Homo sapiens | CSE-HRP surface expression (Cell surface expression-horseradish peroxidase) assay | EC50 = 130 nM | EC50 = 1 µM | PMID: 29251932 | |
| CFTR | Homo sapiens | CSE-HRP cell viability (Cell surface expression-horseradish peroxidase) assay | EC50 > 20 µM | EC50 > 20 µM | PMID: 29251932 | |
| CFTR | U2OS cell line | Homo sapiens | Plasma membrane-expressed enzyme acceptor protein (EA-MEM) assay: F508del CFTR is tagged with a ProLink™ peptide which can complement with a plasma membrane-expressed enzyme acceptor protein (EA-MEM). When the ProLink™ and EA-MEM acceptor are in close proximity i.e. both are located at the plasma membrane, a functional enzyme is formed at which the activity can be measured. | EC50 = 35 nM | EC50 = 3.9 µM | PMID: 29251932 |