Potency data for probe A-192621 and control A-1806262
In vitro potency
| Target name | Target information | Species | Assay description | A-192621 | A-1806262 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| EDNRB | Membranes (20 µg) prepared from CHO cells stably transfected with the human EDNRA | Homo sapiens | Inhibition of 125I labeled ET-3 binding to EDNRB | IC50 = 4.5 nM ± 0.910 nM (n=3) | PMID: 12193066 | |
| EDNRA | Membranes (20 µg) prepared from CHO cells stably transfected with the human EDNRA | Homo sapiens | Inhibition of 125I labeled ET-1 binding to EDNRA | IC50 = 4280 nM ± 1610.000 nM (n=3) | PMID: 12193066 | |
| EDNRB | Homo sapiens | 125I-labelled ET-1 saturation binding studies with EDNRB | Ki = 8.8 nM ± 1.510 nM (n=3) | PMID: 12193066 | ||
| EDNRA | Homo sapiens | 125I-labelled ET-1 saturation binding studies with EDNRA | Ki = 5600 nM ± 1520.000 nM (n=3) | PMID: 12193066 |
In cell potency
| Target name | Target information | Species | Assay description | A-192621 | A-1806262 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| EDNRB | CHO cells stably transfected with human EDNRB | Homo sapiens | EDNRB- dependent phosphatidylinositol hydrolysis assay | IC50 = 0.8 nM (n=3) | PMID: 12193066 | |
| EDNRA | MMQ cells (which contain predominantly EDNRA) | Homo sapiens | EDNRA- dependent phosphatidylinositol hydrolysis assay | IC50 > 1000 nM | PMID: 12193066 | |
| EDNRB | Homo sapiens | Eurofins cellular functional assay - Antagonist (EDNRB) | IC50 = 6.5 nM | IC50 = 1 µM | ||
| EDNRA | Homo sapiens | Eurofins cellular functional assay - Antagonist (EDNRA) | IC50 = 3.6 µM | IC50 = 1.6 µM |