Potency data for probe ABT-546 and control A-545
In vitro potency
| Target name | Target information | Species | Assay description | ABT-546 | A-545 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| EDNRA | Membranes prepared from CHO cells stably transfected with human EDNRA and EDNRB | Homo sapiens | [125I]-endothelin-1 saturation binding | Ki = 0.46 nM ± 0.030 nM (n=3) | Ki = 13000 nM (n=1) | PMID: 10082200 |
| EDNRA, METAP2 | Membranes prepared from CHO cells stably transfected with human EDNRA and EDNRB | Homo sapiens | Inhibition of [125I]-endothelin-1 binding to EDNRA | IC50 = 0.49 nM ± 0.040 nM (n=4) | PMID: 10082200 | |
| EDNRB | Membranes prepared from CHO cells stably transfected with human EDNRA and EDNRB | Homo sapiens | Inhibition of [125I]-endothelin-3 binding to EDNRB | IC50 = 15400 nM ± 1600.000 nM (n=4) | PMID: 10082200 |
In cell potency
| Target name | Target information | Species | Assay description | ABT-546 | A-545 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| EDNRA | MMQ cells (which contain predominantly EDNRA) | Homo sapiens | Endothelin-1-evoked phosphatidylinositol hydrolysis | IC50 = 0.59 nM | PMID: 10082200 |