Potency data for probe BAY-6096 and control BAY-726
In vitro potency
| Target name | Target information | Species | Assay description | BAY-6096 | BAY-726 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| ADRA2B | recombinant; full length | Homo sapiens | Radiometric ADRA2B binding assay (Eurofins #203710) | Ki = 21 nM | Eurofins assay | |
| DRD2 | Homo sapiens | Bayer Inhouse kinase panel (DRD2) | IC50 = 1.4 µM | IC50 > 20 µM |
In cell potency
| Target name | Target information | Species | Assay description | BAY-6096 | BAY-726 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| ADRA2B | recombinant alpha2B receptor CHO cell line (PerkinElmer Life Sciences), also expressing recombinant mtAeq | Homo sapiens | Adrenoceptor Reporter Cell Assay (ADRA2B) | IC50 = 14 nM | IC50 = 7.1 µM | PMID: 36932954 |
| ADRA1A | recombinant alpha1A receptor CHO cell line, also expressing recombinant mtAeq (mitochondrial aequorin) | Homo sapiens | Adrenoceptor reporter cell assay (ADRA1A) | IC50 = 5.516 µM | IC50 > 10 µM | PMID: 36932954 |
| ADRA1B | Homo sapiens | Adrenoceptor reporter cell assay (ADRA1B) | IC50 > 10 µM | PMID: 36932954 | ||
| ADRA1D | Homo sapiens | Adrenoceptor reporter cell assay (ADRA1D) | IC50 > 10 µM | PMID: 36932954 | ||
| ADRA2A | recombinant alpha2A-Galpha16 receptor fusion protein CHO cell line (PerkinElmer Life Sciences), also expressing recombinant mtAeq | Homo sapiens | Adrenoceptor reporter cell assay (ADRA2A) | IC50 = 10 µM | IC50 > 10 µM | PMID: 36932954 |
| ADRA2C | recombinant alpha2C receptor HEK cell line, also expressing a chimeric G protein (Galphaqi3) and Clytin | Homo sapiens | Adrenoceptor reporter cell assay (ADRA2C) | IC50 > 11.83 µM | IC50 > 10 µM | PMID: 36932954 |
| ADRB1 | Homo sapiens | Adrenoceptor reporter cell assay (ADRB1) | IC50 > 10 µM | PMID: 36932954 | ||
| ADRB2 | Homo sapiens | Adrenoceptor reporter cell assay (ADRB2) | IC50 > 10 µM | PMID: 36932954 | ||
| ADRB3 | Homo sapiens | Adrenoceptor reporter cell assay (ADRB3) | IC50 > 10 µM | PMID: 36932954 | ||
| ADRA2B | Rattus norvegicus | Cell based assay rat (ADRA2B) | IC50 = 13 nM | PMID: 36932954 | ||
| ADRA2B | Canis lupus familiaris | Cell based assay dog (ADRA2B) | IC50 = 25 nM | IC50 = 10 µM | PMID: 36932954 | |
| ADRA2B | deletion of three glutamate residues in an acidic stretch of 18 amino acids (of which 15 are glutamates) located in third intracellular loop | Homo sapiens | Adrenoceptor Reporter Cell Assay (ADRA2B deletion mutant): Mutant has a higher risk for myocardial infarction. | IC50 = 25 nM |