Potency data for probe BAY-7081 and control BAY-7424
In vitro potency
| Target name | Target information | Species | Assay description | BAY-7081 | BAY-7424 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| PDE9A | recombinant protein expressed in Sf9 insect cells; full-length human | Homo sapiens | 3H-cAMP and 3H-cGMP Scintillation Proximity Assay (PDE9A): SPA assay system from Perkin Elmer | IC50 = 15 nM | IC50 > 10 µM | PMID: 36475653 |
| PDE1 | bovine brain PDE1 mixture from Sigma-Aldrich | Bos taurus | 3H-cAMP and 3H-cGMP Scintillation Proximity Assay (PDE1): SPA assay system from Perkin Elmer | IC50 = 0.753 µM | PMID: 36475653 | |
| PDE2A | recombinant protein expressed in Sf9 insect cells; full-length human | Homo sapiens | 3H-cAMP and 3H-cGMP Scintillation Proximity Assay (PDE2A): SPA assay system from Perkin Elmer | IC50 > 10 µM | PMID: 36475653 | |
| PDE3B | recombinant protein expressed in Sf9 insect cells; full-length human | Homo sapiens | 3H-cAMP and 3H-cGMP Scintillation Proximity Assay (PDE3B): SPA assay system from Perkin Elmer | IC50 > 10 µM | PMID: 36475653 | |
| PDE4B | recombinant protein expressed in Sf9 insect cells; full-length human | Homo sapiens | 3H-cAMP and 3H-cGMP Scintillation Proximity Assay (PDE4B): SPA assay system from Perkin Elmer | IC50 = 3.96 µM | PMID: 36475653 | |
| PDE5A | purified from human platelets; full-length human | Homo sapiens | 3H-cAMP and 3H-cGMP Scintillation Proximity Assay (PDE5A): SPA assay system from Perkin Elmer | IC50 = 2.98 µM | PMID: 36475653 | |
| PDE6 | purified from rod outer segments (ROS) of bovine retinae (bovine protein mix) | Bos taurus | 3H-cAMP and 3H-cGMP Scintillation Proximity Assay (PDE6): SPA assay system from Perkin Elmer | IC50 = 1.56 µM | PMID: 36475653 | |
| PDE7B | recombinant protein expressed in Sf9 insect cells; full-length human | Homo sapiens | 3H-cAMP and 3H-cGMP Scintillation Proximity Assay (PDE7B): SPA assay system from Perkin Elmer | IC50 > 10 µM | PMID: 36475653 | |
| PDE8A | recombinant protein expressed in Sf9 insect cells; full-length human | Homo sapiens | 3H-cAMP and 3H-cGMP Scintillation Proximity Assay (PDE8A): SPA assay system from Perkin Elmer | IC50 = 1.49 µM | PMID: 36475653 | |
| PDE10A | recombinant protein expressed in Sf9 insect cells; full-length human | Homo sapiens | 3H-cAMP and 3H-cGMP Scintillation Proximity Assay (PDE10A): SPA assay system from Perkin Elmer | IC50 > 10 µM | PMID: 36475653 | |
| PDE11A | recombinant protein expressed in Sf9 insect cells; full-length human | Homo sapiens | 3H-cAMP and 3H-cGMP Scintillation Proximity Assay (PDE11A): SPA assay system from Perkin Elmer | IC50 = 6.6 µM | PMID: 36475653 | |
| PDE1A | recombinant protein expressed in Sf9 insect cells; full-length human | Homo sapiens | Panlabs assay PDE1A | Inhibition = 7.7% | ||
| PDE2A | recombinant protein expressed in Sf9 insect cells | Homo sapiens | Panlabs assay PDE2A | Inhibition = 3.5% | ||
| PDE3A | recombinant protein expressed in Sf9 insect cells | Homo sapiens | Panlabs assay PDE3A | Inhibition = -1.3% | ||
| PDE3B | recombinant protein expressed in Sf9 insect cells | Homo sapiens | Panlabs assay PDE3B | Inhibition = 0.8% | ||
| PDE4A | recombinant protein expressed in Sf9 insect cells; splice variant 1A: PDE4A1A | Homo sapiens | Panlabs assay PDE4A1A | Inhibition = 6.8% | ||
| PDE4B | recombinant protein expressed in Sf9 insect cells; splice variant 1: PDE4B1 | Homo sapiens | Panlabs assay PDE4B1 | Inhibition = 10.6% | ||
| PDE4C | recombinant protein expressed in Sf9 insect cells; splice variant 1: PDE4C1 | Homo sapiens | Panlabs assay PDE4C1 | Inhibition = 28.6% | ||
| PDE4D | recombinant protein expressed in Sf9 insect cells; splice variant 2: PDE4D2 | Homo sapiens | Panlabs assay PDE4D2 | Inhibition = 19.1% | ||
| PDE5A | recombinant protein expressed in Sf9 insect cells | Homo sapiens | Panlabs assay PDE5A | Inhibition = 12.2% | ||
| PDE6 | Bovine retina | Bos taurus | Panlabs assay PDE6 | Inhibition = 16.7% | ||
| PDE7A | recombinant protein expressed in Sf9 insect cells | Homo sapiens | Panlabs assay PDE7A | Inhibition = -1.6% | ||
| PDE7B | recombinant protein expressed in Sf9 insect cells | Homo sapiens | Panlabs assay PDE7B | Inhibition = -2.1% | ||
| PDE8A | recombinant protein expressed in Sf9 insect cells; splice variant 1: PDE8A1 | Homo sapiens | Panlabs assay PDE8A1 | Inhibition = 2.9% | ||
| PDE9A | recombinant protein expressed in Sf9 insect cells; splice variant 2: PDE9A2 | Homo sapiens | Panlabs assay PDE9A2 | IC50 = 7.47 µM | ||
| PDE10A | recombinant protein expressed in Sf9 insect cells; splice variant 2: PDE10A2 | Homo sapiens | Panlabs assay PDE10A2 | Inhibition = 1.6% | ||
| PDE11A | recombinant protein expressed in Sf9 insect cells; splice variant 4: PDE11A4 | Homo sapiens | Panlabs assay PDE11A4 | Inhibition = 1.3% |
In cell potency
| Target name | Target information | Species | Assay description | BAY-7081 | BAY-7424 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| PDE9A | recombinant CHO cell line stably expressing murine PDE9A | Mus musculus | Cellular PDE9A assay | EC50 = 995 nM | EC50 > 10 µM | PMID: 36475653 |