Potency data for probe THPP-1 and control THPP-1-NC
In vitro potency
| Target name | Target information | Species | Assay description | THPP-1 | THPP-1-NC | Publication of assay conditions |
|---|---|---|---|---|---|---|
| PDE10A | Homo sapiens | Biochemical assay (PDE10A): IMAP phosphodiesterase assay (Molecular devices): Measurement of the cAMP accumulation due to inhibition of PDE10A | Ki = 1 nM | Ki = 522 nM | PMID: 22892116 | |
| PDE6A | Homo sapiens | Biochemical assay (PDE6A): IMAP phosphodiesterase assay (Molecular devices) | Ki = 44 nM | Ki = 22.18 µM | PMID: 22892116 | |
| PDE1A | Homo sapiens | Biochemical assay (PDE1A): IMAP phosphodiesterase assay (Molecular devices) | Ki > 50 µM | Ki > 58.33 µM | PMID: 22892116 | |
| PDE2A | Homo sapiens | Biochemical assay (PDE2A): IMAP phosphodiesterase assay (Molecular devices) | Ki = 1200 nM | Ki > 100 µM | PMID: 22892116 | |
| PDE3A | Homo sapiens | Biochemical assay (PDE3A): IMAP phosphodiesterase assay (Molecular devices) | Ki = 3300 nM | Ki > 50 µM | PMID: 22892116 | |
| PDE4A | Homo sapiens | Biochemical assay (PDE4A): IMAP phosphodiesterase assay (Molecular devices) | Ki = 5900 nM | Ki = 9.83 µM | PMID: 22892116 | |
| PDE5A | Homo sapiens | Biochemical assay (PDE5A): IMAP phosphodiesterase assay (Molecular devices) | Ki = 116 nM | Ki = 6.89 µM | PMID: 22892116 | |
| PDE7A | Homo sapiens | Biochemical assay (PDE7A): IMAP phosphodiesterase assay (Molecular devices) | Ki = 11.2 µM | Ki > 25.31 µM | PMID: 22892116 | |
| PDE8A | Homo sapiens | Biochemical assay (PDE8A): IMAP phosphodiesterase assay (Molecular devices) | Ki > 50 µM | Ki > 50 µM | PMID: 22892116 | |
| PDE9A | Homo sapiens | Biochemical assay (PDE9A): IMAP phosphodiesterase assay (Molecular devices) | Ki > 50 µM | Ki > 54.55 µM | PMID: 22892116 | |
| PDE11A | Homo sapiens | Biochemical assay (PDE11A): IMAP phosphodiesterase assay (Molecular devices) | Ki = 298 nM | Ki = 8.8 µM | PMID: 22892116 |
In cell potency
| Target name | Target information | Species | Assay description | THPP-1 | THPP-1-NC | Publication of assay conditions |
|---|---|---|---|---|---|---|
| PDE10A | Homo sapiens | Cell assay | IC50 = 49 nM | PMID: 22892116 |