Proteins > cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
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cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
A cAMP and cAMP-inhibited cGMP 3,5-cyclic phosphodiesterase 10A that is encoded in the genome of rat. [OMA:Q9QYJ6, PRO:DNx]
Synonyms
EC 3.1.4.17;
EC 3.1.4.35
Research
Bioassay Publications (9)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 2 (22.22) | 29.6817 |
| 2010's | 7 (77.78) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (2)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| papaverine | Rattus norvegicus (Norway rat) | IC50 | 0.0360 | 4 | 4 |
| papaverine | Rattus norvegicus (Norway rat) | Ki | 0.2377 | 1 | 3 |
| pf-2545920 | Rattus norvegicus (Norway rat) | IC50 | 0.0004 | 6 | 7 |
| pf-2545920 | Rattus norvegicus (Norway rat) | Ki | 0.0002 | 1 | 1 |
Benzothiophene derivatives as phosphodiesterase 10A (PDE10A) inhibitors: Hit-to-lead studies.Bioorganic & medicinal chemistry letters, , 06-01, Volume: 29, Issue:11, 2019
Inhibitors of phosphodiesterase as cancer therapeutics.European journal of medicinal chemistry, , Apr-25, Volume: 150, 2018
Fragment-assisted hit investigation involving integrated HTS and fragment screening: Application to the identification of phosphodiesterase 10A (PDE10A) inhibitors.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 26, Issue:1, 2016
Synthesis and in vitro evaluation of new analogues as inhibitors for phosphodiesterase 10A.European journal of medicinal chemistry, , Volume: 46, Issue:9, 2011
Discovery of a series of 6,7-dimethoxy-4-pyrrolidylquinazoline PDE10A inhibitors.Journal of medicinal chemistry, , Jan-25, Volume: 50, Issue:2, 2007
Discovery of a potent, selective, and orally active phosphodiesterase 10A inhibitor for the potential treatment of schizophrenia.Journal of medicinal chemistry, , May-22, Volume: 57, Issue:10, 2014
Rapid identification of a novel small molecule phosphodiesterase 10A (PDE10A) tracer.Journal of medicinal chemistry, , May-24, Volume: 55, Issue:10, 2012
Synthesis, in vivo occupancy, and radiolabeling of potent phosphodiesterase subtype-10 inhibitors as candidates for positron emission tomography imaging.Journal of medicinal chemistry, , Aug-25, Volume: 54, Issue:16, 2011
Synthesis and in vitro evaluation of new analogues as inhibitors for phosphodiesterase 10A.European journal of medicinal chemistry, , Volume: 46, Issue:9, 2011
Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia.Journal of medicinal chemistry, , Aug-27, Volume: 52, Issue:16, 2009