Compounds > 6-((3s,4s)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl)-1-(tetrahydro-2h-pyran-4-yl)-1,5-dihydro-4h-pyrazolo(3,4-d)pyrimidin-4-one
Page last updated: 2024-08-04 05:55:36

6-((3s,4s)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl)-1-(tetrahydro-2h-pyran-4-yl)-1,5-dihydro-4h-pyrazolo(3,4-d)pyrimidin-4-one

Description

Cross-References

ID SourceID
PubMed CID135564558
CHEMBL ID2179105
SCHEMBL ID1716847
SCHEMBL ID20588503
MeSH IDM0573888

Synonyms (31)

Synonym
pf-04447943
pf-4447943
6-[(3s,4s)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2h-pyran-4-yl)-1,5-dihydro-4h-pyrazolo[3,4-d]pyrimidin-4-one
7rg ,
bdbm50397838
chembl2179105 ,
HY-15441
4h-pyrazolo(3,4-d)pyrimidin-4-one, 1,5-dihydro-6-((3s,4s)-4-methyl-1-(2-pyrimidinylmethyl)-3-pyrrolidinyl)-1-(tetrahydro-2h-pyran-4-yl)-
1082744-20-4
7n969w8y4o ,
unii-7n969w8y4o
6-((3s,4s)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl)-1-(tetrahydro-2h-pyran-4-yl)-1,5-dihydro-4h-pyrazolo(3,4-d)pyrimidin-4-one
CS-0942 ,
IWXUVYOOUMLUTQ-CZUORRHYSA-N
SCHEMBL1716847
6-((3s,4s)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl)-1-(tetrahydro-2h-pyran-4-yl)-1h-pyrazolo[3,4-d]pyrimidin-4(5h)-one
pf 4447943
AKOS030238886
mfcd22665724
NCGC00379008-02
4h-pyrazolo[3,4-d]pyrimidin-4-one, 1,5-dihydro-6-[(3s,4s)-4-methyl-1-(2-pyrimidinylmethyl)-3-pyrrolidinyl]-1-(tetrahydro-2h-pyran-4-yl)-
DB11953
SCHEMBL20588503
6-[(3s,4s)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(oxan-4-yl)-5h-pyrazolo[3,4-d]pyrimidin-4-one
AS-35203
6-[(3s,4s)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2h-pyran-4-yl)-1,5-dihydro-4h pyrazolo[3,4-d]pyrimidin-4-one
Q27268601
DTXSID801025596
EX-A7959
AKOS040742392
PD118512

Protein Targets (8)

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
cGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)IC5010.0000AID708583
High affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)IC500.0184AID1413085; AID1872588; AID1895838; AID708596
High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8BHomo sapiens (human)IC5010.0000AID708578
cAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)IC5010.0000AID708585
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CHomo sapiens (human)IC501.3940AID708595
cGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)IC5010.0000AID708584
cAMP-specific 3',5'-cyclic phosphodiesterase 7BHomo sapiens (human)IC5010.0000AID708581

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
High affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AMus musculus (house mouse)EC501.7000AID1897927

Bioassays (57)

Assay IDTitleYearJournalArticle
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
ISSN: 2472-5560		Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
ISSN: 1091-6490		Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
ISSN: 1091-6490		Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
ISSN: 1521-0111		A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
ISSN: 1521-0111		A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1897899Volume of distribution at steady state in Wistar rat at 1 mg/kg, po or 0.3 mg/kg, iv measured over 24 hrs by LC-MS/MS analysis2022Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24
ISSN: 1520-4804		BAY-7081: A Potent, Selective, and Orally Bioavailable Cyanopyridone-Based PDE9A Inhibitor.
AID708567Half life in human2012Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
ISSN: 1520-4804		Design and discovery of 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one (PF-04447943), a selective brain penetrant PDE9A inhibitor for the treatment of cognitive disor
AID708566Procognitive activity in Tg2576 mouse overexpressing amyloid precursor protein assessed as increase in cGMP level in CSF administered as chronic dose relative to control2012Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
ISSN: 1520-4804		Design and discovery of 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one (PF-04447943), a selective brain penetrant PDE9A inhibitor for the treatment of cognitive disor
AID1897905Oral bioavailability in dog at 1 mg/kg measured over 24 hrs by LC-MS/MS analysis2022Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24
ISSN: 1520-4804		BAY-7081: A Potent, Selective, and Orally Bioavailable Cyanopyridone-Based PDE9A Inhibitor.
AID1897951In vivo inhibition of PDE9A in mouse myocardial hypertrophy model with transverse aortic constriction assessed as reduction of hypertrophy of the left atrium at 10 mg/kg administered twice daily for 5 weeks2022Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24
ISSN: 1520-4804		BAY-7081: A Potent, Selective, and Orally Bioavailable Cyanopyridone-Based PDE9A Inhibitor.
AID708571Clearance in fasted dog at 0.3 mg/kg, iv2012Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
ISSN: 1520-4804		Design and discovery of 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one (PF-04447943), a selective brain penetrant PDE9A inhibitor for the treatment of cognitive disor
AID1413084Basic dissociation constant, pKa of compound at 10 uM by UV/Vis spectroscopy2018MedChemComm, May-01, Volume: 9, Issue:5
ISSN: 2040-2503		Elucidation of fluorine's impact on p
AID1897927Inhibition of mouse PDE9A expressed in recombinant CHO cells coexpressing soluble guanylate cyclase incubated for 6 mins by [3H]-cGMP scintillation proximity assay2022Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24
ISSN: 1520-4804		BAY-7081: A Potent, Selective, and Orally Bioavailable Cyanopyridone-Based PDE9A Inhibitor.
AID1872590Ratio of drug concentration in rat brain to plasma2022European journal of medicinal chemistry, Mar-15, Volume: 232ISSN: 1768-3254Therapeutic potential of phosphodiesterase inhibitors for cognitive amelioration in Alzheimer's disease.
AID708569Volume of distribution in dog at 0.3 mg/kg, iv and 0.3 mg/kg, po2012Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
ISSN: 1520-4804		Design and discovery of 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one (PF-04447943), a selective brain penetrant PDE9A inhibitor for the treatment of cognitive disor
AID1897947Toxicity in rat assessed as increase in blood pressure at 10 to 50 mg/kg, po administered twice daily via gavage and measured every 5 mins by telemetry system based analysis2022Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24
ISSN: 1520-4804		BAY-7081: A Potent, Selective, and Orally Bioavailable Cyanopyridone-Based PDE9A Inhibitor.
AID708572Ratio of drug uptake in CSF to fraction unbound in plasma in beagle dog at 1 mg/kg, po by LC-MS/MS analysis2012Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
ISSN: 1520-4804		Design and discovery of 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one (PF-04447943), a selective brain penetrant PDE9A inhibitor for the treatment of cognitive disor
AID1895838Inhibition of PDE9A (unknown origin)2021European journal of medicinal chemistry, Dec-15, Volume: 226ISSN: 1768-3254Inhibition of Histone Deacetylase 6 (HDAC6) as a therapeutic strategy for Alzheimer's disease: A review (2010-2020).
AID708577Inhibition of PDE112012Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
ISSN: 1520-4804		Design and discovery of 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one (PF-04447943), a selective brain penetrant PDE9A inhibitor for the treatment of cognitive disor
AID1897953In vivo inhibition of PDE9A in mouse myocardial hypertrophy model with transverse aortic constriction assessed as reduction in minimal diastolic left ventricular pressure at 10 mg/kg administered twice daily for 5 weeks2022Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24
ISSN: 1520-4804		BAY-7081: A Potent, Selective, and Orally Bioavailable Cyanopyridone-Based PDE9A Inhibitor.
AID1897904MRT in dog at 0.3 mg/kg, iv measured over 24 hrs by LC-MS/MS analysis2022Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24
ISSN: 1520-4804		BAY-7081: A Potent, Selective, and Orally Bioavailable Cyanopyridone-Based PDE9A Inhibitor.
AID708587Inhibition of PDE22012Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
ISSN: 1520-4804		Design and discovery of 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one (PF-04447943), a selective brain penetrant PDE9A inhibitor for the treatment of cognitive disor
AID708585Inhibition of PDE4C2012Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
ISSN: 1520-4804		Design and discovery of 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one (PF-04447943), a selective brain penetrant PDE9A inhibitor for the treatment of cognitive disor
AID708592Binding affinity to MDR assessed as efflux ratio of permeability from basal to apical to apical to basal side2012Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
ISSN: 1520-4804		Design and discovery of 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one (PF-04447943), a selective brain penetrant PDE9A inhibitor for the treatment of cognitive disor
AID708576Ratio of drug uptake in brain to plasma in FVB/N mouse at 1 mg/kg, sc measured from 0.5 to 2 hrs by LC-MS/MS analysis2012Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
ISSN: 1520-4804		Design and discovery of 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one (PF-04447943), a selective brain penetrant PDE9A inhibitor for the treatment of cognitive disor
AID708590Drug uptake in Sprague-Dawley rat brain at 1 mg/kg, sc administered as bolus dose measured at 0.5 hrs by LC-MS/MS analysis2012Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
ISSN: 1520-4804		Design and discovery of 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one (PF-04447943), a selective brain penetrant PDE9A inhibitor for the treatment of cognitive disor
AID1897900MRT in Wistar rat at 0.3 mg/kg, iv measured over 24 hrs by LC-MS/MS analysis2022Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24
ISSN: 1520-4804		BAY-7081: A Potent, Selective, and Orally Bioavailable Cyanopyridone-Based PDE9A Inhibitor.
AID708596Inhibition of human recombinant PDE9A expressed in Sf9 cells using [3H]cGMP as substrate after 30 mins by scintillation proximity assay2012Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
ISSN: 1520-4804		Design and discovery of 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one (PF-04447943), a selective brain penetrant PDE9A inhibitor for the treatment of cognitive disor
AID708575Ratio of fraction unbound in brain to fraction unbound in plasma in Sprague-Dawley rat at 1 mg/kg, sc measured at 0.5 hrs by LC-MS/MS analysis2012Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
ISSN: 1520-4804		Design and discovery of 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one (PF-04447943), a selective brain penetrant PDE9A inhibitor for the treatment of cognitive disor
AID708583Inhibition of PDE52012Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
ISSN: 1520-4804		Design and discovery of 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one (PF-04447943), a selective brain penetrant PDE9A inhibitor for the treatment of cognitive disor
AID1413083Acidic dissociation constant, pKa of compound at 10 uM by UV/Vis spectroscopy2018MedChemComm, May-01, Volume: 9, Issue:5
ISSN: 2040-2503		Elucidation of fluorine's impact on p
AID708573Ratio of fraction unbound in brain to fraction unbound in plasma in FVB/N mouse at 1 mg/kg, sc measured from 0.5 to 2 hrs by LC-MS/MS analysis2012Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
ISSN: 1520-4804		Design and discovery of 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one (PF-04447943), a selective brain penetrant PDE9A inhibitor for the treatment of cognitive disor
AID708595Inhibition of human recombinant PDE1C expressed in Sf9 cells using [3H]cAMP as substrate after 30 mins by scintillation proximity assay2012Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
ISSN: 1520-4804		Design and discovery of 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one (PF-04447943), a selective brain penetrant PDE9A inhibitor for the treatment of cognitive disor
AID708586Oral bioavailability in Sprague-Dawley rat at 1 mg/kg2012Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
ISSN: 1520-4804		Design and discovery of 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one (PF-04447943), a selective brain penetrant PDE9A inhibitor for the treatment of cognitive disor
AID1897903Volume of distribution at steady state in dog at 1 mg/kg, po or 0.3 mg/kg, iv measured over 24 hrs by LC-MS/MS analysis2022Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24
ISSN: 1520-4804		BAY-7081: A Potent, Selective, and Orally Bioavailable Cyanopyridone-Based PDE9A Inhibitor.
AID708584Inhibition of PDE3A2012Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
ISSN: 1520-4804		Design and discovery of 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one (PF-04447943), a selective brain penetrant PDE9A inhibitor for the treatment of cognitive disor
AID1413085Inhibition of PDE9 (unknown origin) using [3H]-cGMP as substrate after 1 hr by scintillation counting method2018MedChemComm, May-01, Volume: 9, Issue:5
ISSN: 2040-2503		Elucidation of fluorine's impact on p
AID708568Oral bioavailability in dog at 0.3 mg/kg2012Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
ISSN: 1520-4804		Design and discovery of 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one (PF-04447943), a selective brain penetrant PDE9A inhibitor for the treatment of cognitive disor
AID708578Inhibition of PDE8B2012Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
ISSN: 1520-4804		Design and discovery of 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one (PF-04447943), a selective brain penetrant PDE9A inhibitor for the treatment of cognitive disor
AID1413082Efflux ratio of permeability across basolateral to apical over apical to basolateral side in MDCK cells expressing MDR1 at 0.5 uM after 60 mins by LC-MS/MS analysis2018MedChemComm, May-01, Volume: 9, Issue:5
ISSN: 2040-2503		Elucidation of fluorine's impact on p
AID1897945In vivo inhibition of PDE9A in Sprague-Dawley rat assessed as increase in cGMP level in urine at 10 to 50 mg/kg, po measured after 85 mins by ELISA2022Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24
ISSN: 1520-4804		BAY-7081: A Potent, Selective, and Orally Bioavailable Cyanopyridone-Based PDE9A Inhibitor.
AID1897952In vivo inhibition of PDE9A in mouse myocardial hypertrophy model with transverse aortic constriction assessed as improvement of heart function at 10 mg/kg administered twice daily for 5 weeks2022Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24
ISSN: 1520-4804		BAY-7081: A Potent, Selective, and Orally Bioavailable Cyanopyridone-Based PDE9A Inhibitor.
AID708580Inhibition of PDE62012Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
ISSN: 1520-4804		Design and discovery of 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one (PF-04447943), a selective brain penetrant PDE9A inhibitor for the treatment of cognitive disor
AID1897902Blood clearance in dog at 1 mg/kg, po or 0.3 mg/kg, iv measured over 24 hrs by LC-MS/MS analysis2022Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24
ISSN: 1520-4804		BAY-7081: A Potent, Selective, and Orally Bioavailable Cyanopyridone-Based PDE9A Inhibitor.
AID708570Clearance in fasted Sprague-Dawley rat at 1 mg/kg, iv2012Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
ISSN: 1520-4804		Design and discovery of 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one (PF-04447943), a selective brain penetrant PDE9A inhibitor for the treatment of cognitive disor
AID708588Volume of distribution in Sprague-Dawley rat at 1 mg/kg, iv and 1 mg/kg, po2012Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
ISSN: 1520-4804		Design and discovery of 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one (PF-04447943), a selective brain penetrant PDE9A inhibitor for the treatment of cognitive disor
AID1897898Blood clearance in Wistar rat at 1 mg/kg, po or 0.3 mg/kg, iv measured over 24 hrs by LC-MS/MS analysis2022Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24
ISSN: 1520-4804		BAY-7081: A Potent, Selective, and Orally Bioavailable Cyanopyridone-Based PDE9A Inhibitor.
AID708579Inhibition of PDE102012Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
ISSN: 1520-4804		Design and discovery of 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one (PF-04447943), a selective brain penetrant PDE9A inhibitor for the treatment of cognitive disor
AID708593Intrinsic clearance in human liver microsomes at 0.1 uM by LC-MS/MS analysis2012Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
ISSN: 1520-4804		Design and discovery of 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one (PF-04447943), a selective brain penetrant PDE9A inhibitor for the treatment of cognitive disor
AID708581Inhibition of PDE7B2012Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
ISSN: 1520-4804		Design and discovery of 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one (PF-04447943), a selective brain penetrant PDE9A inhibitor for the treatment of cognitive disor
AID1872588Inhibition of PDE9 (unknown origin)2022European journal of medicinal chemistry, Mar-15, Volume: 232ISSN: 1768-3254Therapeutic potential of phosphodiesterase inhibitors for cognitive amelioration in Alzheimer's disease.
AID1897948Toxicity in rat assessed as increase in heart rate at 10 to 50 mg/kg, po administered twice daily via gavage and measured every 5 mins by telemetry system based analysis2022Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24
ISSN: 1520-4804		BAY-7081: A Potent, Selective, and Orally Bioavailable Cyanopyridone-Based PDE9A Inhibitor.
AID708582Procognitive activity in healthy human assessed as increase in cGMP level in CSF at 40 mg, administered as single dose relative to control2012Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
ISSN: 1520-4804		Design and discovery of 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one (PF-04447943), a selective brain penetrant PDE9A inhibitor for the treatment of cognitive disor
AID708589Ratio of drug uptake in brain to plasma in Sprague-Dawley rat at 1 mg/kg, sc measured at 0.5 hrs by LC-MS/MS analysis2012Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
ISSN: 1520-4804		Design and discovery of 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one (PF-04447943), a selective brain penetrant PDE9A inhibitor for the treatment of cognitive disor
AID1872589Oral bioavailability in rat2022European journal of medicinal chemistry, Mar-15, Volume: 232ISSN: 1768-3254Therapeutic potential of phosphodiesterase inhibitors for cognitive amelioration in Alzheimer's disease.
AID708574Ratio of drug uptake in CSF to fraction unbound in plasma in Sprague-Dawley rat at 1 mg/kg, sc measured at 0.5 hrs by LC-MS/MS analysis2012Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
ISSN: 1520-4804		Design and discovery of 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one (PF-04447943), a selective brain penetrant PDE9A inhibitor for the treatment of cognitive disor
AID1897901Oral bioavailability in Wistar rat at 1 mg/kg measured over 24 hrs by LC-MS/MS analysis2022Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24
ISSN: 1520-4804		BAY-7081: A Potent, Selective, and Orally Bioavailable Cyanopyridone-Based PDE9A Inhibitor.

Research

Studies (8)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's3 (37.50)24.3611
2020's5 (62.50)2.80

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews2 (25.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other6 (75.00%)84.16%
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
tacrine
1
acridines;
aromatic amine		EC 3.1.1.7 (acetylcholinesterase) inhibitor202120213.0low000001
cilostazol
1
lactam;
tetrazoles		anticoagulant;
bronchodilator agent;
EC 3.1.4.17 (3',5'-cyclic-nucleotide phosphodiesterase) inhibitor;
fibrin modulating drug;
neuroprotective agent;
platelet aggregation inhibitor;
vasodilator agent		202220222.0low000001
rolipram
1
pyrrolidin-2-onesantidepressant;
EC 3.1.4.* (phosphoric diester hydrolase) inhibitor		202220222.0low000001
vorinostat
1
dicarboxylic acid diamide;
hydroxamic acid		antineoplastic agent;
apoptosis inducer;
EC 3.5.1.98 (histone deacetylase) inhibitor		202120213.0low000001
papaverine hydrochloride
1
202220222.0low000001
tadalafil
1
benzodioxoles;
pyrazinopyridoindole		EC 3.1.4.35 (3',5'-cyclic-GMP phosphodiesterase) inhibitor;
vasodilator agent		202220222.0low000001
vinpocetine
1
alkaloidgeroprotector202220222.0low000001
trichostatin a
1
antibiotic antifungal agent;
hydroxamic acid;
trichostatin		bacterial metabolite;
EC 3.5.1.98 (histone deacetylase) inhibitor;
geroprotector		202120213.0low000001
roflumilast
1
aromatic ether;
benzamides;
chloropyridine;
cyclopropanes;
organofluorine compound		anti-asthmatic drug;
phosphodiesterase IV inhibitor		202220222.0low000001
3-(n,n-dimethylsulfonamido)-4-methyl-nitrobenzene
1
C-nitro compound;
sulfonamide;
toluenes		bone density conservation agent;
EC 3.1.4.53 (3',5'-cyclic-AMP phosphodiesterase) inhibitor;
geroprotector		202220222.0low000001
tubacin
1
1,3-oxazoles202120213.0low000001
pf-2545920
1
202220222.0low000001
(2R,3S)-EHNA hydrochloride
1
hydrochlorideEC 3.1.4.* (phosphoric diester hydrolase) inhibitor;
EC 3.5.4.4 (adenosine deaminase) inhibitor		202220222.0medium000001
tubastatin a
1
hydroxamic acid;
pyridoindole;
tertiary amino compound		EC 3.5.1.98 (histone deacetylase) inhibitor202120213.0low000001
acy-1215
1
pyrimidinecarboxylic acid202120213.0low000001
acy-738
1
202120213.0medium000001
2-((1-(3-fluorophenyl)cyclohexyl)amino)-n-hydroxypyrimidine-5-carboxamide
1
202120213.0medium000001
sildenafil
1
piperazines;
pyrazolopyrimidine;
sulfonamide		EC 3.1.4.35 (3',5'-cyclic-GMP phosphodiesterase) inhibitor;
vasodilator agent		202220222.0low000001
zaprinast
1
triazolopyrimidines202220222.0low000001
bay 60-7550
1
202220222.0medium000001
ConditionIndicatedStudiesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
Acute Confusional Senile Dementia0
2
202120222.5medium000002
Alzheimer Disease1
2
202120222.5medium000002
Cardiac Failure0
2
202220222.0medium000002
Cognition Disorders0
1
2012201212.0low000010
Congenital Zika Syndrome0
1
202020204.0low000010
Disease Models, Animal0
1
202020204.0low000010
Heart Failure0
2
202220222.0medium000002
Zika Virus Infection0
1
202020204.0low000010

Bioavailability (2)

ArticleYear
BAY-7081: A Potent, Selective, and Orally Bioavailable Cyanopyridone-Based PDE9A Inhibitor.
Journal of medicinal chemistry, , 12-22, Volume: 65, Issue:24		2022
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Molecular pharmacology, , Volume: 96, Issue:5		2019