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 profile

ID Source	ID
PubMed CID	135564558
CHEMBL ID	2179105
SCHEMBL ID	1716847
SCHEMBL ID	20588503
MeSH ID	M0573888

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

Excerpt	Reference
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."	( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019)
" We herein report the identification of BAY-7081, a potent, selective, and orally bioavailable PDE9A inhibitor with very good aqueous solubility starting from a high-throughput screening hit."	( BAY-7081: A Potent, Selective, and Orally Bioavailable Cyanopyridone-Based PDE9A Inhibitor. Andreevski, AL; Anlauf, S; Bogner, P; Dieskau, AP; Dreher, J; Eitner, F; Fliegner, D; Follmann, M; Gericke, KM; Maassen, S; Meibom, D; Meyer, J; Micus, S; Schlemmer, KH; Steuber, H; Tersteegen, A; von Buehler, CJ; Wunder, F, 2022)

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
cGMP-specific 3',5'-cyclic phosphodiesterase	Homo sapiens (human)	IC50 (µMol)	10.0000	0.0000	1.1843	9.6140	AID708583
High affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9A	Homo sapiens (human)	IC50 (µMol)	0.0184	0.0080	1.1617	5.6000	AID1413085; AID1872588; AID1895838; AID708596
cAMP-specific 3',5'-cyclic phosphodiesterase 4C	Homo sapiens (human)	IC50 (µMol)	10.0000	0.0000	1.4651	10.0000	AID708585
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1C	Homo sapiens (human)	IC50 (µMol)	1.3940	0.2300	1.9814	9.0000	AID708595
cGMP-inhibited 3',5'-cyclic phosphodiesterase A	Homo sapiens (human)	IC50 (µMol)	10.0000	0.0003	1.9901	10.0000	AID708584
cAMP-specific 3',5'-cyclic phosphodiesterase 7B	Homo sapiens (human)	IC50 (µMol)	10.0000	0.0000	2.0513	9.2000	AID708581
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
High affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9A	Mus musculus (house mouse)	EC50 (µMol)	1.7000	1.7000	1.7000	1.7000	AID1897927
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
positive regulation of cardiac muscle hypertrophy	cGMP-specific 3',5'-cyclic phosphodiesterase	Homo sapiens (human)
regulation of nitric oxide mediated signal transduction	cGMP-specific 3',5'-cyclic phosphodiesterase	Homo sapiens (human)
T cell proliferation	cGMP-specific 3',5'-cyclic phosphodiesterase	Homo sapiens (human)
negative regulation of T cell proliferation	cGMP-specific 3',5'-cyclic phosphodiesterase	Homo sapiens (human)
cGMP catabolic process	cGMP-specific 3',5'-cyclic phosphodiesterase	Homo sapiens (human)
oocyte development	cGMP-specific 3',5'-cyclic phosphodiesterase	Homo sapiens (human)
negative regulation of cardiac muscle contraction	cGMP-specific 3',5'-cyclic phosphodiesterase	Homo sapiens (human)
relaxation of cardiac muscle	cGMP-specific 3',5'-cyclic phosphodiesterase	Homo sapiens (human)
positive regulation of oocyte development	cGMP-specific 3',5'-cyclic phosphodiesterase	Homo sapiens (human)
cAMP-mediated signaling	cGMP-specific 3',5'-cyclic phosphodiesterase	Homo sapiens (human)
signal transduction	High affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9A	Homo sapiens (human)
positive regulation of cardiac muscle hypertrophy	High affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9A	Homo sapiens (human)
cGMP metabolic process	High affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9A	Homo sapiens (human)
cGMP catabolic process	High affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9A	Homo sapiens (human)
positive regulation of long-term synaptic potentiation	High affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9A	Homo sapiens (human)
negative regulation of neural precursor cell proliferation	High affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9A	Homo sapiens (human)
cAMP-mediated signaling	High affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9A	Homo sapiens (human)
behavioral fear response	High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8B	Homo sapiens (human)
cAMP catabolic process	High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8B	Homo sapiens (human)
visual learning	High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8B	Homo sapiens (human)
operant conditioning	High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8B	Homo sapiens (human)
neuromuscular process controlling balance	High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8B	Homo sapiens (human)
negative regulation of insulin secretion involved in cellular response to glucose stimulus	High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8B	Homo sapiens (human)
negative regulation of steroid hormone biosynthetic process	High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8B	Homo sapiens (human)
cAMP-mediated signaling	High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8B	Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascade	High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8B	Homo sapiens (human)
cAMP catabolic process	cAMP-specific 3',5'-cyclic phosphodiesterase 4C	Homo sapiens (human)
cAMP-mediated signaling	cAMP-specific 3',5'-cyclic phosphodiesterase 4C	Homo sapiens (human)
cAMP-mediated signaling	Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1C	Homo sapiens (human)
oocyte maturation	cGMP-inhibited 3',5'-cyclic phosphodiesterase A	Homo sapiens (human)
lipid metabolic process	cGMP-inhibited 3',5'-cyclic phosphodiesterase A	Homo sapiens (human)
G protein-coupled receptor signaling pathway	cGMP-inhibited 3',5'-cyclic phosphodiesterase A	Homo sapiens (human)
response to xenobiotic stimulus	cGMP-inhibited 3',5'-cyclic phosphodiesterase A	Homo sapiens (human)
cAMP-mediated signaling	cGMP-inhibited 3',5'-cyclic phosphodiesterase A	Homo sapiens (human)
cGMP-mediated signaling	cGMP-inhibited 3',5'-cyclic phosphodiesterase A	Homo sapiens (human)
regulation of meiotic nuclear division	cGMP-inhibited 3',5'-cyclic phosphodiesterase A	Homo sapiens (human)
negative regulation of apoptotic process	cGMP-inhibited 3',5'-cyclic phosphodiesterase A	Homo sapiens (human)
negative regulation of vascular permeability	cGMP-inhibited 3',5'-cyclic phosphodiesterase A	Homo sapiens (human)
positive regulation of vascular permeability	cGMP-inhibited 3',5'-cyclic phosphodiesterase A	Homo sapiens (human)
steroid hormone mediated signaling pathway	cGMP-inhibited 3',5'-cyclic phosphodiesterase A	Homo sapiens (human)
negative regulation of cAMP-mediated signaling	cGMP-inhibited 3',5'-cyclic phosphodiesterase A	Homo sapiens (human)
positive regulation of oocyte development	cGMP-inhibited 3',5'-cyclic phosphodiesterase A	Homo sapiens (human)
regulation of ribonuclease activity	cGMP-inhibited 3',5'-cyclic phosphodiesterase A	Homo sapiens (human)
cellular response to cGMP	cGMP-inhibited 3',5'-cyclic phosphodiesterase A	Homo sapiens (human)
cellular response to transforming growth factor beta stimulus	cGMP-inhibited 3',5'-cyclic phosphodiesterase A	Homo sapiens (human)
apoptotic signaling pathway	cGMP-inhibited 3',5'-cyclic phosphodiesterase A	Homo sapiens (human)
negative regulation of adenylate cyclase-activating G protein-coupled receptor signaling pathway	cGMP-inhibited 3',5'-cyclic phosphodiesterase A	Homo sapiens (human)
cAMP catabolic process	cAMP-specific 3',5'-cyclic phosphodiesterase 7B	Homo sapiens (human)
signal transduction	cAMP-specific 3',5'-cyclic phosphodiesterase 7B	Homo sapiens (human)
chemical synaptic transmission	cAMP-specific 3',5'-cyclic phosphodiesterase 7B	Homo sapiens (human)
cAMP-mediated signaling	cAMP-specific 3',5'-cyclic phosphodiesterase 7B	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
3',5'-cyclic-nucleotide phosphodiesterase activity	cGMP-specific 3',5'-cyclic phosphodiesterase	Homo sapiens (human)
protein binding	cGMP-specific 3',5'-cyclic phosphodiesterase	Homo sapiens (human)
cGMP binding	cGMP-specific 3',5'-cyclic phosphodiesterase	Homo sapiens (human)
metal ion binding	cGMP-specific 3',5'-cyclic phosphodiesterase	Homo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activity	cGMP-specific 3',5'-cyclic phosphodiesterase	Homo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activity	cGMP-specific 3',5'-cyclic phosphodiesterase	Homo sapiens (human)
3',5'-cyclic-nucleotide phosphodiesterase activity	High affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9A	Homo sapiens (human)
protein binding	High affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9A	Homo sapiens (human)
metal ion binding	High affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9A	Homo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activity	High affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9A	Homo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activity	High affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9A	Homo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activity	High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8B	Homo sapiens (human)
metal ion binding	High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8B	Homo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activity	High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8B	Homo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activity	cAMP-specific 3',5'-cyclic phosphodiesterase 4C	Homo sapiens (human)
metal ion binding	cAMP-specific 3',5'-cyclic phosphodiesterase 4C	Homo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activity	cAMP-specific 3',5'-cyclic phosphodiesterase 4C	Homo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activity	Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1C	Homo sapiens (human)
calmodulin-activated dual specificity 3',5'-cyclic-GMP, 3',5'-cyclic-AMP phosphodiesterase activity	Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1C	Homo sapiens (human)
calmodulin binding	Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1C	Homo sapiens (human)
metal ion binding	Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1C	Homo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activity	Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1C	Homo sapiens (human)
calmodulin-activated 3',5'-cyclic-GMP phosphodiesterase activity	Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1C	Homo sapiens (human)
3',5'-cyclic-nucleotide phosphodiesterase activity	cGMP-inhibited 3',5'-cyclic phosphodiesterase A	Homo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activity	cGMP-inhibited 3',5'-cyclic phosphodiesterase A	Homo sapiens (human)
cGMP-inhibited cyclic-nucleotide phosphodiesterase activity	cGMP-inhibited 3',5'-cyclic phosphodiesterase A	Homo sapiens (human)
protein binding	cGMP-inhibited 3',5'-cyclic phosphodiesterase A	Homo sapiens (human)
nuclear estrogen receptor activity	cGMP-inhibited 3',5'-cyclic phosphodiesterase A	Homo sapiens (human)
metal ion binding	cGMP-inhibited 3',5'-cyclic phosphodiesterase A	Homo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activity	cGMP-inhibited 3',5'-cyclic phosphodiesterase A	Homo sapiens (human)
estrogen binding	cGMP-inhibited 3',5'-cyclic phosphodiesterase A	Homo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activity	cAMP-specific 3',5'-cyclic phosphodiesterase 7B	Homo sapiens (human)
metal ion binding	cAMP-specific 3',5'-cyclic phosphodiesterase 7B	Homo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activity	cAMP-specific 3',5'-cyclic phosphodiesterase 7B	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
cellular_component	cGMP-specific 3',5'-cyclic phosphodiesterase	Homo sapiens (human)
cytosol	cGMP-specific 3',5'-cyclic phosphodiesterase	Homo sapiens (human)
nucleoplasm	High affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9A	Homo sapiens (human)
endoplasmic reticulum	High affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9A	Homo sapiens (human)
Golgi apparatus	High affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9A	Homo sapiens (human)
cytosol	High affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9A	Homo sapiens (human)
plasma membrane	High affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9A	Homo sapiens (human)
ruffle membrane	High affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9A	Homo sapiens (human)
sarcolemma	High affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9A	Homo sapiens (human)
perikaryon	High affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9A	Homo sapiens (human)
perinuclear region of cytoplasm	High affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9A	Homo sapiens (human)
cellular_component	High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8B	Homo sapiens (human)
cytosol	High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8B	Homo sapiens (human)
perinuclear region of cytoplasm	High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8B	Homo sapiens (human)
nucleus	High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8B	Homo sapiens (human)
cytosol	High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8B	Homo sapiens (human)
extracellular space	cAMP-specific 3',5'-cyclic phosphodiesterase 4C	Homo sapiens (human)
cytosol	cAMP-specific 3',5'-cyclic phosphodiesterase 4C	Homo sapiens (human)
cilium	cAMP-specific 3',5'-cyclic phosphodiesterase 4C	Homo sapiens (human)
cytosol	cAMP-specific 3',5'-cyclic phosphodiesterase 4C	Homo sapiens (human)
nucleus	cAMP-specific 3',5'-cyclic phosphodiesterase 4C	Homo sapiens (human)
perinuclear region of cytoplasm	cAMP-specific 3',5'-cyclic phosphodiesterase 4C	Homo sapiens (human)
lysosome	Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1C	Homo sapiens (human)
cytosol	Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1C	Homo sapiens (human)
neuronal cell body	Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1C	Homo sapiens (human)
cytosol	cGMP-inhibited 3',5'-cyclic phosphodiesterase A	Homo sapiens (human)
membrane	cGMP-inhibited 3',5'-cyclic phosphodiesterase A	Homo sapiens (human)
cytosol	cGMP-inhibited 3',5'-cyclic phosphodiesterase A	Homo sapiens (human)
cytosol	cAMP-specific 3',5'-cyclic phosphodiesterase 7B	Homo sapiens (human)
synapse	cAMP-specific 3',5'-cyclic phosphodiesterase 7B	Homo sapiens (human)
cytosol	cAMP-specific 3',5'-cyclic phosphodiesterase 7B	Homo sapiens (human)
perinuclear region of cytoplasm	cAMP-specific 3',5'-cyclic phosphodiesterase 7B	Homo sapiens (human)
nucleus	cAMP-specific 3',5'-cyclic phosphodiesterase 7B	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (57)

Assay ID	Title	Year	Journal	Article
AID1296008	Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening	2020	SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1	Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347160	Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347159	Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346986	P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987	P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1897899	Volume 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 analysis	2022	Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24	BAY-7081: A Potent, Selective, and Orally Bioavailable Cyanopyridone-Based PDE9A Inhibitor.
AID708567	Half life in human	2012	Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21	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
AID708566	Procognitive activity in Tg2576 mouse overexpressing amyloid precursor protein assessed as increase in cGMP level in CSF administered as chronic dose relative to control	2012	Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21	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
AID1897905	Oral bioavailability in dog at 1 mg/kg measured over 24 hrs by LC-MS/MS analysis	2022	Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24	BAY-7081: A Potent, Selective, and Orally Bioavailable Cyanopyridone-Based PDE9A Inhibitor.
AID1897951	In 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 weeks	2022	Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24	BAY-7081: A Potent, Selective, and Orally Bioavailable Cyanopyridone-Based PDE9A Inhibitor.
AID708571	Clearance in fasted dog at 0.3 mg/kg, iv	2012	Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21	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
AID1413084	Basic dissociation constant, pKa of compound at 10 uM by UV/Vis spectroscopy	2018	MedChemComm, May-01, Volume: 9, Issue:5	Elucidation of fluorine's impact on p
AID1897927	Inhibition of mouse PDE9A expressed in recombinant CHO cells coexpressing soluble guanylate cyclase incubated for 6 mins by [3H]-cGMP scintillation proximity assay	2022	Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24	BAY-7081: A Potent, Selective, and Orally Bioavailable Cyanopyridone-Based PDE9A Inhibitor.
AID1872590	Ratio of drug concentration in rat brain to plasma	2022	European journal of medicinal chemistry, Mar-15, Volume: 232	Therapeutic potential of phosphodiesterase inhibitors for cognitive amelioration in Alzheimer's disease.
AID708569	Volume of distribution in dog at 0.3 mg/kg, iv and 0.3 mg/kg, po	2012	Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21	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
AID1897947	Toxicity 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 analysis	2022	Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24	BAY-7081: A Potent, Selective, and Orally Bioavailable Cyanopyridone-Based PDE9A Inhibitor.
AID708572	Ratio of drug uptake in CSF to fraction unbound in plasma in beagle dog at 1 mg/kg, po by LC-MS/MS analysis	2012	Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21	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
AID1895838	Inhibition of PDE9A (unknown origin)	2021	European journal of medicinal chemistry, Dec-15, Volume: 226	Inhibition of Histone Deacetylase 6 (HDAC6) as a therapeutic strategy for Alzheimer's disease: A review (2010-2020).
AID708577	Inhibition of PDE11	2012	Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21	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
AID1897953	In 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 weeks	2022	Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24	BAY-7081: A Potent, Selective, and Orally Bioavailable Cyanopyridone-Based PDE9A Inhibitor.
AID1897904	MRT in dog at 0.3 mg/kg, iv measured over 24 hrs by LC-MS/MS analysis	2022	Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24	BAY-7081: A Potent, Selective, and Orally Bioavailable Cyanopyridone-Based PDE9A Inhibitor.
AID708587	Inhibition of PDE2	2012	Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21	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
AID708585	Inhibition of PDE4C	2012	Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21	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
AID708592	Binding affinity to MDR assessed as efflux ratio of permeability from basal to apical to apical to basal side	2012	Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21	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
AID708576	Ratio 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 analysis	2012	Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21	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
AID708590	Drug uptake in Sprague-Dawley rat brain at 1 mg/kg, sc administered as bolus dose measured at 0.5 hrs by LC-MS/MS analysis	2012	Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21	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
AID1897900	MRT in Wistar rat at 0.3 mg/kg, iv measured over 24 hrs by LC-MS/MS analysis	2022	Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24	BAY-7081: A Potent, Selective, and Orally Bioavailable Cyanopyridone-Based PDE9A Inhibitor.
AID708596	Inhibition of human recombinant PDE9A expressed in Sf9 cells using [3H]cGMP as substrate after 30 mins by scintillation proximity assay	2012	Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21	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
AID708575	Ratio 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 analysis	2012	Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21	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
AID708583	Inhibition of PDE5	2012	Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21	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
AID1413083	Acidic dissociation constant, pKa of compound at 10 uM by UV/Vis spectroscopy	2018	MedChemComm, May-01, Volume: 9, Issue:5	Elucidation of fluorine's impact on p
AID708573	Ratio 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 analysis	2012	Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21	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
AID708595	Inhibition of human recombinant PDE1C expressed in Sf9 cells using [3H]cAMP as substrate after 30 mins by scintillation proximity assay	2012	Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21	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
AID708586	Oral bioavailability in Sprague-Dawley rat at 1 mg/kg	2012	Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21	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
AID1897903	Volume 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 analysis	2022	Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24	BAY-7081: A Potent, Selective, and Orally Bioavailable Cyanopyridone-Based PDE9A Inhibitor.
AID708584	Inhibition of PDE3A	2012	Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21	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
AID1413085	Inhibition of PDE9 (unknown origin) using [3H]-cGMP as substrate after 1 hr by scintillation counting method	2018	MedChemComm, May-01, Volume: 9, Issue:5	Elucidation of fluorine's impact on p
AID708568	Oral bioavailability in dog at 0.3 mg/kg	2012	Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21	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
AID708578	Inhibition of PDE8B	2012	Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21	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
AID1413082	Efflux 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 analysis	2018	MedChemComm, May-01, Volume: 9, Issue:5	Elucidation of fluorine's impact on p
AID1897945	In 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 ELISA	2022	Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24	BAY-7081: A Potent, Selective, and Orally Bioavailable Cyanopyridone-Based PDE9A Inhibitor.
AID1897952	In 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 weeks	2022	Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24	BAY-7081: A Potent, Selective, and Orally Bioavailable Cyanopyridone-Based PDE9A Inhibitor.
AID708580	Inhibition of PDE6	2012	Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21	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
AID1897902	Blood clearance in dog at 1 mg/kg, po or 0.3 mg/kg, iv measured over 24 hrs by LC-MS/MS analysis	2022	Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24	BAY-7081: A Potent, Selective, and Orally Bioavailable Cyanopyridone-Based PDE9A Inhibitor.
AID708570	Clearance in fasted Sprague-Dawley rat at 1 mg/kg, iv	2012	Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21	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
AID708588	Volume of distribution in Sprague-Dawley rat at 1 mg/kg, iv and 1 mg/kg, po	2012	Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21	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
AID1897898	Blood clearance in Wistar rat at 1 mg/kg, po or 0.3 mg/kg, iv measured over 24 hrs by LC-MS/MS analysis	2022	Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24	BAY-7081: A Potent, Selective, and Orally Bioavailable Cyanopyridone-Based PDE9A Inhibitor.
AID708579	Inhibition of PDE10	2012	Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21	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
AID708593	Intrinsic clearance in human liver microsomes at 0.1 uM by LC-MS/MS analysis	2012	Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21	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
AID708581	Inhibition of PDE7B	2012	Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21	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
AID1872588	Inhibition of PDE9 (unknown origin)	2022	European journal of medicinal chemistry, Mar-15, Volume: 232	Therapeutic potential of phosphodiesterase inhibitors for cognitive amelioration in Alzheimer's disease.
AID1897948	Toxicity 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 analysis	2022	Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24	BAY-7081: A Potent, Selective, and Orally Bioavailable Cyanopyridone-Based PDE9A Inhibitor.
AID708582	Procognitive activity in healthy human assessed as increase in cGMP level in CSF at 40 mg, administered as single dose relative to control	2012	Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21	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
AID708589	Ratio 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 analysis	2012	Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21	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
AID1872589	Oral bioavailability in rat	2022	European journal of medicinal chemistry, Mar-15, Volume: 232	Therapeutic potential of phosphodiesterase inhibitors for cognitive amelioration in Alzheimer's disease.
AID708574	Ratio 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 analysis	2012	Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21	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
AID1897901	Oral bioavailability in Wistar rat at 1 mg/kg measured over 24 hrs by LC-MS/MS analysis	2022	Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24	BAY-7081: A Potent, Selective, and Orally Bioavailable Cyanopyridone-Based PDE9A Inhibitor.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	0 (0.00)	29.6817
2010's	3 (37.50)	24.3611
2020's	5 (62.50)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	0 (0.00%)	5.53%
Reviews	2 (25.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	6 (75.00%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
tacrine Tacrine: A cholinesterase inhibitor that crosses the blood-brain barrier. Tacrine has been used to counter the effects of muscle relaxants, as a respiratory stimulant, and in the treatment of Alzheimer's disease and other central nervous system disorders.. tacrine : A member of the class of acridines that is 1,2,3,4-tetrahydroacridine substituted by an amino group at position 9. It is used in the treatment of Alzheimer's disease.	3.41	1	acridines; aromatic amine	EC 3.1.1.7 (acetylcholinesterase) inhibitor
cilostazol [no description available]	3.51	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
rolipram [no description available]	3.51	1	pyrrolidin-2-ones	antidepressant; EC 3.1.4.* (phosphoric diester hydrolase) inhibitor
vorinostat Vorinostat: A hydroxamic acid and anilide derivative that acts as a HISTONE DEACETYLASE inhibitor. It is used in the treatment of CUTANEOUS T-CELL LYMPHOMA and SEZARY SYNDROME.. vorinostat : A dicarboxylic acid diamide comprising suberic (octanedioic) acid coupled to aniline and hydroxylamine. A histone deacetylase inhibitor, it is marketed under the name Zolinza for the treatment of cutaneous T cell lymphoma (CTCL).	3.41	1	dicarboxylic acid diamide; hydroxamic acid	antineoplastic agent; apoptosis inducer; EC 3.5.1.98 (histone deacetylase) inhibitor
papaverine hydrochloride [no description available]	3.51	1
tadalafil [no description available]	3.51	1	benzodioxoles; pyrazinopyridoindole	EC 3.1.4.35 (3',5'-cyclic-GMP phosphodiesterase) inhibitor; vasodilator agent
vinpocetine vinpocetine: whole issue of Arzneim Forsch (23 articles) discuss this drug; Arzneim Forsch 26(10a);1976; RN given refers to parent cpd with unspecified isomeric designation	3.51	1	alkaloid	geroprotector
trichostatin a trichostatin A: chelates zinc ion in the active site of histone deacetylases, resulting in preventing histone unpacking so DNA is less available for transcription; do not confuse with TRICHOSANTHIN which is a protein; found in STREPTOMYCES	3.41	1	antibiotic antifungal agent; hydroxamic acid; trichostatin	bacterial metabolite; EC 3.5.1.98 (histone deacetylase) inhibitor; geroprotector
roflumilast [no description available]	3.51	1	aromatic ether; benzamides; chloropyridine; cyclopropanes; organofluorine compound	anti-asthmatic drug; phosphodiesterase IV inhibitor
3-(n,n-dimethylsulfonamido)-4-methyl-nitrobenzene BRL-50481 : A C-nitro compound that is benzene substituted by N,N-dimethylaminosulfonyl, methyl and nitro groups at positions 1, 2 and 5, respectively. It is a phosphodiesterase inhibitor selective for the PDE7 subtype (Ki = 180 nM).	3.51	1	C-nitro compound; sulfonamide; toluenes	bone density conservation agent; EC 3.1.4.53 (3',5'-cyclic-AMP phosphodiesterase) inhibitor; geroprotector
tubacin tubacin: inhibits histone deacetylase 6; structure in first source	3.41	1	1,3-oxazoles
pf-2545920 [no description available]	3.51	1
(2R,3S)-EHNA hydrochloride (2R,3S)-EHNA hydrochloride : A hydrochloride salt obtained by reaction of (2R,3S)-EHNA with one equivalent of hydrochloric acid. Selective inhibitor of cGMP-stimulated phosphodiesterase (PDE2) (IC50 = 0.8 - 4 mM). Also a potent inhibitor of adenosine deaminase.	3.51	1	hydrochloride	EC 3.1.4.* (phosphoric diester hydrolase) inhibitor; EC 3.5.4.4 (adenosine deaminase) inhibitor
tubastatin a [no description available]	3.41	1	hydroxamic acid; pyridoindole; tertiary amino compound	EC 3.5.1.98 (histone deacetylase) inhibitor
acy-1215 ricolinostat: an HDAC6 inhibitor; structure in first source	3.41	1	pyrimidinecarboxylic acid
acy-738 [no description available]	3.41	1
2-((1-(3-fluorophenyl)cyclohexyl)amino)-n-hydroxypyrimidine-5-carboxamide [no description available]	3.41	1
sildenafil sildenafil : A pyrazolo[4,3-d]pyrimidin-7-one having a methyl substituent at the 1-position, a propyl substituent at the 3-position and a 2-ethoxy-5-[(4-methylpiperazin-1-yl)sulfonyl]phenyl group at the 5-position.	3.51	1	piperazines; pyrazolopyrimidine; sulfonamide	EC 3.1.4.35 (3',5'-cyclic-GMP phosphodiesterase) inhibitor; vasodilator agent
zaprinast zaprinast: anaphylaxis inhibitor; structure	3.51	1	triazolopyrimidines
bay 60-7550 [no description available]	3.51	1

Condition	Indicated	Relationship Strength	Studies
Cognition Disorders Disorders characterized by disturbances in mental processes related to learning, thinking, reasoning, and judgment.	0	2.07	1
Congenital Zika Syndrome [description not available]	0	2.25	1
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	0	2.25	1
Zika Virus Infection A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.	0	2.25	1
Acute Confusional Senile Dementia [description not available]	0	4.15	2
Alzheimer Disease A degenerative disease of the BRAIN characterized by the insidious onset of DEMENTIA. Impairment of MEMORY, judgment, attention span, and problem solving skills are followed by severe APRAXIAS and a global loss of cognitive abilities. The condition primarily occurs after age 60, and is marked pathologically by severe cortical atrophy and the triad of SENILE PLAQUES; NEUROFIBRILLARY TANGLES; and NEUROPIL THREADS. (From Adams et al., Principles of Neurology, 6th ed, pp1049-57)	1	6.15	2
Cardiac Failure [description not available]	0	3.33	4
Heart Failure A heterogeneous condition in which the heart is unable to pump out sufficient blood to meet the metabolic need of the body. Heart failure can be caused by structural defects, functional abnormalities (VENTRICULAR DYSFUNCTION), or a sudden overload beyond its capacity. Chronic heart failure is more common than acute heart failure which results from sudden insult to cardiac function, such as MYOCARDIAL INFARCTION.	0	3.33	4

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

Cross-References

Synonyms (31)

Bioavailability

Protein Targets (8)

Inhibition Measurements

Activation Measurements

Biological Processes (39)

Molecular Functions (12)

Ceullar Components (17)

Bioassays (57)

Research

Studies (8)

Study Types

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

Cross-References

Synonyms (31)

Bioavailability

Protein Targets (8)

Inhibition Measurements

Activation Measurements

Biological Processes (39)

Molecular Functions (12)

Ceullar Components (17)

Bioassays (57)

Research

Studies (8)

Study Types

Related Drugs (20)

Related Conditions (8)