Page last updated: 2024-11-12

pf-2545920

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Cross-References

ID Source	ID
PubMed CID	11581936
CHEMBL ID	562318
SCHEMBL ID	1414700
MeSH ID	M0547755

Synonyms (75)

Synonym
HY-50098
pf-02545920
pf-2545920 ,
mp-10
mardepodect
DB08387
CHEMBL562318
2-{[4-(1-methyl-4-pyridin-4-yl-1h-pyrazol-3-yl)phenoxy]methyl}quinoline
pf9 ,
2-[(4-(1-methyl-4-(pyridin-4-yl)-1h-pyrazol-3-yl)phenoxy)methyl]quinoline
1292799-56-4
FT-0687460
BCP0726000246
NCGC00346630-01
BRD-K31519811-001-01-4
CS-0501
S2687
2-((4-(1-(methyl-11c)-4-(4-pyridinyl)-1h-pyrazol-3-yl)phenoxy)methyl)quinoline
pf-0254920
unii-r9y8ey0g42
mardepodect [usan]
r9y8ey0g42 ,
pf 2545920
2-(4-(1-methyl-4-pyridin-4-yl-1h-pyrazol-3-yl)-phenoxymethyl)quinoline
898562-94-2
quinoline, 2-((4-(1-methyl-4-(4-pyridinyl)-1h-pyrazol-3-yl)phenoxy)methyl)-
AKOS022179845
MLS006011117
smr004702898
bdbm31592
substituted pyrazole, 9
3HR1
mp-10 compound
(11c)mp-10 cpd
((11)c)mp-10
mardepodect [who-dd]
mardepodect [inn]
2-[4-(1-methyl-4-pyridin4-yl-1h-pyrazol-3-yl)-phenoxymethyl]-quinoline
2-[4-(1-methyl-4-pyridin-4-yl-1h-pyrazol-3-yl)-phenoxymethyl]-quinoline
AZEXWHKOMMASPA-UHFFFAOYSA-N
SCHEMBL1414700
pf-2545920 hydrochloride
2-((4-(1-methyl-4-(pyridin-4-yl)-1h-pyrazol-3-yl)phenoxy)methyl)quinoline
AC-32620
2-[[4-(1-methyl-4-pyridin-4-ylpyrazol-3-yl)phenoxy]methyl]quinoline
EX-A949
J-505225
gtpl9617
pyrazole 9 [pmid: 19630403]
pf2545920
mfcd28144518
2-[[4-[1-(methyl-11c)-4-(4-pyridinyl)-1h-pyrazol-3-yl]phenoxy]methyl]quinoline
NCGC00346630-05
SW222234-1
pf-2545920(mp-10)
FT-0700157
BCP05602
2-(4-(1-methyl-4-pyridin-4-yl-1h-pyrazol-3-yl)phenoxymethyl)quinoline
quinoline, 2-[[4-[1-methyl-4-(4-pyridinyl)-1h-pyrazol-3-yl]phenoxy]methyl]-
EX-A2373
[11c]mp 10
pf 2545920;pf2545920;pf-2545920
BCP23364
Q7119048
SB16688
HMS3884H14
HMS3750K09
CCG-268557
mardepodect (usan/inn)
D11171
MS-26564
NCGC00346630-02
YKB56294
DTXSID001025873
AC-36046

Research Excerpts

Bioavailability

Excerpt	Reference	Relevance
"We describe the discovery of potent and orally bioavailable tetrahydropyridopyrimidine inhibitors of phosphodiesterase 10A by systematic optimization of a novel HTS lead."	( Discovery of tetrahydropyridopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia. Breslin, MJ; Coleman, PJ; Cox, CD; Fandozzi, C; Fuerst, J; Hill, N; Huszar, S; Kandebo, M; Kim, SH; Ma, B; McGaughey, G; Raheem, IT; Renger, JJ; Schreier, JD; Sharma, S; Smith, S; Uslaner, J; Yan, Y, 2012)	0.38
" We highlight the discovery of PyP-1, a potent, highly selective, and orally bioavailable pyrazolopyrimidine inhibitor of PDE10A."	( Discovery of pyrazolopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia. Coleman, PJ; Cox, CD; Fuerst, J; Gantert, L; Hostetler, ED; Huszar, S; Joshi, A; Kandebo, M; Kim, SH; Li, J; Ma, B; McGaughey, G; Raheem, IT; Renger, JJ; Schreier, JD; Sharma, S; Shipe, WD; Smith, SM; Uslaner, J; Vandeveer, GH; Yan, Y, 2016)	0.43
"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)	0.51

Dosage Studied

Excerpt	Relevance	Reference
" The compound exhibited high peripheral and adequate brain levels upon oral dosing in rodents."	( Design, synthesis and pharmacological evaluation of novel polycyclic heteroarene ethers as PDE10A inhibitors: part II. Avhad, VB; Bajpai, M; Bhateja, DK; Das, S; Gandhi, MN; Gudi, GS; Gullapalli, S; Gupta, PK; Harde, RL; Jadhav, SB; Joshi, AA; Khairatkar-Joshi, N; Mahat, MY; Marathe, MY; Shelke, DE; Thomas, A, 2014)	0.4

[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (19)

Potency Measurements

Protein	Taxonomy	Measurement	Average (µ)	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
PPM1D protein	Homo sapiens (human)	Potency	16.5388	0.0052	9.4661	32.9993	AID1347411
cytochrome P450 family 3 subfamily A polypeptide 4	Homo sapiens (human)	Potency	0.8487	0.0123	7.9835	43.2770	AID1645841
EWS/FLI fusion protein	Homo sapiens (human)	Potency	17.7023	0.0013	10.1577	42.8575	AID1259252; AID1259253; AID1259255; AID1259256
G	Vesicular stomatitis virus	Potency	0.6008	0.0123	8.9648	39.8107	AID1645842
cytochrome P450 2D6	Homo sapiens (human)	Potency	7.5637	0.0010	8.3798	61.1304	AID1645840
Interferon beta	Homo sapiens (human)	Potency	12.5543	0.0033	9.1582	39.8107	AID1347411; AID1645842
HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)	Potency	0.6008	0.0123	8.9648	39.8107	AID1645842
Inositol hexakisphosphate kinase 1	Homo sapiens (human)	Potency	0.6008	0.0123	8.9648	39.8107	AID1645842
cytochrome P450 2C9, partial	Homo sapiens (human)	Potency	0.6008	0.0123	8.9648	39.8107	AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Chain A, cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A	Rattus norvegicus (Norway rat)	IC50 (µMol)	0.0004	0.0004	0.0004	0.0004	AID977608
Chain A, cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A	Rattus norvegicus (Norway rat)	IC50 (µMol)	0.0004	0.0004	0.0004	0.0004	AID977608
Chain A, cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A	Rattus norvegicus (Norway rat)	IC50 (µMol)	0.0004	0.0004	0.0004	0.0004	AID977608
Chain A, cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A	Rattus norvegicus (Norway rat)	IC50 (µMol)	0.0004	0.0004	0.0004	0.0004	AID977608
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A	Rattus norvegicus (Norway rat)	IC50 (µMol)	0.0004	0.0002	0.0134	0.0360	AID1141259; AID1799159; AID428630; AID615724; AID628043; AID677554
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A	Rattus norvegicus (Norway rat)	Ki	0.0002	0.0002	0.1783	0.4170	AID677554
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A	Homo sapiens (human)	IC50 (µMol)	0.0013	0.0000	1.4904	9.2000	AID1140226; AID1140351; AID1190578; AID1235025; AID1557506; AID484805; AID598564; AID705199; AID767814
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Galectin-3	Homo sapiens (human)	Kd	0.2200	0.1500	0.2200	0.2900	AID1724759; AID1724761
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
High affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9A	Homo sapiens (human)	Activity	0.0021	0.0021	0.0021	0.0021	AID442317
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1C	Homo sapiens (human)	Activity	0.0021	0.0021	0.0021	0.0021	AID442318
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (87)

Process	via Protein(s)	Taxonomy
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)
cell surface receptor signaling pathway via JAK-STAT	Interferon beta	Homo sapiens (human)
response to exogenous dsRNA	Interferon beta	Homo sapiens (human)
B cell activation involved in immune response	Interferon beta	Homo sapiens (human)
cell surface receptor signaling pathway	Interferon beta	Homo sapiens (human)
cell surface receptor signaling pathway via JAK-STAT	Interferon beta	Homo sapiens (human)
response to virus	Interferon beta	Homo sapiens (human)
positive regulation of autophagy	Interferon beta	Homo sapiens (human)
cytokine-mediated signaling pathway	Interferon beta	Homo sapiens (human)
natural killer cell activation	Interferon beta	Homo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT protein	Interferon beta	Homo sapiens (human)
cellular response to interferon-beta	Interferon beta	Homo sapiens (human)
B cell proliferation	Interferon beta	Homo sapiens (human)
negative regulation of viral genome replication	Interferon beta	Homo sapiens (human)
innate immune response	Interferon beta	Homo sapiens (human)
positive regulation of innate immune response	Interferon beta	Homo sapiens (human)
regulation of MHC class I biosynthetic process	Interferon beta	Homo sapiens (human)
negative regulation of T cell differentiation	Interferon beta	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Interferon beta	Homo sapiens (human)
defense response to virus	Interferon beta	Homo sapiens (human)
type I interferon-mediated signaling pathway	Interferon beta	Homo sapiens (human)
neuron cellular homeostasis	Interferon beta	Homo sapiens (human)
cellular response to exogenous dsRNA	Interferon beta	Homo sapiens (human)
cellular response to virus	Interferon beta	Homo sapiens (human)
negative regulation of Lewy body formation	Interferon beta	Homo sapiens (human)
negative regulation of T-helper 2 cell cytokine production	Interferon beta	Homo sapiens (human)
positive regulation of apoptotic signaling pathway	Interferon beta	Homo sapiens (human)
response to exogenous dsRNA	Interferon beta	Homo sapiens (human)
B cell differentiation	Interferon beta	Homo sapiens (human)
natural killer cell activation involved in immune response	Interferon beta	Homo sapiens (human)
adaptive immune response	Interferon beta	Homo sapiens (human)
T cell activation involved in immune response	Interferon beta	Homo sapiens (human)
humoral immune response	Interferon beta	Homo sapiens (human)
positive regulation of T cell mediated cytotoxicity	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
adaptive immune response	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independent	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of T cell anergy	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
defense response	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
immune response	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
detection of bacterium	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of interleukin-12 production	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of interleukin-6 production	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
protection from natural killer cell mediated cytotoxicity	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
innate immune response	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of dendritic cell differentiation	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class Ib	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
positive regulation of dendritic cell differentiation	Galectin-1	Homo sapiens (human)
plasma cell differentiation	Galectin-1	Homo sapiens (human)
apoptotic process	Galectin-1	Homo sapiens (human)
T cell costimulation	Galectin-1	Homo sapiens (human)
regulation of apoptotic process	Galectin-1	Homo sapiens (human)
positive regulation of apoptotic process	Galectin-1	Homo sapiens (human)
positive regulation of canonical NF-kappaB signal transduction	Galectin-1	Homo sapiens (human)
myoblast differentiation	Galectin-1	Homo sapiens (human)
positive regulation of viral entry into host cell	Galectin-1	Homo sapiens (human)
positive regulation of inflammatory response	Galectin-1	Homo sapiens (human)
cell-cell adhesion	Galectin-1	Homo sapiens (human)
positive regulation of dendritic cell differentiation	Galectin-3	Homo sapiens (human)
monocyte chemotaxis	Galectin-3	Homo sapiens (human)
mRNA processing	Galectin-3	Homo sapiens (human)
RNA splicing	Galectin-3	Homo sapiens (human)
neutrophil chemotaxis	Galectin-3	Homo sapiens (human)
epithelial cell differentiation	Galectin-3	Homo sapiens (human)
positive regulation of protein-containing complex assembly	Galectin-3	Homo sapiens (human)
regulation of T cell proliferation	Galectin-3	Homo sapiens (human)
innate immune response	Galectin-3	Homo sapiens (human)
negative regulation of endocytosis	Galectin-3	Homo sapiens (human)
eosinophil chemotaxis	Galectin-3	Homo sapiens (human)
macrophage chemotaxis	Galectin-3	Homo sapiens (human)
negative regulation of T cell receptor signaling pathway	Galectin-3	Homo sapiens (human)
positive chemotaxis	Galectin-3	Homo sapiens (human)
regulation of T cell apoptotic process	Galectin-3	Homo sapiens (human)
mononuclear cell migration	Galectin-3	Homo sapiens (human)
positive regulation of mononuclear cell migration	Galectin-3	Homo sapiens (human)
positive regulation of calcium ion import	Galectin-3	Homo sapiens (human)
regulation of extrinsic apoptotic signaling pathway via death domain receptors	Galectin-3	Homo sapiens (human)
positive regulation of protein localization to plasma membrane	Galectin-3	Homo sapiens (human)
negative regulation of protein tyrosine phosphatase activity	Galectin-3	Homo sapiens (human)
negative regulation of immunological synapse formation	Galectin-3	Homo sapiens (human)
negative regulation of T cell activation via T cell receptor contact with antigen bound to MHC molecule on antigen presenting cell	Galectin-3	Homo sapiens (human)
negative regulation of extrinsic apoptotic signaling pathway	Galectin-3	Homo sapiens (human)
cAMP-mediated signaling	Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1C	Homo sapiens (human)
inositol phosphate metabolic process	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic process	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
negative regulation of cold-induced thermogenesis	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol phosphate biosynthetic process	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
cAMP catabolic process	cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A	Homo sapiens (human)
cGMP catabolic process	cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A	Homo sapiens (human)
negative regulation of cGMP-mediated signaling	cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A	Homo sapiens (human)
cAMP-mediated signaling	cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (38)

Process	via Protein(s)	Taxonomy
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)
cytokine activity	Interferon beta	Homo sapiens (human)
cytokine receptor binding	Interferon beta	Homo sapiens (human)
type I interferon receptor binding	Interferon beta	Homo sapiens (human)
protein binding	Interferon beta	Homo sapiens (human)
chloramphenicol O-acetyltransferase activity	Interferon beta	Homo sapiens (human)
TAP binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
signaling receptor binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
protein binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
peptide antigen binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
TAP binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
protein-folding chaperone binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
RNA binding	Galectin-1	Homo sapiens (human)
protein binding	Galectin-1	Homo sapiens (human)
laminin binding	Galectin-1	Homo sapiens (human)
lactose binding	Galectin-1	Homo sapiens (human)
RNA binding	Galectin-3	Homo sapiens (human)
protein phosphatase inhibitor activity	Galectin-3	Homo sapiens (human)
protein binding	Galectin-3	Homo sapiens (human)
IgE binding	Galectin-3	Homo sapiens (human)
protein phosphatase binding	Galectin-3	Homo sapiens (human)
carbohydrate binding	Galectin-3	Homo sapiens (human)
chemoattractant activity	Galectin-3	Homo sapiens (human)
laminin binding	Galectin-3	Homo sapiens (human)
molecular condensate scaffold activity	Galectin-3	Homo sapiens (human)
disaccharide binding	Galectin-3	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)
inositol-1,3,4,5,6-pentakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol heptakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate 5-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
protein binding	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
ATP binding	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate 1-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate 3-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
3',5'-cyclic-nucleotide phosphodiesterase activity	cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A	Homo sapiens (human)
cGMP-stimulated cyclic-nucleotide phosphodiesterase activity	cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A	Homo sapiens (human)
cAMP binding	cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A	Homo sapiens (human)
cGMP binding	cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A	Homo sapiens (human)
metal ion binding	cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A	Homo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activity	cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A	Homo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activity	cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (35)

Process	via Protein(s)	Taxonomy
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)
extracellular space	Interferon beta	Homo sapiens (human)
extracellular region	Interferon beta	Homo sapiens (human)
Golgi membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
endoplasmic reticulum	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
Golgi apparatus	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
plasma membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
cell surface	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
ER to Golgi transport vesicle membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
secretory granule membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
phagocytic vesicle membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
early endosome membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
recycling endosome membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
extracellular exosome	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
lumenal side of endoplasmic reticulum membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
MHC class I protein complex	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
extracellular space	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
external side of plasma membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
collagen-containing extracellular matrix	Galectin-1	Homo sapiens (human)
extracellular region	Galectin-1	Homo sapiens (human)
extracellular space	Galectin-1	Homo sapiens (human)
cytoplasm	Galectin-1	Homo sapiens (human)
endoplasmic reticulum lumen	Galectin-1	Homo sapiens (human)
cytosol	Galectin-1	Homo sapiens (human)
collagen-containing extracellular matrix	Galectin-1	Homo sapiens (human)
extracellular exosome	Galectin-1	Homo sapiens (human)
galectin complex	Galectin-1	Homo sapiens (human)
extracellular space	Galectin-1	Homo sapiens (human)
collagen-containing extracellular matrix	Galectin-3	Homo sapiens (human)
immunological synapse	Galectin-3	Homo sapiens (human)
extracellular region	Galectin-3	Homo sapiens (human)
extracellular space	Galectin-3	Homo sapiens (human)
nucleus	Galectin-3	Homo sapiens (human)
nucleoplasm	Galectin-3	Homo sapiens (human)
cytoplasm	Galectin-3	Homo sapiens (human)
mitochondrial inner membrane	Galectin-3	Homo sapiens (human)
cytosol	Galectin-3	Homo sapiens (human)
plasma membrane	Galectin-3	Homo sapiens (human)
cell surface	Galectin-3	Homo sapiens (human)
membrane	Galectin-3	Homo sapiens (human)
secretory granule membrane	Galectin-3	Homo sapiens (human)
collagen-containing extracellular matrix	Galectin-3	Homo sapiens (human)
extracellular exosome	Galectin-3	Homo sapiens (human)
ficolin-1-rich granule membrane	Galectin-3	Homo sapiens (human)
spliceosomal complex	Galectin-3	Homo sapiens (human)
cytoplasm	Galectin-3	Homo sapiens (human)
immunological synapse	Galectin-3	Homo sapiens (human)
nucleus	Galectin-3	Homo sapiens (human)
extracellular space	Galectin-3	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)
fibrillar center	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
nucleoplasm	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
cytosol	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
nucleus	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
cytoplasm	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
cytosol	cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (132)

Assay ID	Title	Year	Journal	Article
AID1347092	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347081	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Confirmatory Screen	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
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.
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.
AID1347096	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347095	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347084	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Confirmatory Screen - GLuc reporter signal	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347086	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347083	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347082	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347154	Primary screen GU AMC 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.
AID1347097	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347088	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): Viability assay - Alamar blue signal for LCMV Confirmatory Screen	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1745845	Primary qHTS for Inhibitors of ATXN expression
AID1347108	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630	Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay	2021	Cell reports, 04-27, Volume: 35, Issue:4	A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347091	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347087	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Confirmatory Screen - GLuc reporter signal	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1190578	Binding affinity to PDE10A (unknown origin)	2015	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 25, Issue:4	Synthesis and in vitro characterization of cinnoline and benzimidazole analogues as phosphodiesterase 10A inhibitors.
AID715546	Selectivity ratio of Ki for human PDE11A to Ki for human PDE10A	2012	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18	Discovery of tetrahydropyridopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia.
AID1724759	Binding affinity to recombinant human galectin 3 assessed as dissociation constant by fluorescent anisotropy assay	2020	ACS medicinal chemistry letters, Sep-10, Volume: 11, Issue:9	Quinoline-Pyrazole Scaffold as a Novel Ligand of Galectin-3 and Suppressor of TREM2 Signaling.
AID442318	Binding affinity to PDE1C	2009	Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24	Identification of a brain penetrant PDE9A inhibitor utilizing prospective design and chemical enablement as a rapid lead optimization strategy.
AID428644	Volume of distribution at steady state in Beagle dog at 0.3 mg/kg, iv	2009	Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16	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.
AID767808	Intrinsic clearance in human liver microsomes	2013	Bioorganic & medicinal chemistry, Oct-01, Volume: 21, Issue:19	N-Methylanilide and N-methylbenzamide derivatives as phosphodiesterase 10A (PDE10A) inhibitors.
AID677554	Displacement of [3H]5-(6,7-dimethoxycinnolin-4-yl)-N-isopropyl-3-methylpyridin-2-amine from PDE10A in Sprague-Dawley rat striatum	2012	Journal of medicinal chemistry, May-24, Volume: 55, Issue:10	Rapid identification of a novel small molecule phosphodiesterase 10A (PDE10A) tracer.
AID705195	Selectivity ratio of IC50 for PDE4 to IC50 for PDE10A	2012	Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17	Current landscape of phosphodiesterase 10A (PDE10A) inhibition.
AID1724766	Antiinflammatory activity in mouse BV-2 cells assessed as reduction in Abeta-induced IL-12 release at 10 uM incubated for 12 hrs by ELISA relative to control	2020	ACS medicinal chemistry letters, Sep-10, Volume: 11, Issue:9	Quinoline-Pyrazole Scaffold as a Novel Ligand of Galectin-3 and Suppressor of TREM2 Signaling.
AID1724762	Antiinflammatory activity in mouse BV-2 cells assessed as reduction in Abeta-induced TNFalpha release incubated for 12 hrs by ELISA	2020	ACS medicinal chemistry letters, Sep-10, Volume: 11, Issue:9	Quinoline-Pyrazole Scaffold as a Novel Ligand of Galectin-3 and Suppressor of TREM2 Signaling.
AID715549	Selectivity ratio of Ki for human PDE7A to Ki for human PDE10A	2012	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18	Discovery of tetrahydropyridopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia.
AID615724	Inhibition of rat PDE10A	2011	European journal of medicinal chemistry, Sep, Volume: 46, Issue:9	Synthesis and in vitro evaluation of new analogues as inhibitors for phosphodiesterase 10A.
AID428642	Hepatic clearance in cynomolgus monkey at 0.03 mg/kg, iv	2009	Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16	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.
AID1235025	Inhibition of PDE10A (unknown origin)	2015	Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15	BN/CC isosterism in borazaronaphthalenes towards phosphodiesterase 10A (PDE10A) inhibitors.
AID428650	Half life in cynomolgus monkey at 0.03 mg/kg, iv	2009	Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16	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.
AID428654	Behavioral effect in mouse assessed as conditioned avoidance response at 115 nM plasma exposure	2009	Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16	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.
AID1724764	Antiinflammatory activity in mouse BV-2 cells assessed as reduction in Abeta-induced IL-8 release incubated for 12 hrs by ELISA	2020	ACS medicinal chemistry letters, Sep-10, Volume: 11, Issue:9	Quinoline-Pyrazole Scaffold as a Novel Ligand of Galectin-3 and Suppressor of TREM2 Signaling.
AID705190	Selectivity ratio of IC50 for PDE9 to IC50 for PDE10A	2012	Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17	Current landscape of phosphodiesterase 10A (PDE10A) inhibition.
AID442317	Binding affinity to PDE9A	2009	Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24	Identification of a brain penetrant PDE9A inhibitor utilizing prospective design and chemical enablement as a rapid lead optimization strategy.
AID428628	Increase in cGMP level in sc dosed mouse striatum	2009	Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16	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.
AID1724765	Antiinflammatory activity in mouse BV-2 cells assessed as reduction in Abeta-induced TNFalpha release at 10 uM incubated for 12 hrs by ELISA relative to control	2020	ACS medicinal chemistry letters, Sep-10, Volume: 11, Issue:9	Quinoline-Pyrazole Scaffold as a Novel Ligand of Galectin-3 and Suppressor of TREM2 Signaling.
AID705199	Inhibition of PDE10A	2012	Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17	Current landscape of phosphodiesterase 10A (PDE10A) inhibition.
AID715547	Selectivity ratio of Ki for human PDE9A to Ki for human PDE10A	2012	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18	Discovery of tetrahydropyridopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia.
AID428648	Half life in Beagle dog at 0.3 mg/kg, iv	2009	Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16	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.
AID1141266	Ex vivo PDE10A receptor occupancy in po dosed Wistar rat striatum assessed as inhibition of [3H]-MP10 binding after 1 hr by autoradiography	2014	Journal of medicinal chemistry, May-22, Volume: 57, Issue:10	Discovery of a potent, selective, and orally active phosphodiesterase 10A inhibitor for the potential treatment of schizophrenia.
AID767804	Antipsychotic activity in rat assessed as inhibition of amphetamine-stimulated locomotor activity	2013	Bioorganic & medicinal chemistry, Oct-01, Volume: 21, Issue:19	N-Methylanilide and N-methylbenzamide derivatives as phosphodiesterase 10A (PDE10A) inhibitors.
AID628043	Inhibition of rat recombinant PDE10A expressed in baculovirus infected insect Sf9 cells using [3H]cAMP as substrate after 60 mins by scintillation counting	2011	Journal of medicinal chemistry, Aug-25, Volume: 54, Issue:16	Synthesis, in vivo occupancy, and radiolabeling of potent phosphodiesterase subtype-10 inhibitors as candidates for positron emission tomography imaging.
AID767807	Intrinsic clearance in rat liver microsomes	2013	Bioorganic & medicinal chemistry, Oct-01, Volume: 21, Issue:19	N-Methylanilide and N-methylbenzamide derivatives as phosphodiesterase 10A (PDE10A) inhibitors.
AID1557548	Inhibition of PDE10 in PDGF-BB-induced human pulmonary artery smooth muscle cells assessed as reduction in proliferating cell nuclear antigen at 0.1 to 1 uM after 22 hrs by Western blot analysis	2019	Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7	Validation of Phosphodiesterase-10 as a Novel Target for Pulmonary Arterial Hypertension via Highly Selective and Subnanomolar Inhibitors.
AID428637	Metabolic stability in human liver microsome assessed as intrinsic clearance	2009	Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16	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.
AID615725	Selectivity ratio of IC50 for rat PDE10A to IC50 for rat PDE3B	2011	European journal of medicinal chemistry, Sep, Volume: 46, Issue:9	Synthesis and in vitro evaluation of new analogues as inhibitors for phosphodiesterase 10A.
AID428645	Volume of distribution at steady state in cynomolgus monkey at 0.03 mg/kg, iv	2009	Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16	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.
AID428630	Inhibition of rat recombinant PDE10A transfected in Sf9 cells	2009	Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16	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.
AID715550	Selectivity ratio of Ki for human PDE6A to Ki for human PDE10A	2012	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18	Discovery of tetrahydropyridopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia.
AID1724761	Binding affinity to recombinant human galectin 3 assessed as dissociation constant by SPR assay	2020	ACS medicinal chemistry letters, Sep-10, Volume: 11, Issue:9	Quinoline-Pyrazole Scaffold as a Novel Ligand of Galectin-3 and Suppressor of TREM2 Signaling.
AID1140351	Inhibition of N-terminal GST-tagged human recombinant PDE10A assessed as substrate hydrolysis using [3H]cAMP as substrate after 30 mins by two-step radiometric assay	2014	Bioorganic & medicinal chemistry letters, May-01, Volume: 24, Issue:9	Design, synthesis and pharmacological evaluation of novel polycyclic heteroarene ethers as PDE10A inhibitors: Part I.
AID428636	Efflux ratio of permeability from basolateral to apical side over apical to basolateral side in MDR1 overexpressing MDCK cells	2009	Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16	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.
AID715555	Selectivity ratio of Ki for human PDE1A to Ki for human PDE10A	2012	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18	Discovery of tetrahydropyridopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia.
AID428634	Behavioral effect in sc dosed mouse assessed as conditioned avoidance response after 30 mins	2009	Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16	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.
AID428656	Behavioral effect in sc dosed PDE10A knockout mouse assessed as conditioned avoidance response after 30 mins	2009	Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16	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.
AID705189	Selectivity ratio of IC50 for PDE11 to IC50 for PDE10A	2012	Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17	Current landscape of phosphodiesterase 10A (PDE10A) inhibition.
AID428638	Increase in cGMP level in mouse striatum at 1 mg/kg, sc relative to control	2009	Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16	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.
AID428653	Oral bioavailability in cynomolgus monkey rat at 3 mg/kg, po	2009	Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16	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.
AID428629	Half life in Beagle dog at 3 mg/kg, po	2009	Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16	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.
AID767814	Inhibition of PDE10A (unknown origin)	2013	Bioorganic & medicinal chemistry, Oct-01, Volume: 21, Issue:19	N-Methylanilide and N-methylbenzamide derivatives as phosphodiesterase 10A (PDE10A) inhibitors.
AID428643	Volume of distribution at steady state in Sprague-Dawley rat at 0.1 mg/kg, iv	2009	Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16	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.
AID1557506	Inhibition of human PDE10A2 catalytic domain (446 to 789 residues) expressed in Escherichia coli BL21 cells using [3H]-cGMP as substrate after 15 mins by liquid scintillation analysis	2019	Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7	Validation of Phosphodiesterase-10 as a Novel Target for Pulmonary Arterial Hypertension via Highly Selective and Subnanomolar Inhibitors.
AID1872562	Inhibition of PDE10 (unknown origin)	2022	European journal of medicinal chemistry, Mar-15, Volume: 232	Therapeutic potential of phosphodiesterase inhibitors for cognitive amelioration in Alzheimer's disease.
AID1724767	Inhibition of galectin 3 in mouse BWZ cells transfected with TREM2 and DAP12 assessed as reduction in lacZ activity incubated for 24 hrs by lacZ reporter gene based beta-galactosidase assay	2020	ACS medicinal chemistry letters, Sep-10, Volume: 11, Issue:9	Quinoline-Pyrazole Scaffold as a Novel Ligand of Galectin-3 and Suppressor of TREM2 Signaling.
AID705193	Selectivity ratio of IC50 for PDE5 to IC50 for PDE10A	2012	Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17	Current landscape of phosphodiesterase 10A (PDE10A) inhibition.
AID1141264	Antipsychotic activity in sc dosed Wiga rat assessed as reversal of apomorphine-induced stereotypy treated 30 mins prior to apomorphine challenge measured every 5 mins over first hour after apomorphine injection	2014	Journal of medicinal chemistry, May-22, Volume: 57, Issue:10	Discovery of a potent, selective, and orally active phosphodiesterase 10A inhibitor for the potential treatment of schizophrenia.
AID715552	Selectivity ratio of Ki for human PDE4A to Ki for human PDE10A	2012	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18	Discovery of tetrahydropyridopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia.
AID715551	Selectivity ratio of Ki for human PDE5A to Ki for human PDE10A	2012	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18	Discovery of tetrahydropyridopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia.
AID428649	Half life in Beagle dog at 0.1 mg/kg, po	2009	Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16	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.
AID428655	Unbound fraction in mouse plasma	2009	Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16	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.
AID1557569	Inhibition of PDE10 in PDGF-BB-induced human pulmonary artery smooth muscle cells assessed as increase in alpha-SMA expression at 0.1 to 1 uM after 22 hrs by Western blot analysis	2019	Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7	Validation of Phosphodiesterase-10 as a Novel Target for Pulmonary Arterial Hypertension via Highly Selective and Subnanomolar Inhibitors.
AID428652	Oral bioavailability in Beagle dog at 0.1 mg/kg, po	2009	Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16	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.
AID715548	Selectivity ratio of Ki for human PDE8A to Ki for human PDE10A	2012	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18	Discovery of tetrahydropyridopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia.
AID428640	Hepatic clearance in Sprague-Dawley rat at 0.1 mg/kg, iv	2009	Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16	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.
AID705196	Selectivity ratio of IC50 for PDE2 to IC50 for PDE10A	2012	Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17	Current landscape of phosphodiesterase 10A (PDE10A) inhibition.
AID1724760	Binding affinity to recombinant human galectin 1 assessed as dissociation constant by fluorescent anisotropy assay	2020	ACS medicinal chemistry letters, Sep-10, Volume: 11, Issue:9	Quinoline-Pyrazole Scaffold as a Novel Ligand of Galectin-3 and Suppressor of TREM2 Signaling.
AID1141267	Plasma protein binding in Sprague-Dawley rat at 5 uM after 4.5 hrs	2014	Journal of medicinal chemistry, May-22, Volume: 57, Issue:10	Discovery of a potent, selective, and orally active phosphodiesterase 10A inhibitor for the potential treatment of schizophrenia.
AID1724758	Inhibition of recombinant human galectin-3/recombinant human TREM2 interaction assessed as reduction in TR-FRET signal incubated for 3 hrs by TR-FRET assay	2020	ACS medicinal chemistry letters, Sep-10, Volume: 11, Issue:9	Quinoline-Pyrazole Scaffold as a Novel Ligand of Galectin-3 and Suppressor of TREM2 Signaling.
AID1181667	Antipsychotic activity in Sprague-Dawley rat conditioned avoidance response model assessed as reversal of MK-801-induced stereotypy at 3 mg/kg, ip administered 2 hrs prior to MK-801 challenge measured every 5 mins for 1 hr starting 15 mins post MK-801 inj	2014	Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15	Design, synthesis and pharmacological evaluation of novel polycyclic heteroarene ethers as PDE10A inhibitors: part II.
AID705197	Selectivity ratio of IC50 for PDE3 to IC50 for PDE10A	2012	Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17	Current landscape of phosphodiesterase 10A (PDE10A) inhibition.
AID1140226	Inhibition of full-length human recombinant PDE10A using cyclic AMP as substrate by scintillation proximity assay	2014	Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9	Radiosyntheses and in vivo evaluation of carbon-11 PET tracers for PDE10A in the brain of rodent and nonhuman primate.
AID715554	Selectivity ratio of Ki for human PDE2A to Ki for human PDE10A	2012	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18	Discovery of tetrahydropyridopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia.
AID1141268	Protein binding in Sprague-Dawley rat brain at 5 uM after 5 hrs	2014	Journal of medicinal chemistry, May-22, Volume: 57, Issue:10	Discovery of a potent, selective, and orally active phosphodiesterase 10A inhibitor for the potential treatment of schizophrenia.
AID1181668	Antipsychotic activity in Sprague-Dawley rat conditioned avoidance response model assessed as reversal of MK-801-induced ataxia at 3 mg/kg, ip administered 2 hrs prior to MK-801 challenge measured every 5 mins for 1 hr starting 15 mins post MK-801 injecti	2014	Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15	Design, synthesis and pharmacological evaluation of novel polycyclic heteroarene ethers as PDE10A inhibitors: part II.
AID428647	Half life in Sprague-Dawley rat at 1 mg/kg, po	2009	Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16	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.
AID428639	Increase in cGMP level in mouse striatum at 3.2 mg/kg, sc relative to control	2009	Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16	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.
AID1181666	Antipsychotic activity in Sprague-Dawley rat conditioned avoidance response model assessed as reversal of MK-801-induced locomotion at 3 mg/kg, ip administered 2 hrs prior to MK-801 challenge measured every 5 mins for 1 hr starting 15 mins post MK-801 inj	2014	Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15	Design, synthesis and pharmacological evaluation of novel polycyclic heteroarene ethers as PDE10A inhibitors: part II.
AID1181683	Antipsychotic activity in Sprague-Dawley rat conditioned avoidance response model assessed as avoidance of shock at 3 mg/kg, ip measured after 30 mins relative to vehicle-treated control	2014	Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15	Design, synthesis and pharmacological evaluation of novel polycyclic heteroarene ethers as PDE10A inhibitors: part II.
AID428646	Half life in Sprague-Dawley rat at 0.1 mg/kg, iv	2009	Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16	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.
AID428641	Hepatic clearance in Beagle dog at 0.3 mg/kg, iv	2009	Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16	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.
AID1557570	Inhibition of PDE10 in PDGF-BB-induced human pulmonary artery smooth muscle cells assessed as increase in SM22alpha expression at 0.1 to 1 uM after 22 hrs by Western blot analysis	2019	Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7	Validation of Phosphodiesterase-10 as a Novel Target for Pulmonary Arterial Hypertension via Highly Selective and Subnanomolar Inhibitors.
AID598564	Inhibition of PDE10A	2011	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12	Triazoloquinazolines as a novel class of phosphodiesterase 10A (PDE10A) inhibitors.
AID705191	Selectivity ratio of IC50 for PDE8 to IC50 for PDE10A	2012	Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17	Current landscape of phosphodiesterase 10A (PDE10A) inhibition.
AID715553	Selectivity ratio of Ki for human PDE3A to Ki for human PDE10A	2012	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18	Discovery of tetrahydropyridopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia.
AID1141258	Antipsychotic activity in sc dosed Wiga rat assessed as reversal of phencyclidine-induced hyperlocomotion administered 60 mins prior to PCP challenge measured for 30 mins	2014	Journal of medicinal chemistry, May-22, Volume: 57, Issue:10	Discovery of a potent, selective, and orally active phosphodiesterase 10A inhibitor for the potential treatment of schizophrenia.
AID1235026	Intrinsic clearance in rat liver microsomes	2015	Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15	BN/CC isosterism in borazaronaphthalenes towards phosphodiesterase 10A (PDE10A) inhibitors.
AID615722	Selectivity ratio of IC50 for rat PDE10A to IC50 for rat PDE3A	2011	European journal of medicinal chemistry, Sep, Volume: 46, Issue:9	Synthesis and in vitro evaluation of new analogues as inhibitors for phosphodiesterase 10A.
AID1267480	Aqueous solubility of the compound at pH 7	2016	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 26, Issue:1	Discovery of pyrazolopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia.
AID705194	Selectivity ratio of IC50 for PDE6 to IC50 for PDE10A	2012	Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17	Current landscape of phosphodiesterase 10A (PDE10A) inhibition.
AID1724763	Antiinflammatory activity in mouse BV-2 cells assessed as reduction in Abeta-induced IL-12 release incubated for 12 hrs by ELISA	2020	ACS medicinal chemistry letters, Sep-10, Volume: 11, Issue:9	Quinoline-Pyrazole Scaffold as a Novel Ligand of Galectin-3 and Suppressor of TREM2 Signaling.
AID484805	Inhibition of human recombinant PDE10A expressed in baculovirus-SF21 cell system assessed as hydrolysis of [3H]cAMP after 1 hr by liquid scintillation counting	2010	Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11	Discovery of imidazo[1,5-a]pyrido[3,2-e]pyrazines as a new class of phosphodiesterase 10A inhibitiors.
AID1141259	Inhibition of rat recombinant PDE10A expressed in baculovirus infected Sf9 cells using [3H]cAMP as substrate after 60 mins by TopCount scintillation counting analysis	2014	Journal of medicinal chemistry, May-22, Volume: 57, Issue:10	Discovery of a potent, selective, and orally active phosphodiesterase 10A inhibitor for the potential treatment of schizophrenia.
AID705192	Selectivity ratio of IC50 for PDE7 to IC50 for PDE10A	2012	Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17	Current landscape of phosphodiesterase 10A (PDE10A) inhibition.
AID1724757	Inhibition of recombinant human galectin-3/recombinant human TREM2 interaction assessed as reduction in TR-FRET signal at 10 uM incubated for 3 hrs by TR-FRET assay relative to control	2020	ACS medicinal chemistry letters, Sep-10, Volume: 11, Issue:9	Quinoline-Pyrazole Scaffold as a Novel Ligand of Galectin-3 and Suppressor of TREM2 Signaling.
AID1557547	Inhibition of PDE10 in PDGF-BB-induced human pulmonary artery smooth muscle cells assessed as reduction in osteopontin expression at 0.1 to 1 uM after 22 hrs by Western blot analysis	2019	Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7	Validation of Phosphodiesterase-10 as a Novel Target for Pulmonary Arterial Hypertension via Highly Selective and Subnanomolar Inhibitors.
AID428651	Oral bioavailability in Sprague-Dawley rat at 1 mg/kg, po	2009	Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16	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.
AID615723	Lipophilicity, log D of the compound	2011	European journal of medicinal chemistry, Sep, Volume: 46, Issue:9	Synthesis and in vitro evaluation of new analogues as inhibitors for phosphodiesterase 10A.
AID705198	Selectivity ratio of IC50 for PDE1 to IC50 for PDE10A	2012	Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17	Current landscape of phosphodiesterase 10A (PDE10A) inhibition.
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.
AID1347411	qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary	2020	ACS chemical biology, 07-17, Volume: 15, Issue:7	High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1345255	Human phosphodiesterase 10A (Phosphodiesterases, 3',5'-cyclic nucleotide (PDEs))	2009	Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16	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.
AID1799159	PDE Enzyme Inhibition Assay from Article 10.1021/jm900521k: \\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 t	2009	Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16	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.
AID977608	Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB	2009	Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16	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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (28)

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	2 (7.14)	29.6817
2010's	18 (64.29)	24.3611
2020's	8 (28.57)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 17.29

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

Metric	This Compound (vs All)
Research Demand Index	17.29 (24.57)
Research Supply Index	3.37 (2.92)
Research Growth Index	5.48 (4.65)
Search Engine Demand Index	10.37 (26.88)
Search Engine Supply Index	2.00 (0.95)

This Compound (17.29)

All Compounds (24.57)

Study Types

Publication Type	This drug (%)	All Drugs (%)
Trials	0 (0.00%)	5.53%
Reviews	1 (3.57%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	27 (96.43%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
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
haloperidol Haloperidol: A phenyl-piperidinyl-butyrophenone that is used primarily to treat SCHIZOPHRENIA and other PSYCHOSES. It is also used in schizoaffective disorder, DELUSIONAL DISORDERS, ballism, and TOURETTE SYNDROME (a drug of choice) and occasionally as adjunctive therapy in INTELLECTUAL DISABILITY and the chorea of HUNTINGTON DISEASE. It is a potent antiemetic and is used in the treatment of intractable HICCUPS. (From AMA Drug Evaluations Annual, 1994, p279). haloperidol : A compound composed of a central piperidine structure with hydroxy and p-chlorophenyl substituents at position 4 and an N-linked p-fluorobutyrophenone moiety.	2.48	2	aromatic ketone; hydroxypiperidine; monochlorobenzenes; organofluorine compound; tertiary alcohol	antidyskinesia agent; antiemetic; dopaminergic antagonist; first generation antipsychotic; serotonergic antagonist
papaverine Papaverine: An alkaloid found in opium but not closely related to the other opium alkaloids in its structure or pharmacological actions. It is a direct-acting smooth muscle relaxant used in the treatment of impotence and as a vasodilator, especially for cerebral vasodilation. The mechanism of its pharmacological actions is not clear, but it apparently can inhibit phosphodiesterases and it may have direct actions on calcium channels.. papaverine : A benzylisoquinoline alkaloid that is isoquinoline substituted by methoxy groups at positions 6 and 7 and a 3,4-dimethoxybenzyl group at position 1. It has been isolated from Papaver somniferum.	3.59	8	benzylisoquinoline alkaloid; dimethoxybenzene; isoquinolines	antispasmodic drug; vasodilator agent
risperidone Risperidone: A selective blocker of DOPAMINE D2 RECEPTORS and SEROTONIN 5-HT2 RECEPTORS that acts as an atypical antipsychotic agent. It has been shown to improve both positive and negative symptoms in the treatment of SCHIZOPHRENIA.. risperidone : A member of the class of pyridopyrimidines that is 2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one carrying an additional 2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl group at position 2.	2.49	2	1,2-benzoxazoles; heteroarylpiperidine; organofluorine compound; pyridopyrimidine	alpha-adrenergic antagonist; dopaminergic antagonist; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; H1-receptor antagonist; psychotropic drug; second generation antipsychotic; serotonergic antagonist
rolipram [no description available]	3.51	1	pyrrolidin-2-ones	antidepressant; EC 3.1.4.* (phosphoric diester hydrolase) inhibitor
papaverine hydrochloride [no description available]	3.51	1
ziprasidone ziprasidone: a benzisothiazoylpiperazine derivative; has combined dopamine and serotonin receptor antagonist activity; structurally related to tiospirone. ziprasidone : A piperazine compound having 1,2-benzothiazol-3-yl- and 2-(6-chloro-1,3-dihydro-2-oxindol-5-yl)ethyl substituents attached to the nitrogen atoms.	2.07	1	1,2-benzisothiazole; indolones; organochlorine compound; piperazines	antipsychotic agent; dopaminergic antagonist; histamine antagonist; muscarinic antagonist; psychotropic drug; serotonergic antagonist
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
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
(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
clozapine Clozapine: A tricylic dibenzodiazepine, classified as an atypical antipsychotic agent. It binds several types of central nervous system receptors, and displays a unique pharmacological profile. Clozapine is a serotonin antagonist, with strong binding to 5-HT 2A/2C receptor subtype. It also displays strong affinity to several dopaminergic receptors, but shows only weak antagonism at the dopamine D2 receptor, a receptor commonly thought to modulate neuroleptic activity. Agranulocytosis is a major adverse effect associated with administration of this agent.. clozapine : A benzodiazepine that is 5H-dibenzo[b,e][1,4]diazepine substituted by a chloro group at position 8 and a 4-methylpiperazin-1-yl group at position 11. It is a second generation antipsychotic used in the treatment of psychiatric disorders like schizophrenia.	2.47	2	benzodiazepine; N-arylpiperazine; N-methylpiperazine; organochlorine compound	adrenergic antagonist; dopaminergic antagonist; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; environmental contaminant; GABA antagonist; histamine antagonist; muscarinic antagonist; second generation antipsychotic; serotonergic antagonist; xenobiotic
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
olanzapine Olanzapine: A benzodiazepine derivative that binds SEROTONIN RECEPTORS; MUSCARINIC RECEPTORS; HISTAMINE H1 RECEPTORS; ADRENERGIC ALPHA-1 RECEPTORS; and DOPAMINE RECEPTORS. It is an antipsychotic agent used in the treatment of SCHIZOPHRENIA; BIPOLAR DISORDER; and MAJOR DEPRESSIVE DISORDER; it may also reduce nausea and vomiting in patients undergoing chemotherapy.. olanzapine : A benzodiazepine that is 10H-thieno[2,3-b][1,5]benzodiazepine substituted by a methyl group at position 2 and a 4-methylpiperazin-1-yl group at position 4.	2.07	1	benzodiazepine; N-arylpiperazine; N-methylpiperazine	antiemetic; dopaminergic antagonist; histamine antagonist; muscarinic antagonist; second generation antipsychotic; serotonergic antagonist; serotonin uptake inhibitor
zaprinast zaprinast: anaphylaxis inhibitor; structure	3.51	1	triazolopyrimidines
sildenafil citrate Sildenafil Citrate: A PHOSPHODIESTERASE TYPE-5 INHIBITOR; VASODILATOR AGENT and UROLOGICAL AGENT that is used in the treatment of ERECTILE DYSFUNCTION and PRIMARY PULMONARY HYPERTENSION.. sildenafil citrate : The citrate salt of sildenafil.	2.21	1	citrate salt	EC 3.1.4.35 (3',5'-cyclic-GMP phosphodiesterase) inhibitor; vasodilator agent
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 [no description available]	3.51	1
bay 60-7550 [no description available]	3.51	1

Condition	Indicated	Relationship Strength	Studies
Dementia Praecox [description not available]	0	3	4
Schizophrenia A severe emotional disorder of psychotic depth characteristically marked by a retreat from reality with delusion formation, HALLUCINATIONS, emotional disharmony, and regressive behavior.	1	10	4
Pulmonary Hypertension [description not available]	0	2.21	1
Hypertension, Pulmonary Increased VASCULAR RESISTANCE in the PULMONARY CIRCULATION, usually secondary to HEART DISEASES or LUNG DISEASES.	0	2.21	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	3.33	1
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)	0	3.33	1

chemdatabank.com