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 SourceID
PubMed CID11581936
CHEMBL ID562318
SCHEMBL ID1414700
MeSH IDM0547755

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

ExcerptReferenceRelevance
"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

ExcerptRelevanceReference
" 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

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
PPM1D proteinHomo sapiens (human)Potency16.53880.00529.466132.9993AID1347411
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency0.84870.01237.983543.2770AID1645841
EWS/FLI fusion proteinHomo sapiens (human)Potency17.70230.001310.157742.8575AID1259252; AID1259253; AID1259255; AID1259256
GVesicular stomatitis virusPotency0.60080.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency7.56370.00108.379861.1304AID1645840
Interferon betaHomo sapiens (human)Potency12.55430.00339.158239.8107AID1347411; AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency0.60080.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency0.60080.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency0.60080.01238.964839.8107AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10ARattus norvegicus (Norway rat)IC50 (µMol)0.00040.00040.00040.0004AID977608
Chain A, cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10ARattus norvegicus (Norway rat)IC50 (µMol)0.00040.00040.00040.0004AID977608
Chain A, cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10ARattus norvegicus (Norway rat)IC50 (µMol)0.00040.00040.00040.0004AID977608
Chain A, cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10ARattus norvegicus (Norway rat)IC50 (µMol)0.00040.00040.00040.0004AID977608
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A Rattus norvegicus (Norway rat)IC50 (µMol)0.00040.00020.01340.0360AID1141259; AID1799159; AID428630; AID615724; AID628043; AID677554
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A Rattus norvegicus (Norway rat)Ki0.00020.00020.17830.4170AID677554
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)IC50 (µMol)0.00130.00001.49049.2000AID1140226; 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

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Galectin-3Homo sapiens (human)Kd0.22000.15000.22000.2900AID1724759; AID1724761
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
High affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)Activity0.00210.00210.00210.0021AID442317
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CHomo sapiens (human)Activity0.00210.00210.00210.0021AID442318
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (87)

Processvia Protein(s)Taxonomy
signal transductionHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
positive regulation of cardiac muscle hypertrophyHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
cGMP metabolic processHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
cGMP catabolic processHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
positive regulation of long-term synaptic potentiationHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
negative regulation of neural precursor cell proliferationHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
cAMP-mediated signalingHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA 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-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
positive regulation of dendritic cell differentiationGalectin-1Homo sapiens (human)
plasma cell differentiationGalectin-1Homo sapiens (human)
apoptotic processGalectin-1Homo sapiens (human)
T cell costimulationGalectin-1Homo sapiens (human)
regulation of apoptotic processGalectin-1Homo sapiens (human)
positive regulation of apoptotic processGalectin-1Homo sapiens (human)
positive regulation of canonical NF-kappaB signal transductionGalectin-1Homo sapiens (human)
myoblast differentiationGalectin-1Homo sapiens (human)
positive regulation of viral entry into host cellGalectin-1Homo sapiens (human)
positive regulation of inflammatory responseGalectin-1Homo sapiens (human)
cell-cell adhesionGalectin-1Homo sapiens (human)
positive regulation of dendritic cell differentiationGalectin-3Homo sapiens (human)
monocyte chemotaxisGalectin-3Homo sapiens (human)
mRNA processingGalectin-3Homo sapiens (human)
RNA splicingGalectin-3Homo sapiens (human)
neutrophil chemotaxisGalectin-3Homo sapiens (human)
epithelial cell differentiationGalectin-3Homo sapiens (human)
positive regulation of protein-containing complex assemblyGalectin-3Homo sapiens (human)
regulation of T cell proliferationGalectin-3Homo sapiens (human)
innate immune responseGalectin-3Homo sapiens (human)
negative regulation of endocytosisGalectin-3Homo sapiens (human)
eosinophil chemotaxisGalectin-3Homo sapiens (human)
macrophage chemotaxisGalectin-3Homo sapiens (human)
negative regulation of T cell receptor signaling pathwayGalectin-3Homo sapiens (human)
positive chemotaxisGalectin-3Homo sapiens (human)
regulation of T cell apoptotic processGalectin-3Homo sapiens (human)
mononuclear cell migrationGalectin-3Homo sapiens (human)
positive regulation of mononuclear cell migrationGalectin-3Homo sapiens (human)
positive regulation of calcium ion importGalectin-3Homo sapiens (human)
regulation of extrinsic apoptotic signaling pathway via death domain receptorsGalectin-3Homo sapiens (human)
positive regulation of protein localization to plasma membraneGalectin-3Homo sapiens (human)
negative regulation of protein tyrosine phosphatase activityGalectin-3Homo sapiens (human)
negative regulation of immunological synapse formationGalectin-3Homo sapiens (human)
negative regulation of T cell activation via T cell receptor contact with antigen bound to MHC molecule on antigen presenting cellGalectin-3Homo sapiens (human)
negative regulation of extrinsic apoptotic signaling pathwayGalectin-3Homo sapiens (human)
cAMP-mediated signalingCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CHomo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
cAMP catabolic processcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)
cGMP catabolic processcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)
negative regulation of cGMP-mediated signalingcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)
cAMP-mediated signalingcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (38)

Processvia Protein(s)Taxonomy
3',5'-cyclic-nucleotide phosphodiesterase activityHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
protein bindingHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
metal ion bindingHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activityHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activityHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
RNA bindingGalectin-1Homo sapiens (human)
protein bindingGalectin-1Homo sapiens (human)
laminin bindingGalectin-1Homo sapiens (human)
lactose bindingGalectin-1Homo sapiens (human)
RNA bindingGalectin-3Homo sapiens (human)
protein phosphatase inhibitor activityGalectin-3Homo sapiens (human)
protein bindingGalectin-3Homo sapiens (human)
IgE bindingGalectin-3Homo sapiens (human)
protein phosphatase bindingGalectin-3Homo sapiens (human)
carbohydrate bindingGalectin-3Homo sapiens (human)
chemoattractant activityGalectin-3Homo sapiens (human)
laminin bindingGalectin-3Homo sapiens (human)
molecular condensate scaffold activityGalectin-3Homo sapiens (human)
disaccharide bindingGalectin-3Homo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CHomo sapiens (human)
calmodulin-activated dual specificity 3',5'-cyclic-GMP, 3',5'-cyclic-AMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CHomo sapiens (human)
calmodulin bindingCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CHomo sapiens (human)
metal ion bindingCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CHomo sapiens (human)
calmodulin-activated 3',5'-cyclic-GMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CHomo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
3',5'-cyclic-nucleotide phosphodiesterase activitycAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)
cGMP-stimulated cyclic-nucleotide phosphodiesterase activitycAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)
cAMP bindingcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)
cGMP bindingcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)
metal ion bindingcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activitycAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activitycAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (35)

Processvia Protein(s)Taxonomy
nucleoplasmHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
endoplasmic reticulumHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
Golgi apparatusHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
cytosolHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
plasma membraneHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
ruffle membraneHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
sarcolemmaHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
perikaryonHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
perinuclear region of cytoplasmHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
collagen-containing extracellular matrixGalectin-1Homo sapiens (human)
extracellular regionGalectin-1Homo sapiens (human)
extracellular spaceGalectin-1Homo sapiens (human)
cytoplasmGalectin-1Homo sapiens (human)
endoplasmic reticulum lumenGalectin-1Homo sapiens (human)
cytosolGalectin-1Homo sapiens (human)
collagen-containing extracellular matrixGalectin-1Homo sapiens (human)
extracellular exosomeGalectin-1Homo sapiens (human)
galectin complexGalectin-1Homo sapiens (human)
extracellular spaceGalectin-1Homo sapiens (human)
collagen-containing extracellular matrixGalectin-3Homo sapiens (human)
immunological synapseGalectin-3Homo sapiens (human)
extracellular regionGalectin-3Homo sapiens (human)
extracellular spaceGalectin-3Homo sapiens (human)
nucleusGalectin-3Homo sapiens (human)
nucleoplasmGalectin-3Homo sapiens (human)
cytoplasmGalectin-3Homo sapiens (human)
mitochondrial inner membraneGalectin-3Homo sapiens (human)
cytosolGalectin-3Homo sapiens (human)
plasma membraneGalectin-3Homo sapiens (human)
cell surfaceGalectin-3Homo sapiens (human)
membraneGalectin-3Homo sapiens (human)
secretory granule membraneGalectin-3Homo sapiens (human)
collagen-containing extracellular matrixGalectin-3Homo sapiens (human)
extracellular exosomeGalectin-3Homo sapiens (human)
ficolin-1-rich granule membraneGalectin-3Homo sapiens (human)
spliceosomal complexGalectin-3Homo sapiens (human)
cytoplasmGalectin-3Homo sapiens (human)
immunological synapseGalectin-3Homo sapiens (human)
nucleusGalectin-3Homo sapiens (human)
extracellular spaceGalectin-3Homo sapiens (human)
lysosomeCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CHomo sapiens (human)
cytosolCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CHomo sapiens (human)
neuronal cell bodyCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CHomo sapiens (human)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (132)

Assay IDTitleYearJournalArticle
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347081qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Confirmatory Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347084qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Confirmatory Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings 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.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347088qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): Viability assay - Alamar blue signal for LCMV Confirmatory Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347087qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Confirmatory Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1190578Binding affinity to PDE10A (unknown origin)2015Bioorganic & medicinal chemistry letters, Feb-15, Volume: 25, Issue:4
Synthesis and in vitro characterization of cinnoline and benzimidazole analogues as phosphodiesterase 10A inhibitors.
AID715546Selectivity ratio of Ki for human PDE11A to Ki for human PDE10A2012Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18
Discovery of tetrahydropyridopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia.
AID1724759Binding affinity to recombinant human galectin 3 assessed as dissociation constant by fluorescent anisotropy assay2020ACS medicinal chemistry letters, Sep-10, Volume: 11, Issue:9
Quinoline-Pyrazole Scaffold as a Novel Ligand of Galectin-3 and Suppressor of TREM2 Signaling.
AID442318Binding affinity to PDE1C2009Journal 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.
AID428644Volume of distribution at steady state in Beagle dog at 0.3 mg/kg, iv2009Journal 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.
AID767808Intrinsic clearance in human liver microsomes2013Bioorganic & medicinal chemistry, Oct-01, Volume: 21, Issue:19
N-Methylanilide and N-methylbenzamide derivatives as phosphodiesterase 10A (PDE10A) inhibitors.
AID677554Displacement of [3H]5-(6,7-dimethoxycinnolin-4-yl)-N-isopropyl-3-methylpyridin-2-amine from PDE10A in Sprague-Dawley rat striatum2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Rapid identification of a novel small molecule phosphodiesterase 10A (PDE10A) tracer.
AID705195Selectivity ratio of IC50 for PDE4 to IC50 for PDE10A2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Current landscape of phosphodiesterase 10A (PDE10A) inhibition.
AID1724766Antiinflammatory 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 control2020ACS medicinal chemistry letters, Sep-10, Volume: 11, Issue:9
Quinoline-Pyrazole Scaffold as a Novel Ligand of Galectin-3 and Suppressor of TREM2 Signaling.
AID1724762Antiinflammatory activity in mouse BV-2 cells assessed as reduction in Abeta-induced TNFalpha release incubated for 12 hrs by ELISA2020ACS medicinal chemistry letters, Sep-10, Volume: 11, Issue:9
Quinoline-Pyrazole Scaffold as a Novel Ligand of Galectin-3 and Suppressor of TREM2 Signaling.
AID715549Selectivity ratio of Ki for human PDE7A to Ki for human PDE10A2012Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18
Discovery of tetrahydropyridopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia.
AID615724Inhibition of rat PDE10A2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and in vitro evaluation of new analogues as inhibitors for phosphodiesterase 10A.
AID428642Hepatic clearance in cynomolgus monkey at 0.03 mg/kg, iv2009Journal 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.
AID1235025Inhibition of PDE10A (unknown origin)2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
BN/CC isosterism in borazaronaphthalenes towards phosphodiesterase 10A (PDE10A) inhibitors.
AID428650Half life in cynomolgus monkey at 0.03 mg/kg, iv2009Journal 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.
AID428654Behavioral effect in mouse assessed as conditioned avoidance response at 115 nM plasma exposure2009Journal 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.
AID1724764Antiinflammatory activity in mouse BV-2 cells assessed as reduction in Abeta-induced IL-8 release incubated for 12 hrs by ELISA2020ACS medicinal chemistry letters, Sep-10, Volume: 11, Issue:9
Quinoline-Pyrazole Scaffold as a Novel Ligand of Galectin-3 and Suppressor of TREM2 Signaling.
AID705190Selectivity ratio of IC50 for PDE9 to IC50 for PDE10A2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Current landscape of phosphodiesterase 10A (PDE10A) inhibition.
AID442317Binding affinity to PDE9A2009Journal 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.
AID428628Increase in cGMP level in sc dosed mouse striatum2009Journal 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.
AID1724765Antiinflammatory 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 control2020ACS medicinal chemistry letters, Sep-10, Volume: 11, Issue:9
Quinoline-Pyrazole Scaffold as a Novel Ligand of Galectin-3 and Suppressor of TREM2 Signaling.
AID705199Inhibition of PDE10A2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Current landscape of phosphodiesterase 10A (PDE10A) inhibition.
AID715547Selectivity ratio of Ki for human PDE9A to Ki for human PDE10A2012Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18
Discovery of tetrahydropyridopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia.
AID428648Half life in Beagle dog at 0.3 mg/kg, iv2009Journal 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.
AID1141266Ex vivo PDE10A receptor occupancy in po dosed Wistar rat striatum assessed as inhibition of [3H]-MP10 binding after 1 hr by autoradiography2014Journal 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.
AID767804Antipsychotic activity in rat assessed as inhibition of amphetamine-stimulated locomotor activity2013Bioorganic & medicinal chemistry, Oct-01, Volume: 21, Issue:19
N-Methylanilide and N-methylbenzamide derivatives as phosphodiesterase 10A (PDE10A) inhibitors.
AID628043Inhibition of rat recombinant PDE10A expressed in baculovirus infected insect Sf9 cells using [3H]cAMP as substrate after 60 mins by scintillation counting2011Journal 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.
AID767807Intrinsic clearance in rat liver microsomes2013Bioorganic & medicinal chemistry, Oct-01, Volume: 21, Issue:19
N-Methylanilide and N-methylbenzamide derivatives as phosphodiesterase 10A (PDE10A) inhibitors.
AID1557548Inhibition 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 analysis2019Journal 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.
AID428637Metabolic stability in human liver microsome assessed as intrinsic clearance2009Journal 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.
AID615725Selectivity ratio of IC50 for rat PDE10A to IC50 for rat PDE3B2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and in vitro evaluation of new analogues as inhibitors for phosphodiesterase 10A.
AID428645Volume of distribution at steady state in cynomolgus monkey at 0.03 mg/kg, iv2009Journal 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.
AID428630Inhibition of rat recombinant PDE10A transfected in Sf9 cells2009Journal 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.
AID715550Selectivity ratio of Ki for human PDE6A to Ki for human PDE10A2012Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18
Discovery of tetrahydropyridopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia.
AID1724761Binding affinity to recombinant human galectin 3 assessed as dissociation constant by SPR assay2020ACS medicinal chemistry letters, Sep-10, Volume: 11, Issue:9
Quinoline-Pyrazole Scaffold as a Novel Ligand of Galectin-3 and Suppressor of TREM2 Signaling.
AID1140351Inhibition of N-terminal GST-tagged human recombinant PDE10A assessed as substrate hydrolysis using [3H]cAMP as substrate after 30 mins by two-step radiometric assay2014Bioorganic & medicinal chemistry letters, May-01, Volume: 24, Issue:9
Design, synthesis and pharmacological evaluation of novel polycyclic heteroarene ethers as PDE10A inhibitors: Part I.
AID428636Efflux ratio of permeability from basolateral to apical side over apical to basolateral side in MDR1 overexpressing MDCK cells2009Journal 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.
AID715555Selectivity ratio of Ki for human PDE1A to Ki for human PDE10A2012Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18
Discovery of tetrahydropyridopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia.
AID428634Behavioral effect in sc dosed mouse assessed as conditioned avoidance response after 30 mins2009Journal 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.
AID428656Behavioral effect in sc dosed PDE10A knockout mouse assessed as conditioned avoidance response after 30 mins2009Journal 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.
AID705189Selectivity ratio of IC50 for PDE11 to IC50 for PDE10A2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Current landscape of phosphodiesterase 10A (PDE10A) inhibition.
AID428638Increase in cGMP level in mouse striatum at 1 mg/kg, sc relative to control2009Journal 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.
AID428653Oral bioavailability in cynomolgus monkey rat at 3 mg/kg, po2009Journal 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.
AID428629Half life in Beagle dog at 3 mg/kg, po2009Journal 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.
AID767814Inhibition of PDE10A (unknown origin)2013Bioorganic & medicinal chemistry, Oct-01, Volume: 21, Issue:19
N-Methylanilide and N-methylbenzamide derivatives as phosphodiesterase 10A (PDE10A) inhibitors.
AID428643Volume of distribution at steady state in Sprague-Dawley rat at 0.1 mg/kg, iv2009Journal 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.
AID1557506Inhibition 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 analysis2019Journal 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.
AID1872562Inhibition of PDE10 (unknown origin)2022European journal of medicinal chemistry, Mar-15, Volume: 232Therapeutic potential of phosphodiesterase inhibitors for cognitive amelioration in Alzheimer's disease.
AID1724767Inhibition 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 assay2020ACS medicinal chemistry letters, Sep-10, Volume: 11, Issue:9
Quinoline-Pyrazole Scaffold as a Novel Ligand of Galectin-3 and Suppressor of TREM2 Signaling.
AID705193Selectivity ratio of IC50 for PDE5 to IC50 for PDE10A2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Current landscape of phosphodiesterase 10A (PDE10A) inhibition.
AID1141264Antipsychotic 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 injection2014Journal 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.
AID715552Selectivity ratio of Ki for human PDE4A to Ki for human PDE10A2012Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18
Discovery of tetrahydropyridopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia.
AID715551Selectivity ratio of Ki for human PDE5A to Ki for human PDE10A2012Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18
Discovery of tetrahydropyridopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia.
AID428649Half life in Beagle dog at 0.1 mg/kg, po2009Journal 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.
AID428655Unbound fraction in mouse plasma2009Journal 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.
AID1557569Inhibition 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 analysis2019Journal 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.
AID428652Oral bioavailability in Beagle dog at 0.1 mg/kg, po2009Journal 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.
AID715548Selectivity ratio of Ki for human PDE8A to Ki for human PDE10A2012Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18
Discovery of tetrahydropyridopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia.
AID428640Hepatic clearance in Sprague-Dawley rat at 0.1 mg/kg, iv2009Journal 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.
AID705196Selectivity ratio of IC50 for PDE2 to IC50 for PDE10A2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Current landscape of phosphodiesterase 10A (PDE10A) inhibition.
AID1724760Binding affinity to recombinant human galectin 1 assessed as dissociation constant by fluorescent anisotropy assay2020ACS medicinal chemistry letters, Sep-10, Volume: 11, Issue:9
Quinoline-Pyrazole Scaffold as a Novel Ligand of Galectin-3 and Suppressor of TREM2 Signaling.
AID1141267Plasma protein binding in Sprague-Dawley rat at 5 uM after 4.5 hrs2014Journal 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.
AID1724758Inhibition of recombinant human galectin-3/recombinant human TREM2 interaction assessed as reduction in TR-FRET signal incubated for 3 hrs by TR-FRET assay2020ACS medicinal chemistry letters, Sep-10, Volume: 11, Issue:9
Quinoline-Pyrazole Scaffold as a Novel Ligand of Galectin-3 and Suppressor of TREM2 Signaling.
AID1181667Antipsychotic 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 inj2014Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15
Design, synthesis and pharmacological evaluation of novel polycyclic heteroarene ethers as PDE10A inhibitors: part II.
AID705197Selectivity ratio of IC50 for PDE3 to IC50 for PDE10A2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Current landscape of phosphodiesterase 10A (PDE10A) inhibition.
AID1140226Inhibition of full-length human recombinant PDE10A using cyclic AMP as substrate by scintillation proximity assay2014Bioorganic & 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.
AID715554Selectivity ratio of Ki for human PDE2A to Ki for human PDE10A2012Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18
Discovery of tetrahydropyridopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia.
AID1141268Protein binding in Sprague-Dawley rat brain at 5 uM after 5 hrs2014Journal 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.
AID1181668Antipsychotic 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 injecti2014Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15
Design, synthesis and pharmacological evaluation of novel polycyclic heteroarene ethers as PDE10A inhibitors: part II.
AID428647Half life in Sprague-Dawley rat at 1 mg/kg, po2009Journal 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.
AID428639Increase in cGMP level in mouse striatum at 3.2 mg/kg, sc relative to control2009Journal 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.
AID1181666Antipsychotic 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 inj2014Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15
Design, synthesis and pharmacological evaluation of novel polycyclic heteroarene ethers as PDE10A inhibitors: part II.
AID1181683Antipsychotic 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 control2014Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15
Design, synthesis and pharmacological evaluation of novel polycyclic heteroarene ethers as PDE10A inhibitors: part II.
AID428646Half life in Sprague-Dawley rat at 0.1 mg/kg, iv2009Journal 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.
AID428641Hepatic clearance in Beagle dog at 0.3 mg/kg, iv2009Journal 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.
AID1557570Inhibition 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 analysis2019Journal 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.
AID598564Inhibition of PDE10A2011Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
Triazoloquinazolines as a novel class of phosphodiesterase 10A (PDE10A) inhibitors.
AID705191Selectivity ratio of IC50 for PDE8 to IC50 for PDE10A2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Current landscape of phosphodiesterase 10A (PDE10A) inhibition.
AID715553Selectivity ratio of Ki for human PDE3A to Ki for human PDE10A2012Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18
Discovery of tetrahydropyridopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia.
AID1141258Antipsychotic activity in sc dosed Wiga rat assessed as reversal of phencyclidine-induced hyperlocomotion administered 60 mins prior to PCP challenge measured for 30 mins2014Journal 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.
AID1235026Intrinsic clearance in rat liver microsomes2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
BN/CC isosterism in borazaronaphthalenes towards phosphodiesterase 10A (PDE10A) inhibitors.
AID615722Selectivity ratio of IC50 for rat PDE10A to IC50 for rat PDE3A2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and in vitro evaluation of new analogues as inhibitors for phosphodiesterase 10A.
AID1267480Aqueous solubility of the compound at pH 72016Bioorganic & medicinal chemistry letters, Jan-01, Volume: 26, Issue:1
Discovery of pyrazolopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia.
AID705194Selectivity ratio of IC50 for PDE6 to IC50 for PDE10A2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Current landscape of phosphodiesterase 10A (PDE10A) inhibition.
AID1724763Antiinflammatory activity in mouse BV-2 cells assessed as reduction in Abeta-induced IL-12 release incubated for 12 hrs by ELISA2020ACS medicinal chemistry letters, Sep-10, Volume: 11, Issue:9
Quinoline-Pyrazole Scaffold as a Novel Ligand of Galectin-3 and Suppressor of TREM2 Signaling.
AID484805Inhibition of human recombinant PDE10A expressed in baculovirus-SF21 cell system assessed as hydrolysis of [3H]cAMP after 1 hr by liquid scintillation counting2010Journal 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.
AID1141259Inhibition of rat recombinant PDE10A expressed in baculovirus infected Sf9 cells using [3H]cAMP as substrate after 60 mins by TopCount scintillation counting analysis2014Journal 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.
AID705192Selectivity ratio of IC50 for PDE7 to IC50 for PDE10A2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Current landscape of phosphodiesterase 10A (PDE10A) inhibition.
AID1724757Inhibition 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 control2020ACS medicinal chemistry letters, Sep-10, Volume: 11, Issue:9
Quinoline-Pyrazole Scaffold as a Novel Ligand of Galectin-3 and Suppressor of TREM2 Signaling.
AID1557547Inhibition 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 analysis2019Journal 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.
AID428651Oral bioavailability in Sprague-Dawley rat at 1 mg/kg, po2009Journal 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.
AID615723Lipophilicity, log D of the compound2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and in vitro evaluation of new analogues as inhibitors for phosphodiesterase 10A.
AID705198Selectivity ratio of IC50 for PDE1 to IC50 for PDE10A2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Current landscape of phosphodiesterase 10A (PDE10A) inhibition.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347411qHTS 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) Libary2020ACS 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.
AID1345255Human phosphodiesterase 10A (Phosphodiesterases, 3',5'-cyclic nucleotide (PDEs))2009Journal 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.
AID1799159PDE 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 t2009Journal 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.
AID977608Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB2009Journal 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)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's2 (7.14)29.6817
2010's18 (64.29)24.3611
2020's8 (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.

MetricThis Compound (vs All)
Research Demand Index17.29 (24.57)
Research Supply Index3.37 (2.92)
Research Growth Index5.48 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (17.29)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (3.57%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other27 (96.43%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]