Page last updated: 2024-10-15

bay 60-7550

Cross-References

ID SourceID
PubMed CID135564787
CHEMBL ID370962
SCHEMBL ID2232786
SCHEMBL ID18380627
SCHEMBL ID19205847
MeSH IDM0579878

Synonyms (34)

Synonym
HY-14992
2-(3,4-dimethoxy-benzyl)-7-[(r)-1-((r)-1-hydroxy-ethyl)-4-phenyl-butyl]-5-methyl-3h-imidazo[5,1-f][1,2,4]triazin-4-one
bdbm50166893
CHEMBL370962 ,
bay-60-7550
2-(3,4-dimethoxybenzyl)-7-[(2r,3r)-2-hydroxy-6-phenylhexan-3-yl]-5-methylimidazo[5,1-f][1,2,4]triazin-4(3h)-one
19F ,
bay60-7550
bay 60-7550
439083-90-6
2-[(3,4-dimethoxyphenyl)methyl]-7-[(1r)-1-[(1r)-1-hydroxyethyl]-4-phenylbutyl]-5-methyl-imidazo[5,1-f][1,2,4]triazin-4(1h)-one
4HTX
CS-0279
gtpl5147
2-[(3,4-dimethoxyphenyl)methyl]-7-[(2r,3r)-2-hydroxy-6-phenylhexan-3-yl]-5-methyl-1h-imidazo[5,1-f][1,2,4]triazin-4-one
bay607550
zrn7lzk9tq ,
bay-607550
imidazo(5,1-f)(1,2,4)triazin-4(1h)-one, 2-((3,4-dimethoxyphenyl)methyl)-7-((1r)-1-((1r)-1-hydroxyethyl)-4-phenylbutyl)-5-methyl-
unii-zrn7lzk9tq
2-(3,4-dimethoxybenzyl)-7-((2r,3r)-2-hydroxy-6-phenylhexan-3-yl)-5-methylimidazo[5,1-f][1,2,4]triazin-4(3h)-one
SCHEMBL2232786
DTXSID50649549
2-[(3,4-dimethoxyphenyl)methyl]-7-[(2r,3r)-2-hydroxy-6-phenylhexan-3-yl]-5-methylimidazo[5,1-f][1,2,4]triazin-4(1h)-one
SCHEMBL18380627
AKOS027323749
SCHEMBL19205847
2-(3,4-dimethoxybenzyl)-7-((2r,3r)-2-hydroxy-6-phenylhexan-3-yl)-5-methylimidazo[1,5-f][1,2,4]triazin-4(3h)-one
BCP14349
Q15634074
C90482
MS-28842
2-[(3,4-dimethoxyphenyl)methyl]-7-[(2r,3r)-2-hydroxy-6-phenylhexan-3-yl]-5-methyl-3h-imidazo[5,1-f][1,2,4]triazin-4-one
Z3244812827
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)IC50 (µMol)0.00320.00001.77679.2000AID1440951; AID1449241; AID1449315; AID1458534; AID1458938; AID1480122; AID1574952; AID1574977; AID1625364; AID240759
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (25)

Processvia Protein(s)Taxonomy
heart valve developmentcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
ventricular septum developmentcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
aorta developmentcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwaycGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
regulation of cGMP-mediated signalingcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cAMP-mediated signalingcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cGMP-mediated signalingcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cellular response to macrophage colony-stimulating factor stimuluscGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
negative regulation of vascular permeabilitycGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
positive regulation of vascular permeabilitycGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
regulation of cAMP-mediated signalingcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cGMP catabolic processcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
positive regulation of inflammatory responsecGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
establishment of endothelial barriercGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cellular response to mechanical stimuluscGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cellular response to cAMPcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cellular response to cGMPcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cellular response to transforming growth factor beta stimuluscGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
negative regulation of adenylate cyclase-activating G protein-coupled receptor signaling pathwaycGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cellular response to 2,3,7,8-tetrachlorodibenzodioxinecGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
positive regulation of gene expressioncGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
negative regulation of cGMP-mediated signalingcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
negative regulation of cAMP-mediated signalingcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
regulation of mitochondrion organizationcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (11)

Processvia Protein(s)Taxonomy
magnesium ion bindingcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activitycGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cGMP-stimulated cyclic-nucleotide phosphodiesterase activitycGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
protein bindingcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
zinc ion bindingcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cAMP bindingcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cGMP bindingcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
TPR domain bindingcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
phosphate ion bindingcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
protein homodimerization activitycGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activitycGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (12)

Processvia Protein(s)Taxonomy
plasma membranecGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
nucleuscGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cytoplasmcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
mitochondrial outer membranecGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
mitochondrial inner membranecGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
endoplasmic reticulumcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
Golgi apparatuscGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cytosolcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
plasma membranecGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
presynaptic membranecGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
perinuclear region of cytoplasmcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
nucleuscGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
mitochondrial inner membranecGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
perinuclear region of cytoplasmcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
mitochondrial outer membranecGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
synaptic membranecGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cytosolcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
mitochondrial matrixcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (70)

Assay IDTitleYearJournalArticle
AID1440951Inhibition of PDE2a (unknown origin) using cAMP as substrate after 30 mins by Scintillation proximity assay2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Design and Synthesis of Novel and Selective Phosphodiesterase 2 (PDE2a) Inhibitors for the Treatment of Memory Disorders.
AID1449249Selectivity ratio of IC50 for PDE9A1 (unknown origin) to IC50 for full length recombinant human FLAG-tagged PDE2A3 expressed in sf21 cells2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor.
AID1625364Inhibition of human His-tagged PDE2A catalytic domain (578 to 919 residues) expressed in Escherichia coli BL21-CodonPlus(DE3) cells using cGMP as substrate by HTRF assay2016Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15
PDEStrIAn: A Phosphodiesterase Structure and Ligand Interaction Annotated Database As a Tool for Structure-Based Drug Design.
AID1058015Selectivity ratio of IC50 for PDE (unknown origin) to IC50 for porcine/bovine heart myocardium PDE22013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
PDE2 inhibition: potential for the treatment of cognitive disorders.
AID1449242Selectivity ratio of IC50 for PDE1B1 (unknown origin) to IC50 for full length recombinant human FLAG-tagged PDE2A3 expressed in sf21 cells2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor.
AID1449247Selectivity ratio of IC50 for PDE7B (unknown origin) to IC50 for full length recombinant human FLAG-tagged PDE2A3 expressed in sf21 cells2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor.
AID1330516Inhibition of PDE1 (unknown origin)2017ACS medicinal chemistry letters, Jan-12, Volume: 8, Issue:1
Potential Treatment of Cognitive Impairment in Schizophrenia by Phosphodiesterase 2 (PDE2) Inhibitors.
AID1058017Inhibition of pig/bovine heart myocardium PDE2 after 15 mins by scintillation proximity assay in presence of [3H]-cAMP2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
PDE2 inhibition: potential for the treatment of cognitive disorders.
AID1480123Intrinsic clearance in human hepatocytes assessed per million cells at 1 uM after 0.5 to 4 hrs by HPLC-HRMS method2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Lead Diversification at the Nanomole Scale Using Liver Microsomes and Quantitative Nuclear Magnetic Resonance Spectroscopy: Application to Phosphodiesterase 2 Inhibitors.
AID1458938Inhibition of PDE2A (unknown origin) using [3H]cGMP as substrate after 30 mins by scintillation proximity assay2017Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18
Discovery of Clinical Candidate N-((1S)-1-(3-Fluoro-4-(trifluoromethoxy)phenyl)-2-methoxyethyl)-7-methoxy-2-oxo-2,3-dihydropyrido[2,3-b]pyrazine-4(1H)-carboxamide (TAK-915): A Highly Potent, Selective, and Brain-Penetrating Phosphodiesterase 2A Inhibitor
AID1480155Drug level in dog liver microsomes treated with 2-(3,4-dimethoxybenzyl)-7-((2R,3R)-2-hydroxy-6-phenylhexan-3-yl)-5-methylimidazo[1,5-f][1,2,4]triazin-4(3H)-one at 20 uM after 1 hr by UHPLC-UV-HRMS method2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Lead Diversification at the Nanomole Scale Using Liver Microsomes and Quantitative Nuclear Magnetic Resonance Spectroscopy: Application to Phosphodiesterase 2 Inhibitors.
AID1596293Inhibition of recombinant N-terminal-GST-Th-tagged full length human PDE2A1 expressed in Sf9 cells using FAM-cAMP as substrate at 1xIC50 incubated for 60 mins by fluorescence plate reader analysis2019European journal of medicinal chemistry, Jul-15, Volume: 174InCl
AID1574966Inhibition of PDE2 in mouse HT22 cells assessed as suppression of corticosterone-induced decrease in cAMP level at 1 uM after 24 hrs by ELISA2019Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3
Design, synthesis of novel purin-6-one derivatives as phosphodiesterase 2 (PDE2) inhibitors: The neuroprotective and anxiolytic-like effects.
AID1458534Inhibition of PDE2A (unknown origin)2017Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18
Discovery of an Orally Bioavailable, Brain-Penetrating, in Vivo Active Phosphodiesterase 2A Inhibitor Lead Series for the Treatment of Cognitive Disorders.
AID1872559Drug concentration in brain of Wistar rat at 10 mg/kg, po measured after 240 mins2022European journal of medicinal chemistry, Mar-15, Volume: 232Therapeutic potential of phosphodiesterase inhibitors for cognitive amelioration in Alzheimer's disease.
AID1596270Inhibition of recombinant N-terminal-GST-Th-tagged full length human PDE2A1 expressed in Sf9 cells using FAM-cAMP as substrate at 0.1xIC50 incubated for 60 mins by fluorescence plate reader analysis2019European journal of medicinal chemistry, Jul-15, Volume: 174InCl
AID1480153Drug metabolism in dog liver microsomes assessed as 7-((2R,3R)-2,6-Dihydroxy-6-phenylhexan-3-yl)-2-(3,4-dimethoxybenzyl)-5-methylimidazo[5,1-f][1,2,4]triazin-4(3H)-one diastereomer 2 formation at 20 uM after 1 hr by UHPLC-UV-HRMS method2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Lead Diversification at the Nanomole Scale Using Liver Microsomes and Quantitative Nuclear Magnetic Resonance Spectroscopy: Application to Phosphodiesterase 2 Inhibitors.
AID1449251Selectivity ratio of IC50 for PDE11A4 (unknown origin) to IC50 for full length recombinant human FLAG-tagged PDE2A3 expressed in sf21 cells2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor.
AID1330524Inhibition of PDE9A (unknown origin)2017ACS medicinal chemistry letters, Jan-12, Volume: 8, Issue:1
Potential Treatment of Cognitive Impairment in Schizophrenia by Phosphodiesterase 2 (PDE2) Inhibitors.
AID1458537Selectivity ratio of IC50 for PDE1C (unknown origin) to IC50 for PDE2A (unknown origin)2017Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18
Discovery of an Orally Bioavailable, Brain-Penetrating, in Vivo Active Phosphodiesterase 2A Inhibitor Lead Series for the Treatment of Cognitive Disorders.
AID1449248Selectivity ratio of IC50 for PDE8B (unknown origin) to IC50 for full length recombinant human FLAG-tagged PDE2A3 expressed in sf21 cells2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor.
AID1449244Selectivity ratio of IC50 for PDE4D3 (unknown origin) to IC50 for full length recombinant human FLAG-tagged PDE2A3 expressed in sf21 cells2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor.
AID240759Inhibition of human phosphodiesterase 22005Journal of medicinal chemistry, May-19, Volume: 48, Issue:10
The next generation of phosphodiesterase inhibitors: structural clues to ligand and substrate selectivity of phosphodiesterases.
AID1596290Inhibition of recombinant N-terminal GST tagged full length human PDE1B expressed in Sf9 cells using FAM-cAMP as substrate at 1xIC50 incubated for 60 mins by fluorescence plate reader analysis2019European journal of medicinal chemistry, Jul-15, Volume: 174InCl
AID1480122Inhibition of human PDE2A1 using 3',5'-[3H]cGMP as substrate after 30 mins by scintillation proximity assay2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Lead Diversification at the Nanomole Scale Using Liver Microsomes and Quantitative Nuclear Magnetic Resonance Spectroscopy: Application to Phosphodiesterase 2 Inhibitors.
AID1449250Selectivity ratio of IC50 for PDE10A1 (unknown origin) to IC50 for full length recombinant human FLAG-tagged PDE2A3 expressed in sf21 cells2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor.
AID1330525Inhibition of PDE10A (unknown origin)2017ACS medicinal chemistry letters, Jan-12, Volume: 8, Issue:1
Potential Treatment of Cognitive Impairment in Schizophrenia by Phosphodiesterase 2 (PDE2) Inhibitors.
AID1368377Inhibition of PDE2 (unknown origin)2018Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1
Discovery of novel purine nucleoside derivatives as phosphodiesterase 2 (PDE2) inhibitors: Structure-based virtual screening, optimization and biological evaluation.
AID1330521Inhibition of PDE5 (unknown origin)2017ACS medicinal chemistry letters, Jan-12, Volume: 8, Issue:1
Potential Treatment of Cognitive Impairment in Schizophrenia by Phosphodiesterase 2 (PDE2) Inhibitors.
AID1449243Selectivity ratio of IC50 for PDE3A1 (unknown origin) to IC50 for full length recombinant human FLAG-tagged PDE2A3 expressed in sf21 cells2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor.
AID1330526Inhibition of PDE11A (unknown origin)2017ACS medicinal chemistry letters, Jan-12, Volume: 8, Issue:1
Potential Treatment of Cognitive Impairment in Schizophrenia by Phosphodiesterase 2 (PDE2) Inhibitors.
AID1449315Inhibition of PDE2A (unknown origin)2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor.
AID1480154Drug metabolism in dog liver microsomes assessed as 2-(3,4-Dimethoxybenzyl)-7-((2R,3R)-2-hydroxy-6-oxo-6-phenylhexan-3-yl)-5-methylimidazo[5,1-f ][1,2,4]triazin-4(3H)-one formation at 20 uM after 1 hr by UHPLC-UV-HRMS method2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Lead Diversification at the Nanomole Scale Using Liver Microsomes and Quantitative Nuclear Magnetic Resonance Spectroscopy: Application to Phosphodiesterase 2 Inhibitors.
AID1574969Anxiolytic activity in ICR mouse model of chronic stress-induced cognitive impairment assessed as increase in time spent in open arms at 0.5 mg/kg, ip measured for 5 mins test period by elevated plus maze test2019Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3
Design, synthesis of novel purin-6-one derivatives as phosphodiesterase 2 (PDE2) inhibitors: The neuroprotective and anxiolytic-like effects.
AID1480152Drug metabolism in dog liver microsomes assessed as 7-((2R,3R)-2,6-Dihydroxy-6-phenylhexan-3-yl)-2-(3,4-dimethoxybenzyl)-5-methylimidazo[5,1-f][1,2,4]triazin-4(3H)-one diastereomer 1 formation at 20 uM after 1 hr by UHPLC-UV-HRMS method2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Lead Diversification at the Nanomole Scale Using Liver Microsomes and Quantitative Nuclear Magnetic Resonance Spectroscopy: Application to Phosphodiesterase 2 Inhibitors.
AID1574965Inhibition of PDE2 in mouse HT22 cells assessed as suppression of corticosterone-induced decrease in cGMP level at 1 uM after 24 hrs by ELISA2019Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3
Design, synthesis of novel purin-6-one derivatives as phosphodiesterase 2 (PDE2) inhibitors: The neuroprotective and anxiolytic-like effects.
AID1480151Drug metabolism in dog liver microsomes assessed as 7-((2R,3R)-2,6-Dihydroxy-6-phenylhexan-3-yl)-2-(4-hydroxy-3-methoxybenzyl)-5-methylimidazo[5,1-f][1,2,4]triazin-4(3H)-one formation at 20 uM after 1 hr by UHPLC-UV-HRMS method2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Lead Diversification at the Nanomole Scale Using Liver Microsomes and Quantitative Nuclear Magnetic Resonance Spectroscopy: Application to Phosphodiesterase 2 Inhibitors.
AID1596267Inhibition of recombinant N-terminal GST-tagged full-length human PDE1A1 expressed in Sf9 cells using FAM-cAMP as substrate at 0.1xIC50 incubated for 60 mins by fluorescence plate reader analysis2019European journal of medicinal chemistry, Jul-15, Volume: 174InCl
AID1058016Selectivity ratio of IC50 for porcine/bovine PDE1C to IC50 for porcine/bovine heart myocardium PDE22013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
PDE2 inhibition: potential for the treatment of cognitive disorders.
AID1330518Inhibition of human PDE2 using FAM-labeled cAMP as substrate after 60 mins in presence of cGMP by florescence polarization assay2017ACS medicinal chemistry letters, Jan-12, Volume: 8, Issue:1
Potential Treatment of Cognitive Impairment in Schizophrenia by Phosphodiesterase 2 (PDE2) Inhibitors.
AID1480149Drug metabolism in dog liver microsomes assessed as 2-(3,4-Dimethoxybenzyl)-5-methyl-7-((2R,3R)-2,5,6-trihydroxy-6-phenylhexan-3-yl)imidazo[5,1-f ][1,2,4]triazin-4(3H)-one formation at 20 uM after 1 hr by UHPLC-UV-HRMS method2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Lead Diversification at the Nanomole Scale Using Liver Microsomes and Quantitative Nuclear Magnetic Resonance Spectroscopy: Application to Phosphodiesterase 2 Inhibitors.
AID1596291Inhibition of recombinant N-terminal GST tagged human PDE1C (2 to 634 aa) expressed in Sf9 cells at 1xIC50 using FAM-cAMP as substrate incubated for 60 mins by fluorescence plate reader analysis2019European journal of medicinal chemistry, Jul-15, Volume: 174InCl
AID1164384Plasma concentration in rat at 10 mg/kg, po after 30 mins2014ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9
Structure-Based Design of a Potent, Selective, and Brain Penetrating PDE2 Inhibitor with Demonstrated Target Engagement.
AID1458939Selectivity ratio of IC50 for pig arota PDE1C to IC50 for PDE2A (unknown origin)2017Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18
Discovery of Clinical Candidate N-((1S)-1-(3-Fluoro-4-(trifluoromethoxy)phenyl)-2-methoxyethyl)-7-methoxy-2-oxo-2,3-dihydropyrido[2,3-b]pyrazine-4(1H)-carboxamide (TAK-915): A Highly Potent, Selective, and Brain-Penetrating Phosphodiesterase 2A Inhibitor
AID1330520Inhibition of PDE4B (unknown origin)2017ACS medicinal chemistry letters, Jan-12, Volume: 8, Issue:1
Potential Treatment of Cognitive Impairment in Schizophrenia by Phosphodiesterase 2 (PDE2) Inhibitors.
AID1164385Drug level in rat brain at 10 mg/kg, po after 30 mins2014ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9
Structure-Based Design of a Potent, Selective, and Brain Penetrating PDE2 Inhibitor with Demonstrated Target Engagement.
AID1480150Drug metabolism in dog liver microsomes assessed as 7-((2R,3R)-2,6-Dihydroxy-6-phenylhexan-3-yl)-2-(4-methoxy-3-hydroxybenzyl)-5-methylimidazo[5,1-f][1,2,4]triazin-4(3H)-one formation at 20 uM after 1 hr by UHPLC-UV-HRMS method2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Lead Diversification at the Nanomole Scale Using Liver Microsomes and Quantitative Nuclear Magnetic Resonance Spectroscopy: Application to Phosphodiesterase 2 Inhibitors.
AID1596314Inhibition of recombinant N-terminal GST tagged human PDE1C (2 to 634 aa) expressed in Sf9 cells at 10xIC50 using FAM-cAMP as substrate incubated for 60 mins by fluorescence plate reader analysis2019European journal of medicinal chemistry, Jul-15, Volume: 174InCl
AID1449245Selectivity ratio of IC50 for bovine PDE5A1 to IC50 for full length recombinant human FLAG-tagged PDE2A3 expressed in sf21 cells2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor.
AID1449253Half life in rat liver microsomes2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor.
AID1872558Displacement of [3H]-cAMP from PDE2 derived form bovine heart incubated for 15 mins by scintillation counting method2022European journal of medicinal chemistry, Mar-15, Volume: 232Therapeutic potential of phosphodiesterase inhibitors for cognitive amelioration in Alzheimer's disease.
AID1449252Apparent intrinsic clearance in human liver microsomes2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor.
AID1164383Ratio of drug level in brain to plasma in rat at 10 mg/kg, po after 30 mins2014ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9
Structure-Based Design of a Potent, Selective, and Brain Penetrating PDE2 Inhibitor with Demonstrated Target Engagement.
AID1330519Inhibition of PDE3B (unknown origin)2017ACS medicinal chemistry letters, Jan-12, Volume: 8, Issue:1
Potential Treatment of Cognitive Impairment in Schizophrenia by Phosphodiesterase 2 (PDE2) Inhibitors.
AID1480124Apparent permeability across RRCK cells after 1.5 hrs2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Lead Diversification at the Nanomole Scale Using Liver Microsomes and Quantitative Nuclear Magnetic Resonance Spectroscopy: Application to Phosphodiesterase 2 Inhibitors.
AID1449241Inhibition of full length recombinant human FLAG-tagged PDE2A3 expressed in sf21 cells using [3H]cGMP as substrate by scintillation proximity assay2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor.
AID1596289Inhibition of recombinant N-terminal GST-tagged full-length human PDE1A1 expressed in Sf9 cells using FAM-cAMP as substrate at 1xIC50 incubated for 60 mins by fluorescence plate reader analysis2019European journal of medicinal chemistry, Jul-15, Volume: 174InCl
AID1574977Inhibition of PDE2 (unknown origin) using [3H]cAMP as substrate measured after 30 mins by scintillation proximity assay2019Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3
Design, synthesis of novel purin-6-one derivatives as phosphodiesterase 2 (PDE2) inhibitors: The neuroprotective and anxiolytic-like effects.
AID1574952Inhibition of PDE2 (unknown origin) using [3H]cAMP or [3H]cGMP as substrate measured after 30 mins by liquid scintillation counting method2019Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3
Design, synthesis of novel purin-6-one derivatives as phosphodiesterase 2 (PDE2) inhibitors: The neuroprotective and anxiolytic-like effects.
AID1330523Inhibition of PDE8A (unknown origin)2017ACS medicinal chemistry letters, Jan-12, Volume: 8, Issue:1
Potential Treatment of Cognitive Impairment in Schizophrenia by Phosphodiesterase 2 (PDE2) Inhibitors.
AID1449254Substrate activity at MDR1 (unknown origin) assessed as efflux ratio of permeability from basolateral to apical side over apical to basolateral side by cell based assay2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor.
AID1330522Inhibition of PDE7B (unknown origin)2017ACS medicinal chemistry letters, Jan-12, Volume: 8, Issue:1
Potential Treatment of Cognitive Impairment in Schizophrenia by Phosphodiesterase 2 (PDE2) Inhibitors.
AID1449246Selectivity ratio of IC50 for bovine PDE6 to IC50 for full length recombinant human FLAG-tagged PDE2A3 expressed in sf21 cells2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor.
AID1440952Selectivity ratio of IC50 for PDE1c (unknown origin) to IC50 for PDE2a (unknown origin)2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Design and Synthesis of Novel and Selective Phosphodiesterase 2 (PDE2a) Inhibitors for the Treatment of Memory Disorders.
AID1596312Inhibition of recombinant N-terminal GST tagged full length human PDE1B expressed in Sf9 cells using FAM-cAMP as substrate at 10xIC50 incubated for 60 mins by fluorescence plate reader analysis2019European journal of medicinal chemistry, Jul-15, Volume: 174InCl
AID1596311Inhibition of recombinant N-terminal GST-tagged full-length human PDE1A1 expressed in Sf9 cells using FAM-cAMP as substrate at 10xIC50 incubated for 60 mins by fluorescence plate reader analysis2019European journal of medicinal chemistry, Jul-15, Volume: 174InCl
AID1596269Inhibition of recombinant N-terminal GST tagged human PDE1C (2 to 634 aa) expressed in Sf9 cells at 0.1xIC50 using FAM-cAMP as substrate incubated for 60 mins by fluorescence plate reader analysis2019European journal of medicinal chemistry, Jul-15, Volume: 174InCl
AID1596268Inhibition of recombinant N-terminal GST tagged full length human PDE1B expressed in Sf9 cells using FAM-cAMP as substrate at 0.1xIC50 incubated for 60 mins by fluorescence plate reader analysis2019European journal of medicinal chemistry, Jul-15, Volume: 174InCl
AID1596315Inhibition of recombinant N-terminal-GST-Th-tagged full length human PDE2A1 expressed in Sf9 cells using FAM-cAMP as substrate at 10xIC50 incubated for 60 mins by fluorescence plate reader analysis2019European journal of medicinal chemistry, Jul-15, Volume: 174InCl
AID977608Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB2013Journal of the American Chemical Society, Aug-14, Volume: 135, Issue:32
X-ray crystal structure of phosphodiesterase 2 in complex with a highly selective, nanomolar inhibitor reveals a binding-induced pocket important for selectivity.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (15)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (6.67)29.6817
2010's13 (86.67)24.3611
2020's1 (6.67)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews3 (20.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other12 (80.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]