BDBM50042058 (-)-rolipram::(4R)-4-[3-(cyclopentyloxy)-4-methoxyphenyl]pyrrolidin-2-one::(R)-(-)-rolipram::(R)-rolipram::CHEMBL430893

SMILES COc1ccc(cc1OC2CCCC2)[C@H]3CC(=O)NC3

InChI Key InChIKey=HJORMJIFDVBMOB-UHFFFAOYSA-N

Data  21 IC50  1 Kd  1 EC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 23 hits for monomerid = 50042058   

TargetcGMP-inhibited 3',5'-cyclic phosphodiesterase 3A/3B(Human)
Vrije Universiteit

Curated by ChEMBL
LigandPNGBDBM50042058((4R)-4-[3-(cyclopentyloxy)-4-methoxyphenyl]pyrroli...)
Affinity DataIC50: 3.16E+3nMAssay Description:Inhibitory activity of the against phosphodiesterase 3 (PDE3); No significant inhibitory activity at pIC50More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/22/2020
Entry Details Article
PubMed
TargetPlatelet-derived growth factor receptor alpha/beta(Mouse)
Massachusetts General Hospital

Curated by ChEMBL
LigandPNGBDBM50042058((4R)-4-[3-(cyclopentyloxy)-4-methoxyphenyl]pyrroli...)
Affinity DataKd:  1.60nMAssay Description:Binding affinity to human PDE4 assessed as dissociation constantMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/19/2024
Entry Details
PubMed
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(Human)
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM50042058((4R)-4-[3-(cyclopentyloxy)-4-methoxyphenyl]pyrroli...)
Affinity DataIC50: 231nMAssay Description:Inhibition of human His-tagged PDE4B catalytic domain expressed in Escherichia coli BL21-CodonPlus(DE3) cells using [3H]cAMP or [3H]cGMP as substrate...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4D(Human)
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM50042058((4R)-4-[3-(cyclopentyloxy)-4-methoxyphenyl]pyrroli...)
Affinity DataIC50: 231nMAssay Description:Inhibition of human PDE4D2 catalytic domain (79 to 438 residues) Escherichia coli BL21-CodonPlus(DE3) cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(Human)
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM50042058((4R)-4-[3-(cyclopentyloxy)-4-methoxyphenyl]pyrroli...)
Affinity DataIC50: 231nMAssay Description:Inhibition of human N-terminal His6-tagged C-terminal FLAG-tagged PDE4B2 expressed in baculovirus infected sf9 cells using cAMP as substrate by micro...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(Human)
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM50042058((4R)-4-[3-(cyclopentyloxy)-4-methoxyphenyl]pyrroli...)
Affinity DataIC50: 231nMAssay Description:Inhibition of human N-terminal His6-tagged C-terminal FLAG-tagged PDE4B2 expressed in baculovirus infected sf9 cells using cAMP as substrate by micro...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(Human)
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM50042058((4R)-4-[3-(cyclopentyloxy)-4-methoxyphenyl]pyrroli...)
Affinity DataIC50: 231nMAssay Description:Inhibition of human His-tagged PDE4B catalytic domain expressed in Escherichia coli BL21-CodonPlus(DE3) cells using [3H]cAMP or [3H]cGMP as substrate...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4D(Human)
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM50042058((4R)-4-[3-(cyclopentyloxy)-4-methoxyphenyl]pyrroli...)
Affinity DataIC50: 231nMAssay Description:Inhibition of human PDE4D2 catalytic domain (79 to 438 residues) Escherichia coli BL21-CodonPlus(DE3) cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4C(Rat)
Smithkline Beecham Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50042058((4R)-4-[3-(cyclopentyloxy)-4-methoxyphenyl]pyrroli...)
Affinity DataIC50: 5nMAssay Description:Competition of [3H]rolipram binding sites in the central nervous system (HPDE4) in rat brain cytosolMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/22/2020
Entry Details Article
PubMed
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4A/4B/4C/4D(Human)
Smithkline Beecham Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50042058((4R)-4-[3-(cyclopentyloxy)-4-methoxyphenyl]pyrroli...)
Affinity DataIC50: 300nMAssay Description:Inhibition activity against human monocyte derived PDE4 catalytic activity (LPDE4)More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/22/2020
Entry Details Article
PubMed
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4A/4B/4C/4D(Human)
Smithkline Beecham Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50042058((4R)-4-[3-(cyclopentyloxy)-4-methoxyphenyl]pyrroli...)
Affinity DataIC50: 50nMAssay Description:Inhibitory concentration against phosphodiesterase 4 (PDE4) in cytosol of human neutrophilsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/22/2020
Entry Details Article
PubMed
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4A/4B/4C/4D(Human)
Smithkline Beecham Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50042058((4R)-4-[3-(cyclopentyloxy)-4-methoxyphenyl]pyrroli...)
Affinity DataIC50: 50nMAssay Description:Inhibition of phosphodiesterase 4 (PDE4) in human neutrophilsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/22/2020
Entry Details Article
PubMed
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4A(Human)
University of Glasgow

Curated by ChEMBL
LigandPNGBDBM50042058((4R)-4-[3-(cyclopentyloxy)-4-methoxyphenyl]pyrroli...)
Affinity DataIC50: 550nMAssay Description:Inhibition of full-length PDE4A4 using cAMP as substrate by two-step radiochemical assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4A/4B/4C/4D(Human)
Smithkline Beecham Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50042058((4R)-4-[3-(cyclopentyloxy)-4-methoxyphenyl]pyrroli...)
Affinity DataIC50: 1.40E+3nMAssay Description:Inhibition of partially-purified PDE 4 from human monocytesMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/10/2019
Entry Details Article
PubMed
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(Human)
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM50042058((4R)-4-[3-(cyclopentyloxy)-4-methoxyphenyl]pyrroli...)
Affinity DataIC50: 39.8nMAssay Description:Inhibition of human recombinant PDE4B by scintillation proximity assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/21/2013
Entry Details Article
PubMed
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(Human)
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM50042058((4R)-4-[3-(cyclopentyloxy)-4-methoxyphenyl]pyrroli...)
Affinity DataIC50: 500nMAssay Description:Inhibition of human recombinant PDE4B2 assessed as decrease in cAMP hydrolysis preincubated with substrate prior to enzyme addition measured after 30...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4A(Human)
University of Glasgow

Curated by ChEMBL
LigandPNGBDBM50042058((4R)-4-[3-(cyclopentyloxy)-4-methoxyphenyl]pyrroli...)
Affinity DataIC50: 162nMAssay Description:Inhibition of human recombinant PDE4AMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/9/2012
Entry Details Article
PubMed
LigandPNGBDBM50042058((4R)-4-[3-(cyclopentyloxy)-4-methoxyphenyl]pyrroli...)
Affinity DataIC50: 3.69E+3nMAssay Description:Inhibition of human recombinant PDE4CMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/9/2012
Entry Details Article
PubMed
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(Human)
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM50042058((4R)-4-[3-(cyclopentyloxy)-4-methoxyphenyl]pyrroli...)
Affinity DataIC50: 231nMAssay Description:Inhibition of human recombinant PDE4BMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/9/2012
Entry Details Article
PubMed
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4D(Human)
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM50042058((4R)-4-[3-(cyclopentyloxy)-4-methoxyphenyl]pyrroli...)
Affinity DataIC50: 622nMAssay Description:Inhibition of human recombinant PDE4DMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/9/2012
Entry Details Article
PubMed
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(Human)
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM50042058((4R)-4-[3-(cyclopentyloxy)-4-methoxyphenyl]pyrroli...)
Affinity DataIC50: 500nMAssay Description:Inhibition of human recombinant PDE4B2-mediated cAMP hydrolysis for 30 mins by colorimetric assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/23/2012
Entry Details Article
PubMed
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4A(Human)
University of Glasgow

Curated by ChEMBL
LigandPNGBDBM50042058((4R)-4-[3-(cyclopentyloxy)-4-methoxyphenyl]pyrroli...)
Affinity DataIC50: 4.00E+3nMAssay Description:PDE4A activity assessed using human recombinant purified GST-PDE4A248More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4A(Human)
University of Glasgow

Curated by ChEMBL
LigandPNGBDBM50042058((4R)-4-[3-(cyclopentyloxy)-4-methoxyphenyl]pyrroli...)
Affinity DataEC50:  480nMAssay Description:Induction of SQSTM1-dependent intracellular redistribution of GFP-tagged PDE4A4 assessed as maximal accretion of enzyme into fociMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed