BDBM14361 (R,S)-Rolipram::4-(3-cyclopentyloxy-4-methoxy-phenyl)pyrrolidin-2-one::4-[3-(cyclopentyloxy)-4-methoxyphenyl]pyrrolidin-2-one::Adeo::CHEMBL63::Rolipram

SMILES COc1ccc(cc1OC1CCCC1)C1CNC(=O)C1

InChI Key InChIKey=HJORMJIFDVBMOB-UHFFFAOYSA-N

Data  28 KI  242 IC50  3 EC50

PDB links: 9 PDB IDs match this monomer.

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
Find this compound or compounds like it in BindingDB:
   Substructure
Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 273 hits for monomerid = 14361   

TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4C(Rattus norvegicus)
Lead Gene

Curated by ChEMBL
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataKi:  0.00230nMAssay Description:Binding affinity towards rolipram binding site on phosphodiesterase 4 using [3H]rolipram as radioligand in crude rat brain homogenateMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4A/4B/4C/4D(Homo sapiens (Human))
Zambon Group

Curated by ChEMBL
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataKi:  1.60nMAssay Description:Inhibition of rolipram binding to Phosphodiesterase 4More data for this Ligand-Target Pair
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4A/4B/4C/4D(Homo sapiens (Human))
Zambon Group

Curated by ChEMBL
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataKi:  1.60nMAssay Description:Inhibition of human VCAM and Ramos cell VLA-4 interactionMore data for this Ligand-Target Pair
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4A/4B/4C/4D(Homo sapiens (Human))
Zambon Group

Curated by ChEMBL
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataKi:  1.60nMAssay Description:Inhibition of rolipram binding to PDE4 from human neutrophilsMore data for this Ligand-Target Pair
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4A/4B/4C/4D(Homo sapiens (Human))
Zambon Group

Curated by ChEMBL
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataKi:  3.80nMAssay Description:Displacement of [3H]- rolipram binding to guinea pig brainMore data for this Ligand-Target Pair
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4A/4B/4C/4D(Homo sapiens (Human))
Zambon Group

Curated by ChEMBL
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataKi:  3.80nMAssay Description:Inhibition of rolipram binding to phosphodiesterase 4More data for this Ligand-Target Pair
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4A/4B/4C/4D(Homo sapiens (Human))
Zambon Group

Curated by ChEMBL
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataKi:  4.5nMAssay Description:Binding affinity against PDE4 was determined using [3H]- rolipram in guinea pig brain membrane binding assayMore data for this Ligand-Target Pair
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4A/4B/4C/4D(Homo sapiens (Human))
Zambon Group

Curated by ChEMBL
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataKi:  4.5nMAssay Description:Inhibition of rolipram binding to Phosphodiesterase 4More data for this Ligand-Target Pair
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4A/4B/4C/4D(Homo sapiens (Human))
Zambon Group

Curated by ChEMBL
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataKi:  4.5nMAssay Description:Affinity for rolipram binding site of phosphodiesterase type IV (PDE4)More data for this Ligand-Target Pair
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataKi:  11nMAssay Description:Inhibition of [3H]rolipram binding to Phosphodiesterase 4 of rat forebrain membraneMore data for this Ligand-Target Pair
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(RAT)
University Of Tennessee

Curated by PDSP Ki Database
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataKi:  16.6nMMore data for this Ligand-Target Pair
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4D(Homo sapiens (Human))
Human Biomolecular Research Institute

LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataKi:  58.9nM ΔG°:  -10.2kcal/molepH: 8.0 T: 2°CAssay Description:The samples were assayed in a solution composed of PDE4, [3H]cAMP/cAMP, and test compounds. To convert AMP to adenosine, snake venom was added to eac...More data for this Ligand-Target Pair
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataKi:  220nMAssay Description:Ability to inhibit the catalytic activity of human Phosphodiesterase 4B (PDE IVB)More data for this Ligand-Target Pair
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataKi:  221nMAssay Description:Inhibition of human Phosphodiesterase 4BMore data for this Ligand-Target Pair
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataKi:  224nMAssay Description:Inhibition of cAMP hydrolysis by the human phosphodiesterase 4B enzymeMore data for this Ligand-Target Pair
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4D(Homo sapiens (Human))
Human Biomolecular Research Institute

LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataKi:  300nMAssay Description:Inhibition of human recombinant PDE4D3 expressed in baculovirus system by radiometric assayMore data for this Ligand-Target Pair
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4D(Homo sapiens (Human))
Human Biomolecular Research Institute

LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataKi:  375nMAssay Description:PDE4 enzyme activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using SPA kit. [3H]-AMP was captured by the SPA beads, and qu...More data for this Ligand-Target Pair
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4D(Homo sapiens (Human))
Human Biomolecular Research Institute

LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataKi:  382nMAssay Description:PDE4 enzyme activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using SPA kit. [3H]-AMP was captured by the SPA beads, and qu...More data for this Ligand-Target Pair
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4D(Homo sapiens (Human))
Human Biomolecular Research Institute

LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataKi:  490nMAssay Description:Inhibition of human recombinant PDE4D1 expressed in baculovirus system by radiometric assayMore data for this Ligand-Target Pair
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4D(Homo sapiens (Human))
Human Biomolecular Research Institute

LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataKi:  930nMAssay Description:Inhibition of human recombinant PDE4D2 expressed in baculovirus system by radiometric assayMore data for this Ligand-Target Pair
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4A/4B/4C/4D(Homo sapiens (Human))
Zambon Group

Curated by ChEMBL
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataKi:  1.00E+3nMAssay Description:Inhibition of human phosphodiesterase 4More data for this Ligand-Target Pair
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataKi:  1.47E+3nMAssay Description:PDE4 enzyme activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using SPA kit. [3H]-AMP was captured by the SPA beads, and qu...More data for this Ligand-Target Pair
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(RAT)
University Of Tennessee

Curated by PDSP Ki Database
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataKi:  4.10E+3nMMore data for this Ligand-Target Pair
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4A(Homo sapiens (Human))
Purdue Pharma

LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataKi:  7.94E+3nM ΔG°:  -6.88kcal/molepH: 8.0 T: 2°CAssay Description:PDE4 enzyme activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using SPA kit. [3H]-AMP was captured by the SPA beads, and qu...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4D(Homo sapiens (Human))
Human Biomolecular Research Institute

LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataKi:  8.46E+3nMAssay Description:PDE4 enzyme activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using SPA kit. [3H]-AMP was captured by the SPA beads, and qu...More data for this Ligand-Target Pair
TargetProtein cereblon(Homo sapiens (Human))
Max Planck Institute For Developmental Biology

Curated by ChEMBL
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataKi:  1.02E+5nMAssay Description:Binding affinity to human CRBN-thalidomide binding domain expressed in Escherichia coli by measuring baseline corrected normalized fluorescence by MS...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-specific 3',5'-cyclic phosphodiesterase(Homo sapiens (Human))
Upr 421 Du Cnrs

Curated by ChEMBL
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataKi: >2.00E+5nMAssay Description:Inhibition of Phosphodiesterase 5More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-dependent 3',5'-cyclic phosphodiesterase(Homo sapiens (Human))
Upr 421 Du Cnrs

Curated by ChEMBL
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataKi: >2.00E+5nMAssay Description:Inhibition of Phosphodiesterase 2More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4A(Homo sapiens (Human))
Purdue Pharma

LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataEC50:  500nMAssay 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 DepthDetails ArticlePubMed
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50: >2.00E+5nMpH: 7.5 T: 2°CAssay Description:Phosphodiesterase activities were assayed in the presence of inhibitor compounds. Measurement takes advantage of the selective binding of 5-AMP or 5-...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-dependent 3',5'-cyclic phosphodiesterase [574-941](Homo sapiens (Human))
Plexxikon

LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50: >2.00E+5nMpH: 7.5 T: 2°CAssay Description:Phosphodiesterase activities were assayed in the presence of inhibitor compounds. Measurement takes advantage of the selective binding of 5-AMP or 5-...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50: >2.00E+5nMAssay Description:Phosphodiesterase activities were assayed in the presence of inhibitor compounds. Measurement takes advantage of the selective binding of 5-AMP or 5-...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50:  570nMAssay Description:Phosphodiesterase activities were assayed in the presence of inhibitor compounds. Measurement takes advantage of the selective binding of 5-AMP or 5-...More data for this Ligand-Target Pair
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50:  1.10E+3nMAssay Description:Phosphodiesterase activities were assayed in the presence of inhibitor compounds. Measurement takes advantage of the selective binding of 5-AMP or 5-...More data for this Ligand-Target Pair
TargetcGMP-specific 3',5'-cyclic phosphodiesterase [531-875](Homo sapiens (Human))
Plexxikon

LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50: >2.00E+5nMAssay Description:Phosphodiesterase activities were assayed in the presence of inhibitor compounds. Measurement takes advantage of the selective binding of 5-AMP or 5-...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50: >2.00E+5nMAssay Description:Phosphodiesterase activities were assayed in the presence of inhibitor compounds. Measurement takes advantage of the selective binding of 5-AMP or 5-...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50: >2.00E+5nMAssay Description:Phosphodiesterase activities were assayed in the presence of inhibitor compounds. Measurement takes advantage of the selective binding of 5-AMP or 5-...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50: >2.00E+5nMAssay Description:Phosphodiesterase activities were assayed in the presence of inhibitor compounds. Measurement takes advantage of the selective binding of 5-AMP or 5-...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50:  1.40E+5nMAssay Description:Phosphodiesterase activities were assayed in the presence of inhibitor compounds. Measurement takes advantage of the selective binding of 5-AMP or 5-...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50: >2.00E+5nMAssay Description:Phosphodiesterase activities were assayed in the presence of inhibitor compounds. Measurement takes advantage of the selective binding of 5-AMP or 5-...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphodiesterase(Trypanosoma cruzi)
University Of North Carolina

LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50: >1.00E+5nMpH: 7.5 T: 2°CAssay Description:Enzymatic activities were assayed using [3H] cAMP and [3H]cGMP as substrate.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4D(Homo sapiens (Human))
Human Biomolecular Research Institute

LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50:  2.00E+3nMpH: 7.5 T: 2°CAssay Description:Enzymatic activities were assayed using [3H] cAMP and [3H]cGMP as substrate.More data for this Ligand-Target Pair
TargetcGMP-specific 3',5'-cyclic phosphodiesterase(Homo sapiens (Human))
Upr 421 Du Cnrs

Curated by ChEMBL
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50:  2.00E+5nMAssay Description:Inhibition of phosphodiesterase 5 at 20 uMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4A/4B/4C/4D(Homo sapiens (Human))
Zambon Group

Curated by ChEMBL
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50:  320nMAssay Description:Inhibition of guinea pig macrophage Phosphodiesterase 4More data for this Ligand-Target Pair
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4A(Homo sapiens (Human))
Purdue Pharma

LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50:  5.90nMAssay Description:Inhibition of phosphodiesterase (PDE) 4AMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(RAT)
University Of Tennessee

Curated by PDSP Ki Database
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50:  5.70nMAssay Description:Inhibition of phosphodiesterase (PDE) 4BMore data for this Ligand-Target Pair
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4D(Homo sapiens (Human))
Human Biomolecular Research Institute

LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50:  6.40nMAssay Description:Inhibition of phosphodiesterase (PDE) 4DMore data for this Ligand-Target Pair
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4C(Rattus norvegicus)
Lead Gene

Curated by ChEMBL
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50:  2.60nMAssay Description:Displacement of [3H]rolipram binding to Phosphodiesterase 4 in rat brainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4C(Rattus norvegicus)
Lead Gene

Curated by ChEMBL
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50:  490nMAssay Description:Inhibition of phosphodiesterase 4 from rat brain cortexMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4A/4B/4C/4D(Homo sapiens (Human))
Zambon Group

Curated by ChEMBL
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50:  3.50E+3nMAssay Description:Inhibition of human phosphodiesterase 4 from U937 cellsMore data for this Ligand-Target Pair
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