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  29 KI  243 IC50  3 EC50

PDB links: 9 PDB IDs match this monomer.

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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   Substructure
Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 59 hits for monomerid = 14361   

LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataKi:  5nMAssay Description:Activity at Histamine H1 receptor using functional H1 receptor assay on guinea pig ileumMore 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
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
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
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
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 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
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50:  35.7nMAssay Description:Inhibition of recombinant human Phosphodiesterase 4BMore data for this Ligand-Target Pair
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50:  625nMAssay Description:Inhibition of release of TNF alpha in human whole bloodMore data for this Ligand-Target Pair
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50:  52nMAssay Description:Inhibition of human recombinant PDE4B1 activity assessed as residual cAMP concentration by HTRF assayMore data for this Ligand-Target Pair
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50:  98nMAssay Description:Inhibition of human recombinant PDE4B2 assessed after 60 mins by IMAP fluorescence polarization assayMore data for this Ligand-Target Pair
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50:  34nMAssay Description:Inhibition of PDE4BMore data for this Ligand-Target Pair
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50:  1.30E+3nMAssay Description:Inhibition of PDE4B isolated from human U937 cells using [3H]-cAMP as substrate after 30 minsMore data for this Ligand-Target Pair
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50:  86nMAssay Description:Inhibition of human full-length PDE4B1 using AM-Cyclic-3',5'-AMP after 60 mins by fluorescence polarization assayMore data for this Ligand-Target Pair
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50:  1.50E+3nMAssay Description:Inhibition of PDE4B derived from human monocytes using [3H]-cAMP as substrate after 30 minsMore data for this Ligand-Target Pair
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50:  498nMAssay Description:Inhibition of PDE4B1 expressed in yeastMore data for this Ligand-Target Pair
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataEC50:  220nMAssay Description:Inhibition of PDE4B expressed in HEK293 cells assessed as fold reduction in forskolin-stimulated cAMP production pretreated for 30 mins measured 4 hr...More data for this Ligand-Target Pair
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50:  741nMAssay Description:Inhibitory activity against recombinant phosphodiesterase 4B (PDE4B) of human mononuclear lymphocytesMore 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 DataIC50:  2.70E+3nMAssay Description:Inhibitory activity against Phosphodiesterase 4B (PDE4B) from rat source expressed in Saccharomyces cerevisiaeMore data for this Ligand-Target Pair
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50:  231nMAssay Description:Inhibition of human recombinant PDE4BMore data for this Ligand-Target Pair
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50:  2.00E+3nMAssay Description:Inhibition of PDE4BMore data for this Ligand-Target Pair
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50:  105nMAssay Description:Inhibition of PDE4B2 expressed in COS7 cells assessed as cAMP hydrolysisMore data for this Ligand-Target Pair
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50:  941nMAssay Description:Inhibition of PDE4B1 (unknown origin) expressed in sf9 cells using cAMP as substrate preincubated for 15 mins before substrate addition measured afte...More data for this Ligand-Target Pair
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50:  1.00E+3nMAssay Description:Inhibition of recombinant His-tagged PDE4B (unknown origin) expressed in Sf9 cells using cAMP as substrate incubated for 15 mins prior to substrate a...More data for this Ligand-Target Pair
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50:  4.00E+3nMAssay Description:Inhibition of human PDE4B2More data for this Ligand-Target Pair
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50:  80nMAssay Description:Inhibition of human PDE4B1 in cytosolic fraction of lungMore data for this Ligand-Target Pair
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50:  50nMAssay Description:Inhibition of human PDE4B1 in particular fraction of lungMore data for this Ligand-Target Pair
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50:  20nMAssay Description:Inhibition of human PDE4B2 in cytosolic fraction of lungMore data for this Ligand-Target Pair
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50:  210nMAssay Description:Inhibition of human PDE4B2 in particular fraction of lungMore data for this Ligand-Target Pair
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50:  50nMAssay Description:Inhibition of human PDE4B3 in cytosolic fraction of lungMore data for this Ligand-Target Pair
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50:  100nMAssay Description:Inhibition of human PDE4B3 in particular fraction of lungMore data for this Ligand-Target Pair
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50:  86nMAssay Description:Inhibition of full length human PDE4B1 using FAM-3',5'-cAMP as substrate after 1 hr by fluorescence polarization assayMore data for this Ligand-Target Pair
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50:  1.80E+3nMAssay Description:Inhibition of human U937 cells-derived PDE4B using [3H]cAMP as substrate after 30 minsMore data for this Ligand-Target Pair
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50:  1.22E+3nMAssay Description:Inhibition of PDE4B isolated from human U937 cells using [3H]-cAMP incubated for 30 minsMore data for this Ligand-Target Pair
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50:  1.22E+3nMAssay Description:Inhibition of human U937 cells-derived PDE4B using [3H]-cAMP as substrate after 30 minsMore data for this Ligand-Target Pair
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50:  1.10E+3nMAssay Description:Inhibition of human GST-tagged PDE4B expressed in baculovirus infected Sf9 insect cells using cAMP as substrate after 10 mins by PDE-Glo Phosphodiest...More data for this Ligand-Target Pair
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50:  1.27E+3nMAssay Description:Inhibition of recombinant full length human N-terminal GST-tagged PDE4B1 expressed in baculovirus infected Sf9 cells using cAMP as substrate after 1 ...More data for this Ligand-Target Pair
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50:  1.27E+3nMAssay Description:Inhibition of recombinant human full length N-terminal GST-tagged PDE4B1 expressed in baculovirus infected Sf9 cells using cAMP as substrate after 1 ...More data for this Ligand-Target Pair
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50:  1.90E+3nMAssay Description:Inhibition of human U937 cells-derived PDE4B using [3H]-cAMP as substrate measured after 30 minsMore data for this Ligand-Target Pair
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50:  2.00E+3nMAssay Description:Inhibition of human U937 cells-derived PDE4B using [3H]-cAMP as substrate after 30 minsMore data for this Ligand-Target Pair
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50:  1.10E+3nMAssay Description:Inhibition of recombinant human PDE4B using cAMP as substrate after 10 mins by PDE-Glo Phosphodiesterase AssayMore data for this Ligand-Target Pair
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50:  1.14E+4nMAssay Description:Inhibition of PDE4B in human PBMC assessed as inhibition in LPS-induced TNFalpha production preincubated for 30 mins followed by LPS stimulation for ...More data for this Ligand-Target Pair
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50:  1.82E+3nMAssay Description:Inhibition of PDE4B in human U937 cells using [3H] cAMP as substrate incubated for 30 minsMore data for this Ligand-Target Pair
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50:  940nMAssay Description:Inhibition of recombinant His-tagged human PDE4B expressed in Sf9 cells using cAMP as substrate preincubated with enzyme for 15 mins followed by subs...More data for this Ligand-Target Pair
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50:  150nMAssay Description:Inhibition of human full length N-terminal GST-tagged PDE4B1 expressed in baculovirus infected Sf9 cells using cAMP as substrate incubated for 1 hr b...More data for this Ligand-Target Pair
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50:  550nMAssay Description:Inhibition of human PDE4B catalytic domain (152 to 528 residues)More data for this Ligand-Target Pair
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50:  550nMAssay Description:Inhibition of human PDE4B catalytic domain (152 to 528 residues)More data for this Ligand-Target Pair
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50:  550nMAssay 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
LigandPNGBDBM14361((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)
Affinity DataIC50:  550nMAssay 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