Found 21 hits of ic50 for monomerid = 50042058 Target/Host (Institution) | Ligand | Target/Host Links | Ligand Links | Trg + Lig Links | Ki nM | ΔG° kJ/mole | IC50 nM | Kd nM | EC50/IC50 nM | koff s-1 | kon M-1s-1 | pH | Temp °C |
cAMP-specific 3',5'-cyclic phosphodiesterase 4C
(Rattus norvegicus) | BDBM50042058
((-)-rolipram | (4R)-4-[3-(cyclopentyloxy)-4-methox...)Show InChI InChI=1S/C16H21NO3/c1-19-14-7-6-11(12-9-16(18)17-10-12)8-15(14)20-13-4-2-3-5-13/h6-8,12-13H,2-5,9-10H2,1H3,(H,17,18)/t12-/m0/s1 | PDB
UniProtKB/SwissProt
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| Article PubMed
| n/a | n/a | 5 | n/a | n/a | n/a | n/a | n/a | n/a |
SmithKline Beecham Pharmaceuticals
Curated by ChEMBL
| Assay Description Competition of [3H]rolipram binding sites in the central nervous system (HPDE4) in rat brain cytosol |
J Med Chem 41: 821-35 (1998)
Article DOI: 10.1021/jm970090r BindingDB Entry DOI: 10.7270/Q2WD439M |
More data for this Ligand-Target Pair | |
cAMP-specific 3',5'-cyclic phosphodiesterase 4B
(Homo sapiens (Human)) | BDBM50042058
((-)-rolipram | (4R)-4-[3-(cyclopentyloxy)-4-methox...)Show InChI InChI=1S/C16H21NO3/c1-19-14-7-6-11(12-9-16(18)17-10-12)8-15(14)20-13-4-2-3-5-13/h6-8,12-13H,2-5,9-10H2,1H3,(H,17,18)/t12-/m0/s1 | PDB
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| Article PubMed
| n/a | n/a | 39.8 | n/a | n/a | n/a | n/a | n/a | n/a |
GlaxoSmithKline Medicines Research Centre
Curated by ChEMBL
| Assay Description Inhibition of human recombinant PDE4B by scintillation proximity assay |
Bioorg Med Chem Lett 19: 5261-5 (2009)
Article DOI: 10.1016/j.bmcl.2009.04.012 BindingDB Entry DOI: 10.7270/Q2K075HB |
More data for this Ligand-Target Pair | |
cAMP-specific 3',5'-cyclic phosphodiesterase 4A/4B/4C/4D
(Homo sapiens (Human)) | BDBM50042058
((-)-rolipram | (4R)-4-[3-(cyclopentyloxy)-4-methox...)Show InChI InChI=1S/C16H21NO3/c1-19-14-7-6-11(12-9-16(18)17-10-12)8-15(14)20-13-4-2-3-5-13/h6-8,12-13H,2-5,9-10H2,1H3,(H,17,18)/t12-/m0/s1 | PDB
UniProtKB/SwissProt
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| Article PubMed
| n/a | n/a | 50 | n/a | n/a | n/a | n/a | n/a | n/a |
Vrije Universiteit
Curated by ChEMBL
| Assay Description Inhibitory concentration against phosphodiesterase 4 (PDE4) in cytosol of human neutrophils |
J Med Chem 45: 2520-5 (2002)
Article DOI: 10.1021/jm0110340 BindingDB Entry DOI: 10.7270/Q2862K56 |
More data for this Ligand-Target Pair | |
cAMP-specific 3',5'-cyclic phosphodiesterase 4A/4B/4C/4D
(Homo sapiens (Human)) | BDBM50042058
((-)-rolipram | (4R)-4-[3-(cyclopentyloxy)-4-methox...)Show InChI InChI=1S/C16H21NO3/c1-19-14-7-6-11(12-9-16(18)17-10-12)8-15(14)20-13-4-2-3-5-13/h6-8,12-13H,2-5,9-10H2,1H3,(H,17,18)/t12-/m0/s1 | PDB
UniProtKB/SwissProt
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| Article PubMed
| n/a | n/a | 50 | n/a | n/a | n/a | n/a | n/a | n/a |
Vrije Universiteit
Curated by ChEMBL
| Assay Description Inhibition of phosphodiesterase 4 (PDE4) in human neutrophils |
J Med Chem 44: 2523-35 (2001)
Article DOI: 10.1021/jm010838c BindingDB Entry DOI: 10.7270/Q23N2644 |
More data for this Ligand-Target Pair | |
cAMP-specific 3',5'-cyclic phosphodiesterase 4A
(Homo sapiens (Human)) | BDBM50042058
((-)-rolipram | (4R)-4-[3-(cyclopentyloxy)-4-methox...)Show InChI InChI=1S/C16H21NO3/c1-19-14-7-6-11(12-9-16(18)17-10-12)8-15(14)20-13-4-2-3-5-13/h6-8,12-13H,2-5,9-10H2,1H3,(H,17,18)/t12-/m0/s1 | PDB MMDB
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| Article PubMed
| n/a | n/a | 162 | n/a | n/a | n/a | n/a | n/a | n/a |
Pfizer Global Research and Development
Curated by ChEMBL
| Assay Description Inhibition of human recombinant PDE4A |
J Med Chem 50: 344-9 (2007)
Article DOI: 10.1021/jm060904g BindingDB Entry DOI: 10.7270/Q2K0753Z |
More data for this Ligand-Target Pair | |
cAMP-specific 3',5'-cyclic phosphodiesterase 4B
(Homo sapiens (Human)) | BDBM50042058
((-)-rolipram | (4R)-4-[3-(cyclopentyloxy)-4-methox...)Show InChI InChI=1S/C16H21NO3/c1-19-14-7-6-11(12-9-16(18)17-10-12)8-15(14)20-13-4-2-3-5-13/h6-8,12-13H,2-5,9-10H2,1H3,(H,17,18)/t12-/m0/s1 | PDB
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| Article PubMed
| n/a | n/a | 231 | n/a | n/a | n/a | n/a | n/a | n/a |
Vrije Universiteit Amsterdam
Curated by ChEMBL
| Assay 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... |
J Med Chem 59: 7029-65 (2016)
Article DOI: 10.1021/acs.jmedchem.5b01813 BindingDB Entry DOI: 10.7270/Q2RX9GJ4 |
More data for this Ligand-Target Pair | |
cAMP-specific 3',5'-cyclic phosphodiesterase 4B
(Homo sapiens (Human)) | BDBM50042058
((-)-rolipram | (4R)-4-[3-(cyclopentyloxy)-4-methox...)Show InChI InChI=1S/C16H21NO3/c1-19-14-7-6-11(12-9-16(18)17-10-12)8-15(14)20-13-4-2-3-5-13/h6-8,12-13H,2-5,9-10H2,1H3,(H,17,18)/t12-/m0/s1 | PDB
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| Article PubMed
| n/a | n/a | 231 | n/a | n/a | n/a | n/a | n/a | n/a |
Pfizer Global Research and Development
Curated by ChEMBL
| Assay Description Inhibition of human recombinant PDE4B |
J Med Chem 50: 344-9 (2007)
Article DOI: 10.1021/jm060904g BindingDB Entry DOI: 10.7270/Q2K0753Z |
More data for this Ligand-Target Pair | |
cAMP-specific 3',5'-cyclic phosphodiesterase 4B
(Homo sapiens (Human)) | BDBM50042058
((-)-rolipram | (4R)-4-[3-(cyclopentyloxy)-4-methox...)Show InChI InChI=1S/C16H21NO3/c1-19-14-7-6-11(12-9-16(18)17-10-12)8-15(14)20-13-4-2-3-5-13/h6-8,12-13H,2-5,9-10H2,1H3,(H,17,18)/t12-/m0/s1 | PDB
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| Article PubMed
| n/a | n/a | 231 | n/a | n/a | n/a | n/a | n/a | n/a |
Vrije Universiteit Amsterdam
Curated by ChEMBL
| Assay 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... |
J Med Chem 59: 7029-65 (2016)
Article DOI: 10.1021/acs.jmedchem.5b01813 BindingDB Entry DOI: 10.7270/Q2RX9GJ4 |
More data for this Ligand-Target Pair | |
cAMP-specific 3',5'-cyclic phosphodiesterase 4D
(Homo sapiens (Human)) | BDBM50042058
((-)-rolipram | (4R)-4-[3-(cyclopentyloxy)-4-methox...)Show InChI InChI=1S/C16H21NO3/c1-19-14-7-6-11(12-9-16(18)17-10-12)8-15(14)20-13-4-2-3-5-13/h6-8,12-13H,2-5,9-10H2,1H3,(H,17,18)/t12-/m0/s1 | PDB
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| n/a | n/a | 231 | n/a | n/a | n/a | n/a | n/a | n/a |
Vrije Universiteit Amsterdam
Curated by ChEMBL
| Assay Description Inhibition of human PDE4D2 catalytic domain (79 to 438 residues) Escherichia coli BL21-CodonPlus(DE3) cells |
J Med Chem 59: 7029-65 (2016)
Article DOI: 10.1021/acs.jmedchem.5b01813 BindingDB Entry DOI: 10.7270/Q2RX9GJ4 |
More data for this Ligand-Target Pair | |
cAMP-specific 3',5'-cyclic phosphodiesterase 4B
(Homo sapiens (Human)) | BDBM50042058
((-)-rolipram | (4R)-4-[3-(cyclopentyloxy)-4-methox...)Show InChI InChI=1S/C16H21NO3/c1-19-14-7-6-11(12-9-16(18)17-10-12)8-15(14)20-13-4-2-3-5-13/h6-8,12-13H,2-5,9-10H2,1H3,(H,17,18)/t12-/m0/s1 | PDB
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| Article PubMed
| n/a | n/a | 231 | n/a | n/a | n/a | n/a | n/a | n/a |
Vrije Universiteit Amsterdam
Curated by ChEMBL
| Assay 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... |
J Med Chem 59: 7029-65 (2016)
Article DOI: 10.1021/acs.jmedchem.5b01813 BindingDB Entry DOI: 10.7270/Q2RX9GJ4 |
More data for this Ligand-Target Pair | |
cAMP-specific 3',5'-cyclic phosphodiesterase 4D
(Homo sapiens (Human)) | BDBM50042058
((-)-rolipram | (4R)-4-[3-(cyclopentyloxy)-4-methox...)Show InChI InChI=1S/C16H21NO3/c1-19-14-7-6-11(12-9-16(18)17-10-12)8-15(14)20-13-4-2-3-5-13/h6-8,12-13H,2-5,9-10H2,1H3,(H,17,18)/t12-/m0/s1 | PDB
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| Article PubMed
| n/a | n/a | 231 | n/a | n/a | n/a | n/a | n/a | n/a |
Vrije Universiteit Amsterdam
Curated by ChEMBL
| Assay Description Inhibition of human PDE4D2 catalytic domain (79 to 438 residues) Escherichia coli BL21-CodonPlus(DE3) cells |
J Med Chem 59: 7029-65 (2016)
Article DOI: 10.1021/acs.jmedchem.5b01813 BindingDB Entry DOI: 10.7270/Q2RX9GJ4 |
More data for this Ligand-Target Pair | |
cAMP-specific 3',5'-cyclic phosphodiesterase 4B
(Homo sapiens (Human)) | BDBM50042058
((-)-rolipram | (4R)-4-[3-(cyclopentyloxy)-4-methox...)Show InChI InChI=1S/C16H21NO3/c1-19-14-7-6-11(12-9-16(18)17-10-12)8-15(14)20-13-4-2-3-5-13/h6-8,12-13H,2-5,9-10H2,1H3,(H,17,18)/t12-/m0/s1 | PDB
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| Article PubMed
| n/a | n/a | 231 | n/a | n/a | n/a | n/a | n/a | n/a |
Vrije Universiteit Amsterdam
Curated by ChEMBL
| Assay 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... |
J Med Chem 59: 7029-65 (2016)
Article DOI: 10.1021/acs.jmedchem.5b01813 BindingDB Entry DOI: 10.7270/Q2RX9GJ4 |
More data for this Ligand-Target Pair | |
cAMP-specific 3',5'-cyclic phosphodiesterase 4A/4B/4C/4D
(Homo sapiens (Human)) | BDBM50042058
((-)-rolipram | (4R)-4-[3-(cyclopentyloxy)-4-methox...)Show InChI InChI=1S/C16H21NO3/c1-19-14-7-6-11(12-9-16(18)17-10-12)8-15(14)20-13-4-2-3-5-13/h6-8,12-13H,2-5,9-10H2,1H3,(H,17,18)/t12-/m0/s1 | PDB
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| Article PubMed
| n/a | n/a | 300 | n/a | n/a | n/a | n/a | n/a | n/a |
SmithKline Beecham Pharmaceuticals
Curated by ChEMBL
| Assay Description Inhibition activity against human monocyte derived PDE4 catalytic activity (LPDE4) |
J Med Chem 41: 821-35 (1998)
Article DOI: 10.1021/jm970090r BindingDB Entry DOI: 10.7270/Q2WD439M |
More data for this Ligand-Target Pair | |
cAMP-specific 3',5'-cyclic phosphodiesterase 4B
(Homo sapiens (Human)) | BDBM50042058
((-)-rolipram | (4R)-4-[3-(cyclopentyloxy)-4-methox...)Show InChI InChI=1S/C16H21NO3/c1-19-14-7-6-11(12-9-16(18)17-10-12)8-15(14)20-13-4-2-3-5-13/h6-8,12-13H,2-5,9-10H2,1H3,(H,17,18)/t12-/m0/s1 | PDB
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| Article PubMed
| n/a | n/a | 500 | n/a | n/a | n/a | n/a | n/a | n/a |
Sun Yat-sen University
Curated by ChEMBL
| Assay Description Inhibition of human recombinant PDE4B2-mediated cAMP hydrolysis for 30 mins by colorimetric assay |
Bioorg Med Chem Lett 22: 1523-6 (2012)
Article DOI: 10.1016/j.bmcl.2012.01.013 BindingDB Entry DOI: 10.7270/Q2794548 |
More data for this Ligand-Target Pair | |
cAMP-specific 3',5'-cyclic phosphodiesterase 4B
(Homo sapiens (Human)) | BDBM50042058
((-)-rolipram | (4R)-4-[3-(cyclopentyloxy)-4-methox...)Show InChI InChI=1S/C16H21NO3/c1-19-14-7-6-11(12-9-16(18)17-10-12)8-15(14)20-13-4-2-3-5-13/h6-8,12-13H,2-5,9-10H2,1H3,(H,17,18)/t12-/m0/s1 | PDB
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| Article PubMed
| n/a | n/a | 500 | n/a | n/a | n/a | n/a | n/a | n/a |
Sun Yat-sen University
Curated by ChEMBL
| Assay Description Inhibition of human recombinant PDE4B2 assessed as decrease in cAMP hydrolysis preincubated with substrate prior to enzyme addition measured after 30... |
Bioorg Med Chem Lett 23: 1548-52 (2013)
Article DOI: 10.1016/j.bmcl.2012.11.058 BindingDB Entry DOI: 10.7270/Q2WM1FRH |
More data for this Ligand-Target Pair | |
cAMP-specific 3',5'-cyclic phosphodiesterase 4A
(Homo sapiens (Human)) | BDBM50042058
((-)-rolipram | (4R)-4-[3-(cyclopentyloxy)-4-methox...)Show InChI InChI=1S/C16H21NO3/c1-19-14-7-6-11(12-9-16(18)17-10-12)8-15(14)20-13-4-2-3-5-13/h6-8,12-13H,2-5,9-10H2,1H3,(H,17,18)/t12-/m0/s1 | PDB MMDB
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| Article PubMed
| n/a | n/a | 550 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Glasgow
Curated by ChEMBL
| Assay Description Inhibition of full-length PDE4A4 using cAMP as substrate by two-step radiochemical assay |
J Med Chem 54: 3331-47 (2011)
Article DOI: 10.1021/jm200070e BindingDB Entry DOI: 10.7270/Q2CF9R75 |
More data for this Ligand-Target Pair | |
cAMP-specific 3',5'-cyclic phosphodiesterase 4D
(Homo sapiens (Human)) | BDBM50042058
((-)-rolipram | (4R)-4-[3-(cyclopentyloxy)-4-methox...)Show InChI InChI=1S/C16H21NO3/c1-19-14-7-6-11(12-9-16(18)17-10-12)8-15(14)20-13-4-2-3-5-13/h6-8,12-13H,2-5,9-10H2,1H3,(H,17,18)/t12-/m0/s1 | PDB
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| Article PubMed
| n/a | n/a | 622 | n/a | n/a | n/a | n/a | n/a | n/a |
Pfizer Global Research and Development
Curated by ChEMBL
| Assay Description Inhibition of human recombinant PDE4D |
J Med Chem 50: 344-9 (2007)
Article DOI: 10.1021/jm060904g BindingDB Entry DOI: 10.7270/Q2K0753Z |
More data for this Ligand-Target Pair | |
cAMP-specific 3',5'-cyclic phosphodiesterase 4A/4B/4C/4D
(Homo sapiens (Human)) | BDBM50042058
((-)-rolipram | (4R)-4-[3-(cyclopentyloxy)-4-methox...)Show InChI InChI=1S/C16H21NO3/c1-19-14-7-6-11(12-9-16(18)17-10-12)8-15(14)20-13-4-2-3-5-13/h6-8,12-13H,2-5,9-10H2,1H3,(H,17,18)/t12-/m0/s1 | PDB
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| Article PubMed
| n/a | n/a | 1.40E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
SmithKline Beecham Pharmaceuticals
Curated by ChEMBL
| Assay Description Inhibition of partially-purified PDE 4 from human monocytes |
J Med Chem 36: 3274-7 (1993)
Article DOI: 10.1021/jm00074a007 BindingDB Entry DOI: 10.7270/Q24M96RT |
More data for this Ligand-Target Pair | |
cGMP-inhibited 3',5'-cyclic phosphodiesterase 3A/3B
(Homo sapiens (Human)) | BDBM50042058
((-)-rolipram | (4R)-4-[3-(cyclopentyloxy)-4-methox...)Show InChI InChI=1S/C16H21NO3/c1-19-14-7-6-11(12-9-16(18)17-10-12)8-15(14)20-13-4-2-3-5-13/h6-8,12-13H,2-5,9-10H2,1H3,(H,17,18)/t12-/m0/s1 | PDB MMDB
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| Article PubMed
| n/a | n/a | <3.16E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
Vrije Universiteit
Curated by ChEMBL
| Assay Description Inhibitory activity of the against phosphodiesterase 3 (PDE3); No significant inhibitory activity at pIC50 |
J Med Chem 44: 2523-35 (2001)
Article DOI: 10.1021/jm010838c BindingDB Entry DOI: 10.7270/Q23N2644 |
More data for this Ligand-Target Pair | |
cAMP-specific 3',5'-cyclic phosphodiesterase 4C
(Homo sapiens (Human)) | BDBM50042058
((-)-rolipram | (4R)-4-[3-(cyclopentyloxy)-4-methox...)Show InChI InChI=1S/C16H21NO3/c1-19-14-7-6-11(12-9-16(18)17-10-12)8-15(14)20-13-4-2-3-5-13/h6-8,12-13H,2-5,9-10H2,1H3,(H,17,18)/t12-/m0/s1 | PDB
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| Article PubMed
| n/a | n/a | 3.69E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
Pfizer Global Research and Development
Curated by ChEMBL
| Assay Description Inhibition of human recombinant PDE4C |
J Med Chem 50: 344-9 (2007)
Article DOI: 10.1021/jm060904g BindingDB Entry DOI: 10.7270/Q2K0753Z |
More data for this Ligand-Target Pair | |
cAMP-specific 3',5'-cyclic phosphodiesterase 4A
(Homo sapiens (Human)) | BDBM50042058
((-)-rolipram | (4R)-4-[3-(cyclopentyloxy)-4-methox...)Show InChI InChI=1S/C16H21NO3/c1-19-14-7-6-11(12-9-16(18)17-10-12)8-15(14)20-13-4-2-3-5-13/h6-8,12-13H,2-5,9-10H2,1H3,(H,17,18)/t12-/m0/s1 | PDB MMDB
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| PubMed
| n/a | n/a | 4.00E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
Merck Frosst Centre for Therapeutic Research
Curated by ChEMBL
| Assay Description PDE4A activity assessed using human recombinant purified GST-PDE4A248 |
Bioorg Med Chem Lett 9: 323-6 (1999)
BindingDB Entry DOI: 10.7270/Q27S7MXX |
More data for this Ligand-Target Pair | |