Found 13 hits Enz. Inhib. hit(s) with Target = 'cAMP-specific 3',5'-cyclic phosphodiesterase 4A' and Ligand = 'BDBM14361' 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 4A
(Homo sapiens (Human)) | BDBM14361
((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)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) | PDB MMDB
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| 7.94E+3 | -28.8 | n/a | n/a | n/a | n/a | n/a | 8.0 | 22 |
Purdue Pharma LP
| Assay 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... |
J Med Chem 48: 1237-43 (2005)
Article DOI: 10.1021/jm030603w BindingDB Entry DOI: 10.7270/Q2GT5KF0 |
More data for this Ligand-Target Pair | |
cAMP-specific 3',5'-cyclic phosphodiesterase 4A
(Homo sapiens (Human)) | BDBM14361
((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)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) | PDB MMDB
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| n/a | n/a | 4 | n/a | n/a | n/a | n/a | n/a | n/a |
Merck Frosst Centre for Therapeutic Research
Curated by ChEMBL
| Assay Description Inhibition of recombinant human PDE4A expressed in Sf9 cells |
J Med Chem 43: 3820-3 (2000)
BindingDB Entry DOI: 10.7270/Q23T9GG9 |
More data for this Ligand-Target Pair | |
cAMP-specific 3',5'-cyclic phosphodiesterase 4A
(Homo sapiens (Human)) | BDBM14361
((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)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) | PDB MMDB
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| n/a | n/a | 5.90 | n/a | n/a | n/a | n/a | n/a | n/a |
Novartis Horsham Research Center
Curated by ChEMBL
| Assay Description Inhibition of phosphodiesterase (PDE) 4A |
Bioorg Med Chem Lett 8: 3229-34 (1999)
BindingDB Entry DOI: 10.7270/Q2ZS2Z11 |
More data for this Ligand-Target Pair | |
cAMP-specific 3',5'-cyclic phosphodiesterase 4A
(Homo sapiens (Human)) | BDBM14361
((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)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) | PDB MMDB
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| n/a | n/a | 10.7 | n/a | n/a | n/a | n/a | n/a | n/a |
Pfizer Inc.
Curated by ChEMBL
| Assay Description Evaluated in vitro for its inhibitory activity on unpurified recombinant Phosphodiesterase type 4A (PDE4A). |
J Med Chem 41: 266-70 (1998)
Article DOI: 10.1021/jm970685m BindingDB Entry DOI: 10.7270/Q2KD1X11 |
More data for this Ligand-Target Pair | |
cAMP-specific 3',5'-cyclic phosphodiesterase 4A
(Homo sapiens (Human)) | BDBM14361
((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)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) | PDB MMDB
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| n/a | n/a | 11 | n/a | n/a | n/a | n/a | n/a | n/a |
Pfizer, Inc.
Curated by ChEMBL
| Assay Description Inhibition of PDE4A |
Bioorg Med Chem Lett 16: 718-21 (2005)
Article DOI: 10.1016/j.bmcl.2005.10.026 BindingDB Entry DOI: 10.7270/Q2348JXP |
More data for this Ligand-Target Pair | |
cAMP-specific 3',5'-cyclic phosphodiesterase 4A
(Homo sapiens (Human)) | BDBM14361
((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)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) | PDB MMDB
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| n/a | n/a | 67 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description Inhibition of PDE4A (unknown origin) |
Citation and Details
Article DOI: 10.1016/j.ejmech.2020.112492 BindingDB Entry DOI: 10.7270/Q2R21511 |
More data for this Ligand-Target Pair | |
cAMP-specific 3',5'-cyclic phosphodiesterase 4A
(Homo sapiens (Human)) | BDBM14361
((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)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) | PDB MMDB
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| n/a | n/a | 162 | n/a | n/a | n/a | n/a | n/a | n/a |
Universidade Federal do Rio de Janeiro
Curated by ChEMBL
| Assay Description Inhibition of human recombinant PDE4A |
J Med Chem 55: 7525-45 (2012)
Article DOI: 10.1021/jm300514y BindingDB Entry DOI: 10.7270/Q2CC11TC |
More data for this Ligand-Target Pair | |
cAMP-specific 3',5'-cyclic phosphodiesterase 4A
(Homo sapiens (Human)) | BDBM14361
((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)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) | PDB MMDB
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| n/a | n/a | 241 | n/a | n/a | n/a | n/a | n/a | n/a |
Rhône-Poulenc Rorer
Curated by ChEMBL
| Assay Description Inhibition of PDE4A4 expressed in yeast |
J Med Chem 53: 6912-22 (2010)
Article DOI: 10.1021/jm100524j BindingDB Entry DOI: 10.7270/Q2J966K2 |
More data for this Ligand-Target Pair | |
cAMP-specific 3',5'-cyclic phosphodiesterase 4A
(Homo sapiens (Human)) | BDBM14361
((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)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) | PDB MMDB
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| n/a | n/a | 386 | n/a | n/a | n/a | n/a | n/a | n/a |
Southern Medical University
Curated by ChEMBL
| Assay Description Inhibition of full length human PDE4A4 using FAM-3',5'-cAMP as substrate after 1 hr by fluorescence polarization assay |
Eur J Med Chem 124: 372-379 (2016)
Article DOI: 10.1016/j.ejmech.2016.08.052 BindingDB Entry DOI: 10.7270/Q29P33N6 |
More data for this Ligand-Target Pair | |
cAMP-specific 3',5'-cyclic phosphodiesterase 4A
(Homo sapiens (Human)) | BDBM14361
((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)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) | PDB MMDB
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| n/a | n/a | 830 | 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 4A
(Homo sapiens (Human)) | BDBM14361
((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)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) | PDB MMDB
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| n/a | n/a | 1.40E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
Novartis Pharma AG
Curated by ChEMBL
| Assay Description Inhibitory activity against Phosphodiesterase 4A (PDE4A) from human source expressed in Saccharomyces cerevisiae |
J Med Chem 43: 675-82 (2000)
BindingDB Entry DOI: 10.7270/Q2N58N3G |
More data for this Ligand-Target Pair | |
cAMP-specific 3',5'-cyclic phosphodiesterase 4A
(Homo sapiens (Human)) | BDBM14361
((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)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) | PDB MMDB
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| n/a | n/a | 1.95E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
Seoul National University
Curated by ChEMBL
| Assay Description Inhibition of recombinant human N-terminal GST-tagged PDE4A4 (2 to 886 residues) expressed in baculovirus infected Sf9 cells using cAMP as substrate ... |
Eur J Med Chem 145: 673-690 (2018)
Article DOI: 10.1016/j.ejmech.2017.12.069 BindingDB Entry DOI: 10.7270/Q21R6T6D |
More data for this Ligand-Target Pair | |
cAMP-specific 3',5'-cyclic phosphodiesterase 4A
(Homo sapiens (Human)) | BDBM14361
((R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phe...)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) | PDB MMDB
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| n/a | n/a | n/a | n/a | 500 | n/a | n/a | n/a | n/a |
University of Glasgow
Curated by ChEMBL
| Assay Description Induction of SQSTM1-dependent intracellular redistribution of GFP-tagged PDE4A4 assessed as maximal accretion of enzyme into foci |
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 | |