Found 24 hits Enzyme Inhibition Constant Data 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 |
Phosphodiesterase 4
(291/344 = 85%)† (Homo sapiens (Human)) | BDBM14775
 (3-(cyclopentyloxy)-N-(3,5-dichloropyridin-4-yl)-4-...)Show InChI InChI=1S/C18H18Cl2N2O3/c1-24-15-7-6-11(8-16(15)25-12-4-2-3-5-12)18(23)22-17-13(19)9-21-10-14(17)20/h6-10,12H,2-5H2,1H3,(H,21,22,23) | PDB
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| 0.400 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Rh£ne-Poulenc Rorer Central Research
Curated by ChEMBL
| Assay Description Binding affinity against PDE4 was determined using [3H]- rolipram in guinea pig brain membrane binding assay |
Bioorg Med Chem Lett 8: 1867-72 (1998)
Article DOI: 10.1016/s0960-894x(98)00324-2 BindingDB Entry DOI: 10.7270/Q2CJ8GPB |
More data for this Ligand-Target Pair |  3D Structure (crystal) |
Phosphodiesterase 4
(291/344 = 85%)† (Homo sapiens (Human)) | BDBM14775
 (3-(cyclopentyloxy)-N-(3,5-dichloropyridin-4-yl)-4-...)Show InChI InChI=1S/C18H18Cl2N2O3/c1-24-15-7-6-11(8-16(15)25-12-4-2-3-5-12)18(23)22-17-13(19)9-21-10-14(17)20/h6-10,12H,2-5H2,1H3,(H,21,22,23) | PDB
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| 0.400 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Rh£ne-Poulenc Rorer Central Research
Curated by ChEMBL
| Assay Description Affinity for rolipram binding site of phosphodiesterase type IV (PDE4) |
Bioorg Med Chem Lett 8: 3053-8 (1998)
Article DOI: 10.1016/s0960-894x(98)00572-1 BindingDB Entry DOI: 10.7270/Q2PV6NK6 |
More data for this Ligand-Target Pair |  3D Structure (crystal) |
Phosphodiesterase 4
(291/344 = 85%)† (Homo sapiens (Human)) | BDBM14775
 (3-(cyclopentyloxy)-N-(3,5-dichloropyridin-4-yl)-4-...)Show InChI InChI=1S/C18H18Cl2N2O3/c1-24-15-7-6-11(8-16(15)25-12-4-2-3-5-12)18(23)22-17-13(19)9-21-10-14(17)20/h6-10,12H,2-5H2,1H3,(H,21,22,23) | PDB
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| 0.850 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Tanabe Seiyaku Co., Ltd
Curated by ChEMBL
| Assay Description Inhibition of rolipram binding to phosphodiesterase 4 |
Bioorg Med Chem Lett 13: 2347-50 (2003)
Article DOI: 10.1016/s0960-894x(03)00438-4 BindingDB Entry DOI: 10.7270/Q2HQ4236 |
More data for this Ligand-Target Pair |  3D Structure (crystal) |
Phosphodiesterase 4
(291/344 = 85%)† (Homo sapiens (Human)) | BDBM14775
 (3-(cyclopentyloxy)-N-(3,5-dichloropyridin-4-yl)-4-...)Show InChI InChI=1S/C18H18Cl2N2O3/c1-24-15-7-6-11(8-16(15)25-12-4-2-3-5-12)18(23)22-17-13(19)9-21-10-14(17)20/h6-10,12H,2-5H2,1H3,(H,21,22,23) | PDB
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SW 8 Rh£ne-Poulenc Rorer Central Research
Curated by ChEMBL
| Assay Description Binding affinity at Phosphodiesterase 4 by measuring displacement of (+/-)-[3H]- Rolipram to guinea pig brain membranes. |
J Med Chem 41: 4216-23 (1998)
BindingDB Entry DOI: 10.7270/Q2K35XCX |
More data for this Ligand-Target Pair |  3D Structure (crystal) |
Phosphodiesterase 4
(291/344 = 85%)† (Homo sapiens (Human)) | BDBM14775
 (3-(cyclopentyloxy)-N-(3,5-dichloropyridin-4-yl)-4-...)Show InChI InChI=1S/C18H18Cl2N2O3/c1-24-15-7-6-11(8-16(15)25-12-4-2-3-5-12)18(23)22-17-13(19)9-21-10-14(17)20/h6-10,12H,2-5H2,1H3,(H,21,22,23) | PDB
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| 1 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Rh£ne-Poulenc Rorer
Curated by ChEMBL
| Assay Description Inhibition of Rolipram binding to Phosphodiesterase 4 |
Bioorg Med Chem Lett 8: 2737-42 (1998)
Article DOI: 10.1016/s0960-894x(98)00497-1 BindingDB Entry DOI: 10.7270/Q2GB267S |
More data for this Ligand-Target Pair |  3D Structure (crystal) |
Phosphodiesterase 4
(291/344 = 85%)† (Homo sapiens (Human)) | BDBM14775
 (3-(cyclopentyloxy)-N-(3,5-dichloropyridin-4-yl)-4-...)Show InChI InChI=1S/C18H18Cl2N2O3/c1-24-15-7-6-11(8-16(15)25-12-4-2-3-5-12)18(23)22-17-13(19)9-21-10-14(17)20/h6-10,12H,2-5H2,1H3,(H,21,22,23) | PDB
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| 1.5 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Zambon Group
Curated by ChEMBL
| Assay Description Inhibition of rolipram binding to PDE4 from human neutrophils |
Bioorg Med Chem Lett 10: 2235-8 (2000)
Article DOI: 10.1016/s0960-894x(00)00449-2 BindingDB Entry DOI: 10.7270/Q2J105BG |
More data for this Ligand-Target Pair |  3D Structure (crystal) |
Phosphodiesterase 4
(291/344 = 85%)† (Homo sapiens (Human)) | BDBM14775
 (3-(cyclopentyloxy)-N-(3,5-dichloropyridin-4-yl)-4-...)Show InChI InChI=1S/C18H18Cl2N2O3/c1-24-15-7-6-11(8-16(15)25-12-4-2-3-5-12)18(23)22-17-13(19)9-21-10-14(17)20/h6-10,12H,2-5H2,1H3,(H,21,22,23) | PDB
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| 1.5 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Zambon Group
Curated by ChEMBL
| Assay Description Inhibition of rolipram binding to Phosphodiesterase 4 |
Bioorg Med Chem Lett 12: 5-8 (2002)
Article DOI: 10.1016/s0960-894x(01)00668-0 BindingDB Entry DOI: 10.7270/Q2SB47Z5 |
More data for this Ligand-Target Pair |  3D Structure (crystal) |
Phosphodiesterase 4
(291/344 = 85%)† (Homo sapiens (Human)) | BDBM14775
 (3-(cyclopentyloxy)-N-(3,5-dichloropyridin-4-yl)-4-...)Show InChI InChI=1S/C18H18Cl2N2O3/c1-24-15-7-6-11(8-16(15)25-12-4-2-3-5-12)18(23)22-17-13(19)9-21-10-14(17)20/h6-10,12H,2-5H2,1H3,(H,21,22,23) | PDB
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| 1.5 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Zambon Group
Curated by ChEMBL
| Assay Description Inhibition of human VCAM and Ramos cell VLA-4 interaction |
Bioorg Med Chem Lett 11: 33-7 (2001)
Article DOI: 10.1016/s0960-894x(00)00587-4 BindingDB Entry DOI: 10.7270/Q2MS3VZ5 |
More data for this Ligand-Target Pair |  3D Structure (crystal) |
Phosphodiesterase 4
(333/344 = 97%)† (RAT-Rattus norvegicus) | BDBM14775
 (3-(cyclopentyloxy)-N-(3,5-dichloropyridin-4-yl)-4-...)Show InChI InChI=1S/C18H18Cl2N2O3/c1-24-15-7-6-11(8-16(15)25-12-4-2-3-5-12)18(23)22-17-13(19)9-21-10-14(17)20/h6-10,12H,2-5H2,1H3,(H,21,22,23) | PDB MMDB
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| 26 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Janssen-Cilag S.A.
Curated by ChEMBL
| Assay Description Inhibition of [3H]rolipram binding to Phosphodiesterase 4 of rat forebrain membrane |
Bioorg Med Chem Lett 12: 653-8 (2002)
Article DOI: 10.1016/s0960-894x(01)00817-4 BindingDB Entry DOI: 10.7270/Q2DV1KF6 |
More data for this Ligand-Target Pair |  3D Structure (crystal) |
cAMP-specific 3',5'-cyclic phosphodiesterase 4D
(334/344 = 97%)† (Homo sapiens (Human)) | BDBM14775
 (3-(cyclopentyloxy)-N-(3,5-dichloropyridin-4-yl)-4-...)Show InChI InChI=1S/C18H18Cl2N2O3/c1-24-15-7-6-11(8-16(15)25-12-4-2-3-5-12)18(23)22-17-13(19)9-21-10-14(17)20/h6-10,12H,2-5H2,1H3,(H,21,22,23) | PDB
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| n/a | n/a | 0.0210 | n/a | n/a | n/a | n/a | n/a | n/a |
King's College London
Curated by ChEMBL
| Assay Description Inhibition of human PDE4D |
Bioorg Med Chem 18: 2204-18 (2010)
Article DOI: 10.1016/j.bmc.2010.01.070 BindingDB Entry DOI: 10.7270/Q27945MJ |
More data for this Ligand-Target Pair |  3D Structure (crystal) |
Phosphodiesterase Type 4 (PDE4D)
(349/349 = 100%)† (Homo sapiens (Human)) | BDBM14775
 (3-(cyclopentyloxy)-N-(3,5-dichloropyridin-4-yl)-4-...)Show InChI InChI=1S/C18H18Cl2N2O3/c1-24-15-7-6-11(8-16(15)25-12-4-2-3-5-12)18(23)22-17-13(19)9-21-10-14(17)20/h6-10,12H,2-5H2,1H3,(H,21,22,23) | PDB MMDB
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| n/a | n/a | 0.0210 | n/a | n/a | n/a | n/a | n/a | n/a |
Plexxikon
| Assay Description Phosphodiesterase activities were assayed in the presence of inhibitor compounds. Measurement takes advantage of the selective binding of 5-AMP or 5-... |
Structure 12: 2233-47 (2004)
Article DOI: 10.1016/j.str.2004.10.004 BindingDB Entry DOI: 10.7270/Q25B00Q1 |
More data for this Ligand-Target Pair |  3D Structure (crystal) |
Phosphodiesterase 4
(291/344 = 85%)† (Homo sapiens (Human)) | BDBM14775
 (3-(cyclopentyloxy)-N-(3,5-dichloropyridin-4-yl)-4-...)Show InChI InChI=1S/C18H18Cl2N2O3/c1-24-15-7-6-11(8-16(15)25-12-4-2-3-5-12)18(23)22-17-13(19)9-21-10-14(17)20/h6-10,12H,2-5H2,1H3,(H,21,22,23) | PDB
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| n/a | n/a | 0.300 | n/a | n/a | n/a | n/a | n/a | n/a |
Tanabe Seiyaku Co., Ltd
Curated by ChEMBL
| Assay Description Inhibition of phosphodiesterase 4 |
Bioorg Med Chem Lett 13: 2347-50 (2003)
Article DOI: 10.1016/s0960-894x(03)00438-4 BindingDB Entry DOI: 10.7270/Q2HQ4236 |
More data for this Ligand-Target Pair |  3D Structure (crystal) |
cAMP-specific 3',5'-cyclic phosphodiesterase 4D
(334/344 = 97%)† (Homo sapiens (Human)) | BDBM14775
 (3-(cyclopentyloxy)-N-(3,5-dichloropyridin-4-yl)-4-...)Show InChI InChI=1S/C18H18Cl2N2O3/c1-24-15-7-6-11(8-16(15)25-12-4-2-3-5-12)18(23)22-17-13(19)9-21-10-14(17)20/h6-10,12H,2-5H2,1H3,(H,21,22,23) | PDB
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| n/a | n/a | 0.800 | n/a | n/a | n/a | n/a | n/a | n/a |
Pfizer Inc
Curated by ChEMBL
| Assay Description Compound was evaluated in vitro for its inhibitory activity on unpurified recombinant Phosphodiesterase 4D |
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 |  3D Structure (crystal) |
Phosphodiesterase 4
(291/344 = 85%)† (Homo sapiens (Human)) | BDBM14775
 (3-(cyclopentyloxy)-N-(3,5-dichloropyridin-4-yl)-4-...)Show InChI InChI=1S/C18H18Cl2N2O3/c1-24-15-7-6-11(8-16(15)25-12-4-2-3-5-12)18(23)22-17-13(19)9-21-10-14(17)20/h6-10,12H,2-5H2,1H3,(H,21,22,23) | PDB
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| n/a | n/a | 1 | n/a | n/a | n/a | n/a | n/a | n/a |
Rh£ne-Poulenc Rorer Central Research
Curated by ChEMBL
| Assay Description Inhibition of phosphodiesterase type IV (PDE4) activity |
Bioorg Med Chem Lett 8: 3053-8 (1998)
Article DOI: 10.1016/s0960-894x(98)00572-1 BindingDB Entry DOI: 10.7270/Q2PV6NK6 |
More data for this Ligand-Target Pair |  3D Structure (crystal) |
Phosphodiesterase 4
(291/344 = 85%)† (Homo sapiens (Human)) | BDBM14775
 (3-(cyclopentyloxy)-N-(3,5-dichloropyridin-4-yl)-4-...)Show InChI InChI=1S/C18H18Cl2N2O3/c1-24-15-7-6-11(8-16(15)25-12-4-2-3-5-12)18(23)22-17-13(19)9-21-10-14(17)20/h6-10,12H,2-5H2,1H3,(H,21,22,23) | PDB
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Rh£ne-Poulenc Rorer
Curated by ChEMBL
| Assay Description Inhibition of Phosphodiesterase 4 (PDE4) from guinea pig macrophages |
Bioorg Med Chem Lett 8: 2737-42 (1998)
Article DOI: 10.1016/s0960-894x(98)00497-1 BindingDB Entry DOI: 10.7270/Q2GB267S |
More data for this Ligand-Target Pair |  3D Structure (crystal) |
Phosphodiesterase 4
(291/344 = 85%)† (Homo sapiens (Human)) | BDBM14775
 (3-(cyclopentyloxy)-N-(3,5-dichloropyridin-4-yl)-4-...)Show InChI InChI=1S/C18H18Cl2N2O3/c1-24-15-7-6-11(8-16(15)25-12-4-2-3-5-12)18(23)22-17-13(19)9-21-10-14(17)20/h6-10,12H,2-5H2,1H3,(H,21,22,23) | PDB
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| n/a | n/a | 1 | n/a | n/a | n/a | n/a | n/a | n/a |
Rh£ne-Poulenc Rorer
Curated by ChEMBL
| Assay Description Inhibition of PDE4 from guinea pig macrophages |
Bioorg Med Chem Lett 8: 2737-42 (1998)
Article DOI: 10.1016/s0960-894x(98)00497-1 BindingDB Entry DOI: 10.7270/Q2GB267S |
More data for this Ligand-Target Pair |  3D Structure (crystal) |
Phosphodiesterase 4
(291/344 = 85%)† (Homo sapiens (Human)) | BDBM14775
 (3-(cyclopentyloxy)-N-(3,5-dichloropyridin-4-yl)-4-...)Show InChI InChI=1S/C18H18Cl2N2O3/c1-24-15-7-6-11(8-16(15)25-12-4-2-3-5-12)18(23)22-17-13(19)9-21-10-14(17)20/h6-10,12H,2-5H2,1H3,(H,21,22,23) | PDB
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| n/a | n/a | 1 | n/a | n/a | n/a | n/a | n/a | n/a |
Zambon Group
Curated by ChEMBL
| Assay Description Inhibition of Phosphodiesterase 4 from human neutrophils |
Bioorg Med Chem Lett 10: 2235-8 (2000)
Article DOI: 10.1016/s0960-894x(00)00449-2 BindingDB Entry DOI: 10.7270/Q2J105BG |
More data for this Ligand-Target Pair |  3D Structure (crystal) |
Phosphodiesterase 4
(291/344 = 85%)† (Homo sapiens (Human)) | BDBM14775
 (3-(cyclopentyloxy)-N-(3,5-dichloropyridin-4-yl)-4-...)Show InChI InChI=1S/C18H18Cl2N2O3/c1-24-15-7-6-11(8-16(15)25-12-4-2-3-5-12)18(23)22-17-13(19)9-21-10-14(17)20/h6-10,12H,2-5H2,1H3,(H,21,22,23) | PDB
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SW 8 Rh£ne-Poulenc Rorer Central Research
Curated by ChEMBL
| Assay Description Concentration to inhibit 50% of Phosphodiesterase 4 (PDE-4) from guinea pig macrophages |
J Med Chem 41: 4216-23 (1998)
BindingDB Entry DOI: 10.7270/Q2K35XCX |
More data for this Ligand-Target Pair |  3D Structure (crystal) |
Phosphodiesterase 4
(291/344 = 85%)† (Homo sapiens (Human)) | BDBM14775
 (3-(cyclopentyloxy)-N-(3,5-dichloropyridin-4-yl)-4-...)Show InChI InChI=1S/C18H18Cl2N2O3/c1-24-15-7-6-11(8-16(15)25-12-4-2-3-5-12)18(23)22-17-13(19)9-21-10-14(17)20/h6-10,12H,2-5H2,1H3,(H,21,22,23) | PDB
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Rh£ne-Poulenc Rorer Central Research
Curated by ChEMBL
| Assay Description Inhibition of Phosphodiesterase type 4 (PDE4) from guinea-pig macrophage |
Bioorg Med Chem Lett 8: 1867-72 (1998)
Article DOI: 10.1016/s0960-894x(98)00324-2 BindingDB Entry DOI: 10.7270/Q2CJ8GPB |
More data for this Ligand-Target Pair |  3D Structure (crystal) |
Phosphodiesterase 4
(291/344 = 85%)† (Homo sapiens (Human)) | BDBM14775
 (3-(cyclopentyloxy)-N-(3,5-dichloropyridin-4-yl)-4-...)Show InChI InChI=1S/C18H18Cl2N2O3/c1-24-15-7-6-11(8-16(15)25-12-4-2-3-5-12)18(23)22-17-13(19)9-21-10-14(17)20/h6-10,12H,2-5H2,1H3,(H,21,22,23) | PDB
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| n/a | n/a | 1 | n/a | n/a | n/a | n/a | n/a | n/a |
Zambon Group
Curated by ChEMBL
| Assay Description Inhibition of human Phosphodiesterase 4 |
Bioorg Med Chem Lett 12: 5-8 (2002)
Article DOI: 10.1016/s0960-894x(01)00668-0 BindingDB Entry DOI: 10.7270/Q2SB47Z5 |
More data for this Ligand-Target Pair |  3D Structure (crystal) |
cAMP-specific 3',5'-cyclic phosphodiesterase 4D
(334/344 = 97%)† (Homo sapiens (Human)) | BDBM14775
 (3-(cyclopentyloxy)-N-(3,5-dichloropyridin-4-yl)-4-...)Show InChI InChI=1S/C18H18Cl2N2O3/c1-24-15-7-6-11(8-16(15)25-12-4-2-3-5-12)18(23)22-17-13(19)9-21-10-14(17)20/h6-10,12H,2-5H2,1H3,(H,21,22,23) | PDB
Reactome pathway KEGG
UniProtKB/SwissProt UniProtKB/TrEMBL
B.MOAD DrugBank antibodypedia GoogleScholar
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Pfizer Inc
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 |  3D Structure (crystal) |
cAMP-specific 3',5'-cyclic phosphodiesterase 4C isoform 1
(291/344 = 85%)† (Homo sapiens (Human)) | BDBM14775
 (3-(cyclopentyloxy)-N-(3,5-dichloropyridin-4-yl)-4-...)Show InChI InChI=1S/C18H18Cl2N2O3/c1-24-15-7-6-11(8-16(15)25-12-4-2-3-5-12)18(23)22-17-13(19)9-21-10-14(17)20/h6-10,12H,2-5H2,1H3,(H,21,22,23) | PDB
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UniProtKB/SwissProt
antibodypedia GoogleScholar
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| n/a | n/a | 3.80 | 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 4C |
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 |  3D Structure (crystal) |
Phosphodiesterase 4
(291/344 = 85%)† (Homo sapiens (Human)) | BDBM14775
 (3-(cyclopentyloxy)-N-(3,5-dichloropyridin-4-yl)-4-...)Show InChI InChI=1S/C18H18Cl2N2O3/c1-24-15-7-6-11(8-16(15)25-12-4-2-3-5-12)18(23)22-17-13(19)9-21-10-14(17)20/h6-10,12H,2-5H2,1H3,(H,21,22,23) | PDB
Reactome pathway
UniProtKB/SwissProt UniProtKB/TrEMBL
antibodypedia antibodypedia antibodypedia antibodypedia GoogleScholar
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CHEMBL DrugBank MMDB PC cid PC sid PDB UniChem
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| n/a | n/a | 9 | n/a | n/a | n/a | n/a | n/a | n/a |
Pfizer Inc.
Curated by ChEMBL
| Assay Description Inhibitory activity on human eosinophil phosphodiesterase 4. |
J Med Chem 41: 2268-77 (1998)
BindingDB Entry DOI: 10.7270/Q27S7RH6 |
More data for this Ligand-Target Pair |  3D Structure (crystal) |
cAMP-specific 3',5'-cyclic phosphodiesterase 4C isoform 1
(291/344 = 85%)† (Homo sapiens (Human)) | BDBM14775
 (3-(cyclopentyloxy)-N-(3,5-dichloropyridin-4-yl)-4-...)Show InChI InChI=1S/C18H18Cl2N2O3/c1-24-15-7-6-11(8-16(15)25-12-4-2-3-5-12)18(23)22-17-13(19)9-21-10-14(17)20/h6-10,12H,2-5H2,1H3,(H,21,22,23) | PDB
Reactome pathway
UniProtKB/SwissProt
antibodypedia GoogleScholar
| Purchase
CHEMBL DrugBank MMDB PC cid PC sid PDB UniChem
Patents
Similars
| PDB Article PubMed
| n/a | n/a | 14 | n/a | n/a | n/a | n/a | n/a | n/a |
Pfizer Inc
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 |  3D Structure (crystal) |