Target Validation Information
Target ID T02001
Target Name Type IV phosphodiesterase
Target Type
Clinical Trial
Drug Potency against Target CDP840 Drug Info IC50 = 14 nM [527742]
3-Isobutyl-1-methyl-3,9-dihydro-purine-2,6-dione Drug Info IC50 = 6900 nM [533395]
ROLIPRAM Drug Info IC50 = 550 nM [530753]
UCB-101333-3 Drug Info IC50 = 630 nM [527990]
1-Methyl-3-propyl-3,7-dihydro-purine-2,6-dione Drug Info Ki = 10600 nM [526756]
1-Butyl-3-methyl-3,7-dihydro-purine-2,6-dione Drug Info Ki = 19100 nM [526756]
DENBUFYLLINE Drug Info IC50 = 170 nM [526336]
CI-1018 Drug Info IC50 = 1100 nM [527082]
ZARDAVERINE Drug Info IC50 = 390 nM [530753]
SCH-351591 Drug Info IC50 = 60 nM [526350]
L-454560 Drug Info IC50 = 1.2 nM [531102]
CC-1088 Drug Info IC50 = 1100 nM [534801]
ZAPRINAST Drug Info Ki = 8760 nM [527441]
Ro 20-1724 Drug Info IC50 = 9100 nM [533395]
SCH-351591 Drug Info IC50 = 51 nM [526349]
L-869298 Drug Info IC50 = 0.4 nM [528081]
References
Ref 527742Bioorg Med Chem Lett. 2005 Dec 1;15(23):5241-6. Epub 2005 Sep 15.Discovery of a substituted 8-arylquinoline series of PDE4 inhibitors: structure-activity relationship, optimization, and identification of a highly potent, well tolerated, PDE4 inhibitor.
Ref 533395J Med Chem. 1985 May;28(5):537-45.A new generation of phosphodiesterase inhibitors: multiple molecular forms of phosphodiesterase and the potential for drug selectivity.
Ref 530753Bioorg Med Chem. 2010 Mar 15;18(6):2204-18. Epub 2010 Feb 8.In silico search for multi-target anti-inflammatories in Chinese herbs and formulas.
Ref 527990Bioorg Med Chem Lett. 2006 Apr 1;16(7):1834-9. Epub 2006 Jan 24.First dual M3 antagonists-PDE4 inhibitors: synthesis and SAR of 4,6-diaminopyrimidine derivatives.
Ref 526756J Med Chem. 1992 Oct 30;35(22):4039-44.Effects of alkyl substitutions of xanthine skeleton on bronchodilation.
Ref 526756J Med Chem. 1992 Oct 30;35(22):4039-44.Effects of alkyl substitutions of xanthine skeleton on bronchodilation.
Ref 526336J Med Chem. 2002 May 23;45(11):2342-5.Pyrazolopyrimidine-2,4-dione sulfonamides: novel and selective calcitonin inducers.
Ref 527082Bioorg Med Chem Lett. 2004 Jun 21;14(12):3303-6.New substituted triaza-benzo[cd]azulen-9-ones as promising phosphodiesterase-4 inhibitors.
Ref 530753Bioorg Med Chem. 2010 Mar 15;18(6):2204-18. Epub 2010 Feb 8.In silico search for multi-target anti-inflammatories in Chinese herbs and formulas.
Ref 526350Bioorg Med Chem Lett. 2002 Jun 17;12(12):1621-3.Synthesis and profile of SCH351591, a novel PDE4 inhibitor.
Ref 531102Bioorg Med Chem Lett. 2010 Sep 15;20(18):5502-5. Epub 2010 Jul 21.The discovery and synthesis of highly potent subtype selective phosphodiesterase 4D inhibitors.
Ref 534801Bioorg Med Chem Lett. 1998 Oct 6;8(19):2669-74.Thalidomide analogs and PDE4 inhibition.
Ref 527441J Med Chem. 2005 Feb 24;48(4):1237-43.8-Substituted analogues of 3-(3-cyclopentyloxy-4-methoxy-benzyl)-8-isopropyl-adenine: highly potent and selective PDE4 inhibitors.
Ref 533395J Med Chem. 1985 May;28(5):537-45.A new generation of phosphodiesterase inhibitors: multiple molecular forms of phosphodiesterase and the potential for drug selectivity.
Ref 526349Bioorg Med Chem Lett. 2002 Jun 17;12(12):1617-9.8-Methoxyquinolines as PDE4 inhibitors.
Ref 528081J Med Chem. 2006 Mar 23;49(6):1867-73.Enantiomer discrimination illustrated by the high resolution crystal structures of type 4 phosphodiesterase.

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