Target Validation Information
Target ID T61744
Target Name CAMP-specific 3',5'-cyclic phosphodiesterase 4A
Target Type
Successful
Drug Potency against Target NITRAQUAZONE Drug Info IC50 = 10 nM [525939]
L-454560 Drug Info IC50 = 1.4 nM [531102]
UCB-101333-3 Drug Info IC50 = 630 nM [527990]
CDP840 Drug Info IC50 = 14 nM [527742]
SOPHOFLAVESCENOL Drug Info IC50 = 2550 nM [526395]
DENBUFYLLINE Drug Info IC50 = 170 nM [526336]
Enprofylline Drug Info IC50 = 15 microM [553137]
Benzyl-(2-pyridin-3-yl-quinazolin-4-yl)-amine Drug Info IC50 = 9000 nM [533684]
Benzyl-(2-pyridin-4-yl-quinazolin-4-yl)-amine Drug Info IC50 = 7500 nM [533684]
1-Butyl-3-methyl-3,7-dihydro-purine-2,6-dione Drug Info Ki = 19100 nM [526756]
L-869298 Drug Info Ki = 0.43 nM [528081]
KURAIDIN Drug Info IC50 = 8270 nM [526395]
Benzyl-(2-thiophen-2-yl-quinazolin-4-yl)-amine Drug Info IC50 = 7600 nM [533684]
Ro 20-1724 Drug Info IC50 = 6000 nM [530521]
SCH-351591 Drug Info IC50 = 77 nM [526349]
L-791943 Drug Info IC50 = 670 nM [526342]
KURARINOL Drug Info IC50 = 6590 nM [526395]
2,5-Bis-(3-cyclopentyloxy-4-methoxy-phenyl)-furan Drug Info IC50 = 44 nM [525447]
8-(3-Azido-phenyl)-6-iodo-quinoline Drug Info IC50 = 2.7 nM [525895]
4-(2,5-Diphenyl-furan-3-yl)-morpholine Drug Info IC50 = 2300 nM [525447]
Benzyl-(2-imidazol-1-yl-quinazolin-4-yl)-amine Drug Info IC50 = 3100 nM [533684]
(2,5-Diphenyl-furan-3-yl)-phenyl-methanone Drug Info IC50 = 340 nM [525447]
2,5-Bis-(3,4-dimethoxy-phenyl)-furan Drug Info IC50 = 560 nM [525447]
3-Isobutyl-1-methyl-3,9-dihydro-purine-2,6-dione Drug Info IC50 = 6900 nM [533395]
6-Imidazol-1-ylmethyl-8-phenyl-quinoline Drug Info IC50 = 9 nM [525895]
8-(3-Azido-phenyl)-6-pyridin-4-ylmethyl-quinoline Drug Info IC50 = 0.2 nM [525895]
6-Azido-8-(3-iodo-phenyl)-quinoline Drug Info IC50 = 28 nM [525895]
CI-1044 Drug Info IC50 = 1700 nM [525932]
CI-1018 Drug Info IC50 = 1100 nM [527082]
SCH-351591 Drug Info IC50 = 150 nM [526350]
8-(3-Nitro-phenyl)-6-phenyl-[1,7]naphthyridine Drug Info IC50 = 4000 nM [525700]
CC-1088 Drug Info IC50 = 1100 nM [534801]
RS-14491 Drug Info IC50 = 4.8 nM [534389]
1-Methyl-3-propyl-3,7-dihydro-purine-2,6-dione Drug Info Ki = 10600 nM [526756]
Benzyl-(2-phenyl-quinazolin-4-yl)-amine Drug Info IC50 = 8200 nM [533684]
ROLIPRAM Drug Info IC50 = 4 nM
References
Ref 525939Bioorg Med Chem Lett. 2000 Dec 4;10(23):2661-4.Synthesis and biological evaluation of 2,5-dihydropyrazol.
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 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 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 526395Bioorg Med Chem Lett. 2002 Sep 2;12(17):2313-6.A prenylated flavonol, sophoflavescenol: a potent and selective inhibitor of cGMP phosphodiesterase 5.
Ref 526336J Med Chem. 2002 May 23;45(11):2342-5.Pyrazolopyrimidine-2,4-dione sulfonamides: novel and selective calcitonin inducers.
Ref 553137Effects of enprofylline on A1 and A2 adenosine receptors. Eur J Pharmacol. 1985 Oct 29;117(1):25-33.
Ref 533684J Med Chem. 1995 Sep 1;38(18):3547-57.Discovery of potent cyclic GMP phosphodiesterase inhibitors. 2-Pyridyl- and 2-imidazolylquinazolines possessing cyclic GMP phosphodiesterase and thromboxane synthesis inhibitory activities.
Ref 533684J Med Chem. 1995 Sep 1;38(18):3547-57.Discovery of potent cyclic GMP phosphodiesterase inhibitors. 2-Pyridyl- and 2-imidazolylquinazolines possessing cyclic GMP phosphodiesterase and thromboxane synthesis inhibitory activities.
Ref 526756J Med Chem. 1992 Oct 30;35(22):4039-44.Effects of alkyl substitutions of xanthine skeleton on bronchodilation.
Ref 528081J Med Chem. 2006 Mar 23;49(6):1867-73.Enantiomer discrimination illustrated by the high resolution crystal structures of type 4 phosphodiesterase.
Ref 526395Bioorg Med Chem Lett. 2002 Sep 2;12(17):2313-6.A prenylated flavonol, sophoflavescenol: a potent and selective inhibitor of cGMP phosphodiesterase 5.
Ref 533684J Med Chem. 1995 Sep 1;38(18):3547-57.Discovery of potent cyclic GMP phosphodiesterase inhibitors. 2-Pyridyl- and 2-imidazolylquinazolines possessing cyclic GMP phosphodiesterase and thromboxane synthesis inhibitory activities.
Ref 530521J Med Chem. 1991 Jan;34(1):291-8.Calcium-independent phosphodiesterase inhibitors as putative antidepressants: [3-(bicycloalkyloxy)-4-methoxyphenyl]-2-imidazolidinones.
Ref 526349Bioorg Med Chem Lett. 2002 Jun 17;12(12):1617-9.8-Methoxyquinolines as PDE4 inhibitors.
Ref 526342Bioorg Med Chem Lett. 2002 Jun 3;12(11):1457-61.Discovery of L-791,943: a potent, selective, non emetic and orally active phosphodiesterase-4 inhibitor.
Ref 526395Bioorg Med Chem Lett. 2002 Sep 2;12(17):2313-6.A prenylated flavonol, sophoflavescenol: a potent and selective inhibitor of cGMP phosphodiesterase 5.
Ref 525447Bioorg Med Chem Lett. 1999 Feb 8;9(3):323-6.Substituted furans as inhibitors of the PDE4 enzyme.
Ref 525895J Med Chem. 2000 Oct 19;43(21):3820-3.Hunting the emesis and efficacy targets of PDE4 inhibitors: identification of the photoaffinity probe 8-(3-azidophenyl)-6- [(4-iodo-1H-1-imidazolyl)methyl]quinoline (APIIMQ).
Ref 525447Bioorg Med Chem Lett. 1999 Feb 8;9(3):323-6.Substituted furans as inhibitors of the PDE4 enzyme.
Ref 533684J Med Chem. 1995 Sep 1;38(18):3547-57.Discovery of potent cyclic GMP phosphodiesterase inhibitors. 2-Pyridyl- and 2-imidazolylquinazolines possessing cyclic GMP phosphodiesterase and thromboxane synthesis inhibitory activities.
Ref 525447Bioorg Med Chem Lett. 1999 Feb 8;9(3):323-6.Substituted furans as inhibitors of the PDE4 enzyme.
Ref 525447Bioorg Med Chem Lett. 1999 Feb 8;9(3):323-6.Substituted furans as inhibitors of the PDE4 enzyme.
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 525895J Med Chem. 2000 Oct 19;43(21):3820-3.Hunting the emesis and efficacy targets of PDE4 inhibitors: identification of the photoaffinity probe 8-(3-azidophenyl)-6- [(4-iodo-1H-1-imidazolyl)methyl]quinoline (APIIMQ).
Ref 525895J Med Chem. 2000 Oct 19;43(21):3820-3.Hunting the emesis and efficacy targets of PDE4 inhibitors: identification of the photoaffinity probe 8-(3-azidophenyl)-6- [(4-iodo-1H-1-imidazolyl)methyl]quinoline (APIIMQ).
Ref 525895J Med Chem. 2000 Oct 19;43(21):3820-3.Hunting the emesis and efficacy targets of PDE4 inhibitors: identification of the photoaffinity probe 8-(3-azidophenyl)-6- [(4-iodo-1H-1-imidazolyl)methyl]quinoline (APIIMQ).
Ref 525932J Med Chem. 2000 Dec 14;43(25):4850-67.Synthesis, structure-activity relationships, and pharmacological profile of 9-amino-4-oxo-1-phenyl-3,4,6,7-tetrahydro[1,4]diazepino[6, 7,1-hi]indoles: discoveryof potent, selective phosphodiesterase type 4 inhibitors.
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 526350Bioorg Med Chem Lett. 2002 Jun 17;12(12):1621-3.Synthesis and profile of SCH351591, a novel PDE4 inhibitor.
Ref 525700J Med Chem. 2000 Feb 24;43(4):675-82.Palladium-catalyzed cross-coupling reactions for the synthesis of 6, 8-disubstituted 1,7-naphthyridines: a novel class of potent and selective phosphodiesterase type 4D inhibitors.
Ref 534801Bioorg Med Chem Lett. 1998 Oct 6;8(19):2669-74.Thalidomide analogs and PDE4 inhibition.
Ref 534389J Med Chem. 1997 May 9;40(10):1417-21.Novel heterocyclic-fused pyridazinones as potent and selective phosphodiesterase IV inhibitors.
Ref 526756J Med Chem. 1992 Oct 30;35(22):4039-44.Effects of alkyl substitutions of xanthine skeleton on bronchodilation.
Ref 533684J Med Chem. 1995 Sep 1;38(18):3547-57.Discovery of potent cyclic GMP phosphodiesterase inhibitors. 2-Pyridyl- and 2-imidazolylquinazolines possessing cyclic GMP phosphodiesterase and thromboxane synthesis inhibitory activities.

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