Therapeutic Targets Database
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Target Validation Information
TTD IDTTDS00280
Target NameCAMP-specific 3',5'-cyclic phosphodiesterase 4A    
Type of TargetSuccessful target    
Drug Potency against TargetEnprofyllineIC50 = 15 microM[1]
8-(3-Nitro-phenyl)-6-pyridin-4-ylmethyl-quinolineIC50 = 0.07 nM[2]
8-(3-Azido-phenyl)-6-pyridin-4-ylmethyl-quinolineIC50 = 0.2 nM[2]
L-454560IC50 = 1.4 nM[3]
NITRAQUAZONEIC50 = 10 nM[4]
CC-1088IC50 = 1100 nM[5]
CI-1018IC50 = 1100 nM[6]
CDP840IC50 = 14 nM[7]
SCH-351591IC50 = 150 nM[8]
(-)-ROLIPRAMIC50 = 162 nM[9]
DENBUFYLLINEIC50 = 170 nM[10]
CI-1044IC50 = 1700 nM[11]
8-(3-Azido-phenyl)-6-iodo-quinolineIC50 = 2.7 nM[2]
4-(2,5-Diphenyl-furan-3-yl)-morpholineIC50 = 2300 nM[12]
SOPHOFLAVESCENOLIC50 = 2550 nM[13]
6-Azido-8-(3-iodo-phenyl)-quinolineIC50 = 28 nM[2]
Benzyl-(2-imidazol-1-yl-quinazolin-4-yl)-amineIC50 = 3100 nM[14]
(2,5-Diphenyl-furan-3-yl)-phenyl-methanoneIC50 = 340 nM[12]
ROLIPRAMIC50 = 4 nM[15]
RS-14491IC50 = 4.8 nM[16]
8-(3-Nitro-phenyl)-6-phenyl-[1,7]naphthyridineIC50 = 4000 nM[17]
2,5-Bis-(3-cyclopentyloxy-4-methoxy-phenyl)-furanIC50 = 44 nM[12]
2,5-Bis-(3,4-dimethoxy-phenyl)-furanIC50 = 560 nM[12]
RO-201724IC50 = 6000 nM[18]
UCB-101333-3IC50 = 630 nM[19]
KURARINOLIC50 = 6590 nM[13]
L-791943IC50 = 670 nM[20]
3-Isobutyl-1-methyl-3,7-dihydro-purine-2,6-dioneIC50 = 6900 nM[21]
Benzyl-(2-pyridin-4-yl-quinazolin-4-yl)-amineIC50 = 7500 nM[14]
Benzyl-(2-thiophen-2-yl-quinazolin-4-yl)-amineIC50 = 7600 nM[14]
SCH-365351IC50 = 77 nM[22]
Benzyl-(2-phenyl-quinazolin-4-yl)-amineIC50 = 8200 nM[14]
KURAIDINIC50 = 8270 nM[13]
6-Imidazol-1-ylmethyl-8-phenyl-quinolineIC50 = 9 nM[2]
Benzyl-(2-pyridin-3-yl-quinazolin-4-yl)-amineIC50 = 9000 nM[14]
L-869298Ki = 0.43 nM[23]
1-Methyl-3-propyl-3,7-dihydro-purine-2,6-dioneKi = 10600 nM[24]
1-Butyl-3-methyl-3,7-dihydro-purine-2,6-dioneKi = 19100 nM[24]
Ref 1Eur J Pharmacol. 1985 Oct 29;117(1):25-33.Effects of enprofylline on A1 and A2 adenosine receptors. To Reference
Ref 2J 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). To Reference
Ref 3Bioorg 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. To Reference
Ref 4Bioorg Med Chem Lett. 2000 Dec 4;10(23):2661-4.Synthesis and biological evaluation of 2,5-dihydropyrazol. To Reference
Ref 5Bioorg Med Chem Lett. 1998 Oct 6;8(19):2669-74.Thalidomide analogs and PDE4 inhibition. To Reference
Ref 6Bioorg Med Chem Lett. 2004 Jun 21;14(12):3303-6.New substituted triaza-benzo[cd]azulen-9-ones as promising phosphodiesterase-4 inhibitors. To Reference
Ref 7Bioorg 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. To Reference
Ref 8Bioorg Med Chem Lett. 2002 Jun 17;12(12):1621-3.Synthesis and profile of SCH351591, a novel PDE4 inhibitor. To Reference
Ref 9J Med Chem. 2007 Jan 25;50(2):344-9.SAR of a series of 5,6-dihydro-(9H)-pyrazolo[3,4-c]-1,2,4-triazolo[4,3-alpha]pyridines as potent inhibitors of human eosinophil phosphodiesterase. To Reference
Ref 10J Med Chem. 2002 May 23;45(11):2342-5.Pyrazolopyrimidine-2,4-dione sulfonamides: novel and selective calcitonin inducers. To Reference
Ref 11J 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: discovery of potent, selective phosphodiesterase type 4 inhibitors. To Reference
Ref 12Bioorg Med Chem Lett. 1999 Feb 8;9(3):323-6.Substituted furans as inhibitors of the PDE4 enzyme. To Reference
Ref 13Bioorg Med Chem Lett. 2002 Sep 2;12(17):2313-6.A prenylated flavonol, sophoflavescenol: a potent and selective inhibitor of cGMP phosphodiesterase 5. To Reference
Ref 14J 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. To Reference
Ref 15Bioorg. Med. Chem. Lett. 5(17):1965-1968 (1995) To Reference
Ref 16J Med Chem. 1997 May 9;40(10):1417-21.Novel heterocyclic-fused pyridazinones as potent and selective phosphodiesterase IV inhibitors. To Reference
Ref 17J 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. To Reference
Ref 18J Med Chem. 1991 Jan;34(1):291-8.Calcium-independent phosphodiesterase inhibitors as putative antidepressants: [3-(bicycloalkyloxy)-4-methoxyphenyl]-2-imidazolidinones. To Reference
Ref 19Bioorg 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. To Reference
Ref 20Bioorg 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. To Reference
Ref 21J 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. To Reference
Ref 22Bioorg Med Chem Lett. 2002 Jun 17;12(12):1617-9.8-Methoxyquinolines as PDE4 inhibitors. To Reference
Ref 23J Med Chem. 2006 Mar 23;49(6):1867-73.Enantiomer discrimination illustrated by the high resolution crystal structures of type 4 phosphodiesterase. To Reference
Ref 24J Med Chem. 1992 Oct 30;35(22):4039-44.Effects of alkyl substitutions of xanthine skeleton on bronchodilation. To Reference



 

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