Target Validation Information
TTD ID T61744
Target Name Phosphodiesterase 4A (PDE4A)
Type of Target
Successful
Drug Potency against Target Enprofylline Drug Info IC50 = 15 microM [22]
(2,5-Diphenyl-furan-3-yl)-phenyl-methanone Drug Info IC50 = 340 nM [1]
1-Butyl-3-methyl-3,7-dihydro-purine-2,6-dione Drug Info Ki = 19100 nM [11]
1-Methyl-3-propyl-3,7-dihydro-purine-2,6-dione Drug Info Ki = 10600 nM [11]
2,5-Bis-(3,4-dimethoxy-phenyl)-furan Drug Info IC50 = 560 nM [1]
2,5-Bis-(3-cyclopentyloxy-4-methoxy-phenyl)-furan Drug Info IC50 = 44 nM [1]
4-(2,5-Diphenyl-furan-3-yl)-morpholine Drug Info IC50 = 2300 nM [1]
6-Azido-8-(3-iodo-phenyl)-quinoline Drug Info IC50 = 28 nM [3]
6-Imidazol-1-ylmethyl-8-phenyl-quinoline Drug Info IC50 = 9 nM [3]
8-(3-Azido-phenyl)-6-iodo-quinoline Drug Info IC50 = 2.7 nM [3]
8-(3-Azido-phenyl)-6-pyridin-4-ylmethyl-quinoline Drug Info IC50 = 0.2 nM [3]
8-(3-Nitro-phenyl)-6-phenyl-[1,7]naphthyridine Drug Info IC50 = 4000 nM [2]
Benzyl-(2-imidazol-1-yl-quinazolin-4-yl)-amine Drug Info IC50 = 3100 nM [19]
Benzyl-(2-phenyl-quinazolin-4-yl)-amine Drug Info IC50 = 8200 nM [19]
Benzyl-(2-pyridin-3-yl-quinazolin-4-yl)-amine Drug Info IC50 = 9000 nM [19]
Benzyl-(2-pyridin-4-yl-quinazolin-4-yl)-amine Drug Info IC50 = 7500 nM [19]
Benzyl-(2-thiophen-2-yl-quinazolin-4-yl)-amine Drug Info IC50 = 7600 nM [19]
CC-1088 Drug Info IC50 = 1100 nM [21]
CDP840 Drug Info IC50 = 14 nM [13]
CI-1018 Drug Info IC50 = 1100 nM [12]
CI-1044 Drug Info IC50 = 1700 nM [4]
DENBUFYLLINE Drug Info IC50 = 170 nM [6]
isobutylmethylxanthine Drug Info IC50 = 6900 nM [18]
KURAIDIN Drug Info IC50 = 8270 nM [10]
KURARINOL Drug Info IC50 = 6590 nM [10]
L-454560 Drug Info IC50 = 1.4 nM [17]
L-791943 Drug Info IC50 = 670 nM [7]
L-869298 Drug Info Ki = 0.43 nM [15]
NITRAQUAZONE Drug Info IC50 = 10 nM [5]
Ro 20-1724 Drug Info IC50 = 6000 nM [16]
ROLIPRAM Drug Info IC50 = 4 nM
RS-14491 Drug Info IC50 = 4.8 nM [20]
SCH-351591 Drug Info IC50 = 77 nM [8]
SCH-351591 Drug Info IC50 = 150 nM [9]
SOPHOFLAVESCENOL Drug Info IC50 = 2550 nM [10]
UCB-101333-3 Drug Info IC50 = 630 nM [14]
References
REF 1 Substituted furans as inhibitors of the PDE4 enzyme. Bioorg Med Chem Lett. 1999 Feb 8;9(3):323-6.
REF 2 Palladium-catalyzed cross-coupling reactions for the synthesis of 6, 8-disubstituted 1,7-naphthyridines: a novel class of potent and selective phos... J Med Chem. 2000 Feb 24;43(4):675-82.
REF 3 Hunting the emesis and efficacy targets of PDE4 inhibitors: identification of the photoaffinity probe 8-(3-azidophenyl)-6- [(4-iodo-1H-1-imidazolyl... J Med Chem. 2000 Oct 19;43(21):3820-3.
REF 4 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]indol... J Med Chem. 2000 Dec 14;43(25):4850-67.
REF 5 Synthesis and biological evaluation of 2,5-dihydropyrazol. Bioorg Med Chem Lett. 2000 Dec 4;10(23):2661-4.
REF 6 Pyrazolopyrimidine-2,4-dione sulfonamides: novel and selective calcitonin inducers. J Med Chem. 2002 May 23;45(11):2342-5.
REF 7 Discovery of L-791,943: a potent, selective, non emetic and orally active phosphodiesterase-4 inhibitor. Bioorg Med Chem Lett. 2002 Jun 3;12(11):1457-61.
REF 8 8-Methoxyquinolines as PDE4 inhibitors. Bioorg Med Chem Lett. 2002 Jun 17;12(12):1617-9.
REF 9 Synthesis and profile of SCH351591, a novel PDE4 inhibitor. Bioorg Med Chem Lett. 2002 Jun 17;12(12):1621-3.
REF 10 A prenylated flavonol, sophoflavescenol: a potent and selective inhibitor of cGMP phosphodiesterase 5. Bioorg Med Chem Lett. 2002 Sep 2;12(17):2313-6.
REF 11 Effects of alkyl substitutions of xanthine skeleton on bronchodilation. J Med Chem. 1992 Oct 30;35(22):4039-44.
REF 12 New substituted triaza-benzo[cd]azulen-9-ones as promising phosphodiesterase-4 inhibitors. Bioorg Med Chem Lett. 2004 Jun 21;14(12):3303-6.
REF 13 Discovery of a substituted 8-arylquinoline series of PDE4 inhibitors: structure-activity relationship, optimization, and identification of a highly... Bioorg Med Chem Lett. 2005 Dec 1;15(23):5241-6.
REF 14 First dual M3 antagonists-PDE4 inhibitors: synthesis and SAR of 4,6-diaminopyrimidine derivatives. Bioorg Med Chem Lett. 2006 Apr 1;16(7):1834-9.
REF 15 Enantiomer discrimination illustrated by the high resolution crystal structures of type 4 phosphodiesterase. J Med Chem. 2006 Mar 23;49(6):1867-73.
REF 16 Calcium-independent phosphodiesterase inhibitors as putative antidepressants: [3-(bicycloalkyloxy)-4-methoxyphenyl]-2-imidazolidinones. J Med Chem. 1991 Jan;34(1):291-8.
REF 17 The discovery and synthesis of highly potent subtype selective phosphodiesterase 4D inhibitors. Bioorg Med Chem Lett. 2010 Sep 15;20(18):5502-5.
REF 18 A new generation of phosphodiesterase inhibitors: multiple molecular forms of phosphodiesterase and the potential for drug selectivity. J Med Chem. 1985 May;28(5):537-45.
REF 19 Discovery of potent cyclic GMP phosphodiesterase inhibitors. 2-Pyridyl- and 2-imidazolylquinazolines possessing cyclic GMP phosphodiesterase and th... J Med Chem. 1995 Sep 1;38(18):3547-57.
REF 20 Novel heterocyclic-fused pyridazinones as potent and selective phosphodiesterase IV inhibitors. J Med Chem. 1997 May 9;40(10):1417-21.
REF 21 Thalidomide analogs and PDE4 inhibition. Bioorg Med Chem Lett. 1998 Oct 6;8(19):2669-74.
REF 22 Effects of enprofylline on A1 and A2 adenosine receptors. Eur J Pharmacol. 1985 Oct 29;117(1):25-33.

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