Target Validation Information
TTD ID	T10265
Target Name	Phosphodiesterase 4B (PDE4B)
Type of Target	Clinical trial
Drug Potency against Target	8-(3-Nitro-phenyl)-6-phenyl-[1,7]naphthyridine	Drug Info	IC50 = 4000 nM	[1]
	Benzyl-(2-imidazol-1-yl-quinazolin-4-yl)-amine	Drug Info	IC50 = 3100 nM	[15]
	Benzyl-(2-phenyl-quinazolin-4-yl)-amine	Drug Info	IC50 = 8200 nM	[15]
	Benzyl-(2-pyridin-3-yl-quinazolin-4-yl)-amine	Drug Info	IC50 = 9000 nM	[15]
	Benzyl-(2-pyridin-4-yl-quinazolin-4-yl)-amine	Drug Info	IC50 = 7500 nM	[15]
	Benzyl-(2-thiophen-2-yl-quinazolin-4-yl)-amine	Drug Info	IC50 = 7600 nM	[15]
	CC-1088	Drug Info	IC50 = 1100 nM	[17]
	CDP840	Drug Info	IC50 = 14 nM	[9]
	CI-1018	Drug Info	IC50 = 1100 nM	[8]
	CI-1044	Drug Info	IC50 = 1700 nM	[2]
	DENBUFYLLINE	Drug Info	IC50 = 170 nM	[4]
	isobutylmethylxanthine	Drug Info	IC50 = 6900 nM	[14]
	KURAIDIN	Drug Info	IC50 = 8270 nM	[7]
	KURARINOL	Drug Info	IC50 = 6590 nM	[7]
	L-454560	Drug Info	IC50 = 0.5 nM	[13]
	L-869298	Drug Info	IC50 = 0.4 nM	[11]
	NITRAQUAZONE	Drug Info	IC50 = 10 nM	[3]
	Ro 20-1724	Drug Info	IC50 = 6000 nM	[12]
	ROLIPRAM	Drug Info	IC50 = 6 nM	[16]
	RS-14491	Drug Info	IC50 = 4.8 nM	[16]
	SCH-351591	Drug Info	IC50 = 77 nM	[5]
	SCH-351591	Drug Info	IC50 = 150 nM	[6]
	SOPHOFLAVESCENOL	Drug Info	IC50 = 2550 nM	[7]
	UCB-101333-3	Drug Info	IC50 = 630 nM	[10]
References
REF 1	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 2	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 3	Synthesis and biological evaluation of 2,5-dihydropyrazol. Bioorg Med Chem Lett. 2000 Dec 4;10(23):2661-4.
REF 4	Pyrazolopyrimidine-2,4-dione sulfonamides: novel and selective calcitonin inducers. J Med Chem. 2002 May 23;45(11):2342-5.
REF 5	8-Methoxyquinolines as PDE4 inhibitors. Bioorg Med Chem Lett. 2002 Jun 17;12(12):1617-9.
REF 6	Synthesis and profile of SCH351591, a novel PDE4 inhibitor. Bioorg Med Chem Lett. 2002 Jun 17;12(12):1621-3.
REF 7	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 8	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 9	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 10	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 11	Enantiomer discrimination illustrated by the high resolution crystal structures of type 4 phosphodiesterase. J Med Chem. 2006 Mar 23;49(6):1867-73.
REF 12	Calcium-independent phosphodiesterase inhibitors as putative antidepressants: [3-(bicycloalkyloxy)-4-methoxyphenyl]-2-imidazolidinones. J Med Chem. 1991 Jan;34(1):291-8.
REF 13	The discovery and synthesis of highly potent subtype selective phosphodiesterase 4D inhibitors. Bioorg Med Chem Lett. 2010 Sep 15;20(18):5502-5.
REF 14	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 15	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 16	Novel heterocyclic-fused pyridazinones as potent and selective phosphodiesterase IV inhibitors. J Med Chem. 1997 May 9;40(10):1417-21.
REF 17	Thalidomide analogs and PDE4 inhibition. Bioorg Med Chem Lett. 1998 Oct 6;8(19):2669-74.

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