Target Validation Information
TTD ID	T02001
Target Name	Phosphodiesterase 4D (PDE4D)
Type of Target	Successful
Drug Potency against Target	1-Butyl-3-methyl-3,7-dihydro-purine-2,6-dione	Drug Info	Ki = 19100 nM	[4]
	1-Methyl-3-propyl-3,7-dihydro-purine-2,6-dione	Drug Info	Ki = 10600 nM	[4]
	CC-1088	Drug Info	IC50 = 1100 nM	[13]
	CDP840	Drug Info	IC50 = 14 nM	[7]
	CI-1018	Drug Info	IC50 = 1100 nM	[5]
	DENBUFYLLINE	Drug Info	IC50 = 170 nM	[1]
	isobutylmethylxanthine	Drug Info	IC50 = 6900 nM	[12]
	L-454560	Drug Info	IC50 = 1.2 nM	[11]
	L-869298	Drug Info	IC50 = 0.4 nM	[9]
	Ro 20-1724	Drug Info	IC50 = 9100 nM	[12]
	ROLIPRAM	Drug Info	IC50 = 550 nM	[10]
	SCH-351591	Drug Info	IC50 = 60 nM	[3]
	SCH-351591	Drug Info	IC50 = 51 nM	[2]
	UCB-101333-3	Drug Info	IC50 = 630 nM	[8]
	ZAPRINAST	Drug Info	Ki = 8760 nM	[6]
	ZARDAVERINE	Drug Info	IC50 = 390 nM	[10]
References
REF 1	Pyrazolopyrimidine-2,4-dione sulfonamides: novel and selective calcitonin inducers. J Med Chem. 2002 May 23;45(11):2342-5.
REF 2	8-Methoxyquinolines as PDE4 inhibitors. Bioorg Med Chem Lett. 2002 Jun 17;12(12):1617-9.
REF 3	Synthesis and profile of SCH351591, a novel PDE4 inhibitor. Bioorg Med Chem Lett. 2002 Jun 17;12(12):1621-3.
REF 4	Effects of alkyl substitutions of xanthine skeleton on bronchodilation. J Med Chem. 1992 Oct 30;35(22):4039-44.
REF 5	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 6	8-Substituted analogues of 3-(3-cyclopentyloxy-4-methoxy-benzyl)-8-isopropyl-adenine: highly potent and selective PDE4 inhibitors. J Med Chem. 2005 Feb 24;48(4):1237-43.
REF 7	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 8	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 9	Enantiomer discrimination illustrated by the high resolution crystal structures of type 4 phosphodiesterase. J Med Chem. 2006 Mar 23;49(6):1867-73.
REF 10	In silico search for multi-target anti-inflammatories in Chinese herbs and formulas. Bioorg Med Chem. 2010 Mar 15;18(6):2204-2218.
REF 11	The discovery and synthesis of highly potent subtype selective phosphodiesterase 4D inhibitors. Bioorg Med Chem Lett. 2010 Sep 15;20(18):5502-5.
REF 12	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 13	Thalidomide analogs and PDE4 inhibition. Bioorg Med Chem Lett. 1998 Oct 6;8(19):2669-74.

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