Target Validation Information
TTD ID	T56367
Target Name	Phosphodiesterase 1 (PDE1)
Type of Target	Successful
Drug Potency against Target	Vinpocetine	Drug Info	IC50 = 15~30 uM	[4]
	BUFROLIN	Drug Info	IC50 = 16000 nM	[2]
	isobutylmethylxanthine	Drug Info	IC50 = 3400 nM	[2]
	ZAPRINAST	Drug Info	IC50 = 6000 nM	[1]
Action against Disease Model	Vinpocetine	Drug Info	HERG-Lite monitors the expression of hERG at the cell surface in two different stable mammalian cell lines. One cell line acts as a biosensor for drugs that inhibit hERG trafficking, while the other predicts hERG blockers based on their ability to act as pharmacological chaperones. In this study, we have validated the HERG-Lite assay using a panel of 100 drugs: 50 hERG blockers and 50 nonblockers.HERG-Lite correctly predicted hERG risk for all 100 test compounds with no false positives or negatives. All 50 hERG blockers were detected as drugs with hERG risk in the HERG-Lite assay, and fell into two classes: B (for blocker) and C (for complex; block and trafficking inhibition).IC50 on hERG: 32nM	[3]
References
REF 1	The next generation of phosphodiesterase inhibitors: structural clues to ligand and substrate selectivity of phosphodiesterases. J Med Chem. 2005 May 19;48(10):3449-62.
REF 2	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 3	HERG-Lite: a novel comprehensive high-throughput screen for drug-induced hERG risk. J Pharmacol Toxicol Methods. 2005 Jul-Aug;52(1):136-45.
REF 4	Vinpocetine inhibits NF-kappaB-dependent inflammation via an IKK-dependent but PDE-independent mechanism. Proc Natl Acad Sci U S A. 2010 May 25;107(21):9795-800.

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