Target Validation Information
TTD ID	T15334
Target Name	Cholesteryl ester transfer protein (CETP)
Type of Target	Clinical trial
Drug Potency against Target	Anacetrapib	Drug Info	IC50 = 16 nM	[3]
	Dalcetrapib	Drug Info	IC50 = 6 nM	[3]
	Torcetrapib	Drug Info	IC50 = 50 nM	[3]
	NSC-40331	Drug Info	IC50 = 6500 nM	[2]
	NSC-89508	Drug Info	IC50 = 1900 nM	[2]
	SC-795	Drug Info	IC50 = 20 nM	[2]
	TETRAHYDROQUINOLINE A	Drug Info	IC50 = 39 nM	[1]
Action against Disease Model	Dalcetrapib	Drug Info	The mechanism by which cholesteryl ester transfer protein (CETP) activity affects HDL metabolism was investigated using agents that selectively target CETP (dalcetrapib, torcetrapib, anacetrapib). In contrast with torcetrapib and anacetrapib, dalcetrapib requires cysteine 13 to decrease CETP activity, measured as transfer of cholesteryl ester (CE) from HDL to LDL, and does not affect transfer of CE from HDL3 to HDL2. Only dalcetrapib induced a conformational change in CETP, when added to h uMan plasma in vitro, also observed in vivo and correlated with CETP activity. CETP-induced pre-beta-HDL formation in vitro in h uMan plasma was unchanged by dalcetrapib ??? |?M and increased at 10 |?M.	[4]
References
REF 1	Design and synthesis of potent inhibitors of cholesteryl ester transfer protein (CETP) exploiting a 1,2,3,4-tetrahydroquinoline platform. Bioorg Med Chem Lett. 2009 May 1;19(9):2456-60.
REF 2	Discovery of new cholesteryl ester transfer protein inhibitors via ligand-based pharmacophore modeling and QSAR analysis followed by synthetic expl... Eur J Med Chem. 2010 Apr;45(4):1598-617.
REF 3	Cholesteryl ester transfer protein (CETP) inhibitors. Curr Top Med Chem. 2009;9(5):419-27.
REF 4	Modulating cholesteryl ester transfer protein activity maintains efficient pre--HDL formation and increases reverse cholesterol transport. J Lipid Res. 2010 Dec;51(12):3443-54.

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