Target Validation Information
TTD ID	T56625
Target Name	Tripeptidyl-peptidase II (TPP2)
Type of Target	Discontinued
Drug Potency against Target	UCL-2000; butabindide	Drug Info	IC50 = 7 nM	[2]
	(2S)-aminobutyryl-(R)-pipecolinic acid amide	Drug Info	Ki = 12000 nM	[1]
	(2S)-aminobutyryl-L-prolinamide	Drug Info	Ki = 570 nM	[1]
	(2S)-aminobutyryl-L-proline (R)-sec-butylamide	Drug Info	Ki = 4500 nM	[1]
	(2S)-aminobutyryl-L-proline isobutylamide	Drug Info	Ki = 320 nM	[1]
	(2S)-aminobutyryl-L-proline n-butylamide	Drug Info	Ki = 80 nM	[1]
	(2S)-aminobutyryl-L-proline n-pentylamide	Drug Info	Ki = 270 nM	[1]
	(2S)-aminobutyryl-L-proline n-propylamide	Drug Info	Ki = 80 nM	[1]
	(2S)-aminobutyryl-L-proline-(2S)-methylbutylamide	Drug Info	Ki = 500 nM	[1]
	Alpha-methylalanyl-L-proline butylamide	Drug Info	Ki = 5000 nM	[1]
	L-isoleucyl-L-prolinamide	Drug Info	Ki = 4300 nM	[1]
	L-leucyl-L-prolinamide	Drug Info	Ki = 2100 nM	[1]
	L-norleucyl-L-prolinamide	Drug Info	Ki = 2000 nM	[1]
	L-norvalyl-L-prolinamide	Drug Info	Ki = 1600 nM	[1]
	L-valyl-L-prolinamide	Drug Info	Ki = 6000 nM	[1]
	L-valyl-L-proline benzylamide	Drug Info	Ki = 3300 nM	[1]
	L-valyl-L-proline hexylamide	Drug Info	Ki = 900 nM	[1]
References
REF 1	Inhibitors of tripeptidyl peptidase II. 3. Derivation of butabindide by successive structure optimizations leading to a potential general approach ... J Med Chem. 2005 Nov 17;48(23):7333-42.
REF 2	Design, synthesis, and tripeptidyl peptidase II inhibitory activity of a novel series of (S)-2,3-dihydro-2-(4-alkyl-1H-imidazol-2-yl)-1H-indoles. J Med Chem. 2002 Nov 21;45(24):5303-10.

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