Target Validation Information
TTD ID	T16308
Target Name	Rotamase Pin1 (PIN1)
Type of Target	Clinical trial
Drug Potency against Target	(R)-2-(2-naphthamido)-3-m-tolylpropanoic acid	Drug Info	Ki = 2800 nM	[2]
	(R)-2-(2-naphthamido)-3-p-tolylpropanoic acid	Drug Info	Ki = 17000 nM	[2]
	(R)-2-(2-naphthamido)-5-phenylpent-4-ynoic acid	Drug Info	Ki = 12800 nM	[2]
	(R)-3-(2-naphthamido)-4-m-tolylbutanoic acid	Drug Info	Ki = 9700 nM	[2]
	(R,)-2-(2-naphthamido)-5-phenylpent-4-enoic acid	Drug Info	Ki = 1800 nM	[2]
	Ac-Bth-Thr(PO3H2)-Pip-Nal-Gln-NH2	Drug Info	Ki = 258 nM	[1]
	Ac-Phe-D-Thr(PO3H2)-Pip-Nal-Gln-NH2	Drug Info	Ki = 18.3 nM	[1]
	Ac-Phe-Thr(PO3H2)-Pip-Nal-Gln-NH2	Drug Info	Ki = 547 nM	[1]
References
REF 1	Nanomolar inhibitors of the peptidyl prolyl cis/trans isomerase Pin1 from combinatorial peptide libraries. J Med Chem. 2006 Apr 6;49(7):2147-50.
REF 2	Structure-based design of novel human Pin1 inhibitors (II). Bioorg Med Chem Lett. 2010 Apr 1;20(7):2210-4.

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