Target Validation Information
TTD ID	T83369
Target Name	Coagulation factor IX (F9)
Type of Target	Successful
Drug Potency against Target	TTP889	Drug Info	IC50 = 1500 nM	[3]
	4-Benzyloxybenzo[b]thiophene-2-carboxamidine	Drug Info	Ki = 1500 nM	[2]
	4-iodobenzo[b]thiophene 2-carboxamidine	Drug Info	Ki = 950 nM	[2]
	4-Phenyl-benzo[b]thiophene-2-carboxamidine	Drug Info	Ki = 1600 nM	[2]
	5-Benzyloxy-benzo[b]thiophene-2-carboxamidine	Drug Info	Ki = 1900 nM	[2]
	6-Benzyloxybenzo[b]thiophene-2-carboxamidine	Drug Info	Ki = 3800 nM	[2]
	RAZAXABAN	Drug Info	Ki = 9000 nM	[1]
Action against Disease Model	TTP889	Drug Info	In vitro models show dose-dependent inhibition of FIX/FIXa activity with TTP889 to a maxim uM of about 90% (IC50 ??? 1.5 |?m). TTP889 does not appear to accelerate clotting induced by exogenous FXIa or Fxa. The antithrombotic potential of TTP889 has been demonstrated in animal models of venous and arterial thrombosis by inhibiting clotting in two a/v shunt models without prolonging bleeding times	[3]
References
REF 1	Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors. Bioorg Med Chem Lett. 2006 Apr 1;16(7):1795-8.
REF 2	Studies of benzothiophene template as potent factor IXa (FIXa) inhibitors in thrombosis. J Med Chem. 2010 Feb 25;53(4):1465-72.
REF 3	Partial factor IXa inhibition with TTP889 for prevention of venous thromboembolism: an exploratory study. J Thromb Haemost. 2008 Mar;6(3):457-63.

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