Target Validation Information
TTD ID	T23714
Target Name	B2 bradykinin receptor (BDKRB2)
Type of Target	Successful
Drug Potency against Target	Icatibant	Drug Info	IC50 = 1~5 nM	[6]
	Labradimil	Drug Info	IC50 = 10 nM	[5]
	(D)Arg-Arg-Pro-Hyp-Gly-Phe-Ser-(d)Phe-Phe-Arg	Drug Info	Ki = 26.8 nM	[2]
	(D)Arg-Arg-Pro-Hyp-Gly-Thi-Cys-(D)Phe-Phe-Cys-Arg	Drug Info	Ki = 876 nM	[2]
	(D)Arg-Arg-Pro-Hyp-Gly-Thi-Ser-(D)Tic-Aoc-Arg	Drug Info	Ki = 0.176 nM	[2]
	(D)Arg-Arg-Pro-Hyp-Gly-Thi-Ser-(D)Tic-Tic-Arg	Drug Info	Ki = 0.381 nM	[2]
	BRADYKININ	Drug Info	Ki = 0.11 nM	[1]
	FR-173657	Drug Info	IC50 = 1.4 nM	[4]
	H-DArg-Arg-Pro-Hyp-Gly-Igl-Ser-D-BT-OH(JMV1638)	Drug Info	Ki = 325 nM	[1]
	H-Lys-Arg-Pro-Hyp-Gly-Igl-Ser-D-BT-OH(JMV1645)	Drug Info	Ki = 9.2 nM	[1]
	H-Lys-Arg-Pro-Hyp-Gly-Thi-Ser-D-BT-OH(JMV1669)	Drug Info	Ki = 0.4 nM	[1]
	JMV1431	Drug Info	Ki = 4.4 nM	[1]
	NPC-567	Drug Info	Ki = 20 nM	[3]
Action against Disease Model	Icatibant	Drug Info	ALX-0081 selectively targets platelet adhesion under conditions of arterial flow. Platelet adhesion was completely inhibited upon spiking of ~0.4 |?g/mL ALX-0081. ALX-0081 completely blocks ex vivo platelet adhesion in blood samples of patients undergoing a PCI. The effective ALX-0081 dose, ie the concentration of ALX-0081 resulting in less than 3% surface coverage, ranged from 0.2 |?g/mL to 0.8 |?g/mL and was correlated to the VWF levels in the patients???plasma. In all animals treated with ALX-0081 (n = 8), a strong antithrombotic effect was obtained	[7]
References
REF 1	Synthesis and biological evaluation of bradykinin B(1)/B(2) and selective B(1) receptor antagonists. J Med Chem. 2000 Jun 15;43(12):2382-6.
REF 2	Design and conformational analysis of several highly potent bradykinin receptor antagonists. J Med Chem. 1991 Mar;34(3):1230-3.
REF 3	cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain... J Med Chem. 2008 Nov 27;51(22):7094-8.
REF 4	Novel small molecule bradykinin B2 receptor antagonists. J Med Chem. 2009 Jul 23;52(14):4370-9.
REF 5	International union of pharmacology. XLV. Classification of the kinin receptor family: from molecular mechanisms to pathophysiological consequences. Pharmacol Rev. 2005 Mar;57(1):27-77.
REF 6	Therapeutic potential of icatibant (HOE-140, JE-049). Expert Opin Pharmacother. 2008 Sep;9(13):2383-90.
REF 7	Antithrombotic drug candidate ALX-0081 shows superior preclinical efficacy and safety compared with currently marketed antiplatelet drugs. Blood. 2011 Jul 21;118(3):757-65.

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