Target Validation Information
TTD ID	T93509
Target Name	Calcitonin gene-related peptide 1 (CALCA)
Type of Target	Clinical trial
Drug Potency against Target	Gamma Hydroxybutyric Acid	Drug Info	IC50 = 0.24 nM	[3]
	Ac-VTHRLAGLLSRSGGVVKNNFVPTDVGPFAF-NH2	Drug Info	IC50 = 1.74 nM	[1]
	Ac-VTHRLAGLLSRSGGVVRKNFVPTDVGPFAF-NH2	Drug Info	IC50 = 0.71 nM	[1]
	Ac-WVEHRLKGELSRKGGVV[hArg]KNFVPTDVGPFAF-NH2	Drug Info	IC50 = 1.02 nM	[1]
	Ac-WVTHQLAGLLSQSGGVVRKNFVPTDVGPFAF-NH2	Drug Info	IC50 = 0.53 nM	[1]
	Ac-WVTHRLAGLLSRSGGVVRKNFVPTDVGPFAF-NH2	Drug Info	IC50 = 0.2 nM	[1]
	Ac-WVTHRLAGLLS[Cit]SGGVVRKNFVPTDVGPFAF-NH2	Drug Info	IC50 = 0.58 nM	[1]
	Ac-WVTH[Cit]LAGLLSRSGGVVRKNFVPTDVGPFAF-NH2	Drug Info	IC50 = 0.57 nM	[1]
	Ac-WVTH[Cit]LAGLLS[Cit]SGGVVRKNFVPTDVGPFAF-NH2	Drug Info	IC50 = 8.9 nM	[1]
	Ac-WVTH[hArg]LAGLLS[hArg]SGGVVRKNFVPTDVGPFAF-NH2	Drug Info	IC50 = 20.4 nM	[1]
	FV-Aib-TDVGPFAF	Drug Info	IC50 = 740 nM	[1]
	VTHRLAGLLSRSGGVVKNNFVPTNVGSKAF-NH2	Drug Info	IC50 = 4.87 nM	[1]
	WVTHRLAGLLSRSGGVVKNNFVPTNVGSKAF-NH2	Drug Info	IC50 = 0.64 nM	[1]
Action against Disease Model	Olcegepant	Drug Info	In an in vivo model, BIBN4096BS in doses between 1 and 30 micrograms kg-1 (i.v.) inhibited the effects of CGRP, released by stimulation of the trigeminal ganglion, on facial blood flow in marmoset monkeys	[2]
References
REF 1	Identification of potent, selective, and metabolically stable peptide antagonists to the calcitonin gene-related peptide (CGRP) receptor. J Med Chem. 2008 Dec 25;51(24):7889-97.
REF 2	Pharmacological profile of BIBN4096BS, the first selective small molecule CGRP antagonist. Br J Pharmacol. 2000 Feb;129(3):420-3.
REF 3	Progress in developing cholecystokinin (CCK)/gastrin receptor ligands that have therapeutic potential. Curr Opin Pharmacol. 2007 Dec;7(6):583-92.

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