Target Validation Information
TTD ID	T78581
Target Name	Galanin receptor type 1 (GAL1-R)
Type of Target	Literature-reported
Drug Potency against Target	(Sar)WTLNSAGYLLGPKK(Lys-decanoyl)K	Drug Info	Ki = 1.3 nM	[3]
	(Sar)WTLNSAGYLLGPKK(Lys-lauroyl)K	Drug Info	Ki = 1.4 nM	[3]
	(Sar)WTLNSAGYLLGPKK(Lys-MPEG4)K	Drug Info	Ki = 0.5 nM	[3]
	(Sar)WTLNSAGYLLGPKK(Lys-myristoyl)K	Drug Info	Ki = 2.6 nM	[3]
	(Sar)WTLNSAGYLLGPKK(Lys-octanoyl)K	Drug Info	Ki = 0.7 nM	[3]
	(Sar)WTLNSAGYLLGPKK(Lys-palmitoyl)K	Drug Info	Ki = 3.5 nM	[3]
	(Sar)WTLNSAGYLLGPKK(Lys-stearoyl)K	Drug Info	Ki = 4 nM	[3]
	(Sar)WTLNSAGYLLGPKKKK	Drug Info	Ki = 0.4 nM	[3]
	Gal-B5	Drug Info	Ki = 387 nM	[4]
	GALANIN	Drug Info	Ki = 0.35 nM	[1]
	GalB2	Drug Info	Ki = 3.5 nM	[4]
	GWTLNSAGYLLGPHAV-NH2	Drug Info	Ki = 0.5 nM	[2]
	GwTLNSAGYLLGPHAVGNHRSFSDKNGLTS-CONH2	Drug Info	Ki = 545 nM	[4]
	GWTLNSAGYLLGPPPALALA-CONH2	Drug Info	Ki = 0.1 nM	[4]
	GWTLNSAGYLLGPRHYINLITRQRY-CONH2	Drug Info	Ki = 0.3 nM	[4]
	WTLNSAGYLL-CONH2	Drug Info	Ki = 870 nM	[4]
	WTLNSAGYLLGPHAVGNHPSFSDKNGLTS-CONH2	Drug Info	Ki = 51 nM	[4]
	[N-Ac,des-Sar]Gal-B2	Drug Info	Ki = 1.7 nM	[4]
	[N-Me,des-Sar]Gal-B2	Drug Info	Ki = 364.5 nM	[4]
	[Sar1Ala]GAL-B2	Drug Info	Ki = 11 nM	[4]
	[Sar1Gly]GAL-B2	Drug Info	Ki = 2.8 nM	[4]
References
REF 1	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 2	Design, synthesis, and characterization of high-affinity, systemically-active galanin analogues with potent anticonvulsant activities. J Med Chem. 2008 Dec 25;51(24):8038-47.
REF 3	Structural requirements for a lipoamino acid in modulating the anticonvulsant activities of systemically active galanin analogues. J Med Chem. 2009 Mar 12;52(5):1310-6.
REF 4	Engineering galanin analogues that discriminate between GalR1 and GalR2 receptor subtypes and exhibit anticonvulsant activity following systemic de... J Med Chem. 2010 Feb 25;53(4):1871-5.

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