Target Validation Information
Target ID T78581
Target Name Galanin receptor type 1
Target Type
Research
Drug Potency against Target GalB2 Drug Info Ki = 3.5 nM [530680]
[Sar1Ala]GAL-B2 Drug Info Ki = 11 nM [530680]
[Sar1Gly]GAL-B2 Drug Info Ki = 2.8 nM [530680]
(Sar)WTLNSAGYLLGPKK(Lys-myristoyl)K Drug Info Ki = 2.6 nM [529952]
(Sar)WTLNSAGYLLGPKK(Lys-palmitoyl)K Drug Info Ki = 3.5 nM [529952]
(Sar)WTLNSAGYLLGPKKKK Drug Info Ki = 0.4 nM [529952]
GWTLNSAGYLLGPPPALALA-CONH2 Drug Info Ki = 0.1 nM [530680]
GWTLNSAGYLLGPRHYINLITRQRY-CONH2 Drug Info Ki = 0.3 nM [530680]
GWTLNSAGYLLGPHAV-NH2 Drug Info Ki = 0.5 nM [529837]
WTLNSAGYLLGPHAVGNHPSFSDKNGLTS-CONH2 Drug Info Ki = 51 nM [530680]
[N-Ac,des-Sar]Gal-B2 Drug Info Ki = 1.7 nM [530680]
[N-Me,des-Sar]Gal-B2 Drug Info Ki = 364.5 nM [530680]
WTLNSAGYLL-CONH2 Drug Info Ki = 870 nM [530680]
(Sar)WTLNSAGYLLGPKK(Lys-stearoyl)K Drug Info Ki = 4 nM [529952]
(Sar)WTLNSAGYLLGPKK(Lys-octanoyl)K Drug Info Ki = 0.7 nM [529952]
(Sar)WTLNSAGYLLGPKK(Lys-decanoyl)K Drug Info Ki = 1.3 nM [529952]
GwTLNSAGYLLGPHAVGNHRSFSDKNGLTS-CONH2 Drug Info Ki = 545 nM [530680]
(Sar)WTLNSAGYLLGPKK(Lys-lauroyl)K Drug Info Ki = 1.4 nM [529952]
Gal-B5 Drug Info Ki = 387 nM [530680]
(Sar)WTLNSAGYLLGPKK(Lys-MPEG4)K Drug Info Ki = 0.5 nM [529952]
GALANIN Drug Info Ki = 0.35 nM [529789]
References
Ref 530680J Med Chem. 2010 Feb 25;53(4):1871-5.Engineering galanin analogues that discriminate between GalR1 and GalR2 receptor subtypes and exhibit anticonvulsant activity following systemic delivery.
Ref 530680J Med Chem. 2010 Feb 25;53(4):1871-5.Engineering galanin analogues that discriminate between GalR1 and GalR2 receptor subtypes and exhibit anticonvulsant activity following systemic delivery.
Ref 530680J Med Chem. 2010 Feb 25;53(4):1871-5.Engineering galanin analogues that discriminate between GalR1 and GalR2 receptor subtypes and exhibit anticonvulsant activity following systemic delivery.
Ref 529952J Med Chem. 2009 Mar 12;52(5):1310-6.Structural requirements for a lipoamino acid in modulating the anticonvulsant activities of systemically active galanin analogues.
Ref 529952J Med Chem. 2009 Mar 12;52(5):1310-6.Structural requirements for a lipoamino acid in modulating the anticonvulsant activities of systemically active galanin analogues.
Ref 529952J Med Chem. 2009 Mar 12;52(5):1310-6.Structural requirements for a lipoamino acid in modulating the anticonvulsant activities of systemically active galanin analogues.
Ref 530680J Med Chem. 2010 Feb 25;53(4):1871-5.Engineering galanin analogues that discriminate between GalR1 and GalR2 receptor subtypes and exhibit anticonvulsant activity following systemic delivery.
Ref 530680J Med Chem. 2010 Feb 25;53(4):1871-5.Engineering galanin analogues that discriminate between GalR1 and GalR2 receptor subtypes and exhibit anticonvulsant activity following systemic delivery.
Ref 529837J Med Chem. 2008 Dec 25;51(24):8038-47.Design, synthesis, and characterization of high-affinity, systemically-active galanin analogues with potent anticonvulsant activities.
Ref 530680J Med Chem. 2010 Feb 25;53(4):1871-5.Engineering galanin analogues that discriminate between GalR1 and GalR2 receptor subtypes and exhibit anticonvulsant activity following systemic delivery.
Ref 530680J Med Chem. 2010 Feb 25;53(4):1871-5.Engineering galanin analogues that discriminate between GalR1 and GalR2 receptor subtypes and exhibit anticonvulsant activity following systemic delivery.
Ref 530680J Med Chem. 2010 Feb 25;53(4):1871-5.Engineering galanin analogues that discriminate between GalR1 and GalR2 receptor subtypes and exhibit anticonvulsant activity following systemic delivery.
Ref 530680J Med Chem. 2010 Feb 25;53(4):1871-5.Engineering galanin analogues that discriminate between GalR1 and GalR2 receptor subtypes and exhibit anticonvulsant activity following systemic delivery.
Ref 529952J Med Chem. 2009 Mar 12;52(5):1310-6.Structural requirements for a lipoamino acid in modulating the anticonvulsant activities of systemically active galanin analogues.
Ref 529952J Med Chem. 2009 Mar 12;52(5):1310-6.Structural requirements for a lipoamino acid in modulating the anticonvulsant activities of systemically active galanin analogues.
Ref 529952J Med Chem. 2009 Mar 12;52(5):1310-6.Structural requirements for a lipoamino acid in modulating the anticonvulsant activities of systemically active galanin analogues.
Ref 530680J Med Chem. 2010 Feb 25;53(4):1871-5.Engineering galanin analogues that discriminate between GalR1 and GalR2 receptor subtypes and exhibit anticonvulsant activity following systemic delivery.
Ref 529952J Med Chem. 2009 Mar 12;52(5):1310-6.Structural requirements for a lipoamino acid in modulating the anticonvulsant activities of systemically active galanin analogues.
Ref 530680J Med Chem. 2010 Feb 25;53(4):1871-5.Engineering galanin analogues that discriminate between GalR1 and GalR2 receptor subtypes and exhibit anticonvulsant activity following systemic delivery.
Ref 529952J Med Chem. 2009 Mar 12;52(5):1310-6.Structural requirements for a lipoamino acid in modulating the anticonvulsant activities of systemically active galanin analogues.
Ref 529789J Med Chem. 2008 Nov 27;51(22):7094-8.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 responses against carrageenan-induced hyperalgesia.

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