Target Validation Information
TTD ID	T42446
Target Name	Gamma-aminobutyric acid B receptor (GABBR)
Type of Target	Successful
Drug Potency against Target	Baclofen	Drug Info	IC50 = 30 nM	[6]
	Gabapentin	Drug Info	IC50 = 140 nM	[5]
		Drug Info	IC50 = 2000 nM
	((E)-3-Amino-propenyl)-methyl-phosphinic acid	Drug Info	IC50 = 665 nM	[4]
	((Z)-3-Amino-propenyl)-methyl-phosphinic acid	Drug Info	IC50 = 16580 nM	[4]
	(3-Amino-1-ethyl-propyl)-methyl-phosphinic acid	Drug Info	IC50 = 18500 nM	[4]
	(3-Amino-1-hydroxy-propyl)-methyl-phosphinic acid	Drug Info	IC50 = 1160 nM	[4]
	(3-Amino-propyl)-hexyl-phosphinic acid	Drug Info	IC50 = 1000 nM
	(3-Amino-propyl)-hydroxymethyl-phosphinic acid	Drug Info	IC50 = 1050 nM	[4]
	(R)-5-Amino-3-(4-chloro-phenyl)-pentanoic acid	Drug Info	IC50 = 7400 nM	[1]
	3-ammoniopropane-1-sulfinate	Drug Info	IC50 = 60 nM
	4-Amino-3-(2-chloro-phenyl)-butyric acid	Drug Info	IC50 = 800 nM	[2]
	4-Amino-3-(4-fluoro-phenyl)-butyric acid	Drug Info	IC50 = 1330 nM	[2]
	4-Amino-3-(5-bromo-thiophen-2-yl)-butyric acid	Drug Info	IC50 = 1860 nM	[2]
	4-Amino-3-(5-chloro-thiophen-2-yl)-butyric acid	Drug Info	IC50 = 610 nM	[2]
	4-Amino-3-(5-methyl-thiophen-2-yl)-butyric acid	Drug Info	IC50 = 1340 nM	[2]
	4-Amino-3-benzofuran-2-yl-butyric acid	Drug Info	IC50 = 18000 nM	[3]
	4-Amino-3-thiophen-2-yl-butyric acid	Drug Info	IC50 = 9720 nM	[2]
	Baclofen	Drug Info	IC50 = 140 nM	[1]
	CGP 47656	Drug Info	IC50 = 89 nM	[4]
	CGP-34938	Drug Info	IC50 = 77 nM	[4]
	CGP-35024	Drug Info	IC50 = 1 nM
	CGP-35348	Drug Info	IC50 = 2500 nM
	CGP-35582	Drug Info	IC50 = 140 nM	[4]
	CGP-36216	Drug Info	IC50 = 3000 nM
	GSK683699	Drug Info	IC50 = 40 nM	[2]
	[3H]CGP27492	Drug Info	IC50 = 3 nM
References
REF 1	Synthesis and pharmacology of the baclofen homologues 5-amino-4-(4-chlorophenyl)pentanoic acid and the R- and S-enantiomers of 5-amino-3-(4-chlorop... J Med Chem. 1999 Jun 3;42(11):2053-9.
REF 2	3-Thienyl- and 3-furylaminobutyric acids. Synthesis and binding GABAB receptor studies. J Med Chem. 1991 Aug;34(8):2557-60.
REF 3	Synthesis and pharmacological evaluation of gamma-aminobutyric acid analogues. New ligand for GABAB sites. J Med Chem. 1987 Apr;30(4):743-6.
REF 4	Phosphinic acid analogues of GABA. 1. New potent and selective GABAB agonists. J Med Chem. 1995 Aug 18;38(17):3297-312.
REF 5	Synthesis and biological evaluation of conformationally restricted Gabapentin analogues. Bioorg Med Chem Lett. 1999 Aug 16;9(16):2329-34.
REF 6	International Union of Pharmacology. XXXIII. Mammalian gamma-aminobutyric acid(B) receptors: structure and function. Pharmacol Rev. 2002 Jun;54(2):247-64.

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