Target Validation Information
Target ID T42446
Target Name Gamma-aminobutyric acid B receptor
Target Type
Successful
Drug Potency against Target 3-Amino-propane-1-sulfonic acid Drug Info IC50 = 2000 nM
Baclofen Drug Info IC50 = 30 nM [552296]
4-Amino-3-benzofuran-2-yl-butyric acid Drug Info IC50 = 18000 nM [533413]
(3-Amino-propyl)-hexyl-phosphinic acid Drug Info IC50 = 1000 nM
(3-Amino-1-hydroxy-propyl)-methyl-phosphinic acid Drug Info IC50 = 1160 nM [533678]
CGP-35348 Drug Info IC50 = 2500 nM
4-Amino-3-(5-methyl-thiophen-2-yl)-butyric acid Drug Info IC50 = 1340 nM [528071]
4-Amino-3-(5-chloro-thiophen-2-yl)-butyric acid Drug Info IC50 = 610 nM [528071]
(3-Amino-propyl)-hydroxymethyl-phosphinic acid Drug Info IC50 = 1050 nM [533678]
CGP-27492 Drug Info IC50 = 3 nM
4-Amino-3-(2-chloro-phenyl)-butyric acid Drug Info IC50 = 800 nM [528071]
Gabapentin Drug Info IC50 = 140 nM [552201]
((Z)-3-Amino-propenyl)-methyl-phosphinic acid Drug Info IC50 = 16580 nM [533678]
(R)-4-Amino-3-(4-chloro-phenyl)-butyric acid Drug Info IC50 = 140 nM [525508]
(R)-5-Amino-3-(4-chloro-phenyl)-pentanoic acid Drug Info IC50 = 7400 nM [525508]
CGP-35024 Drug Info IC50 = 1 nM
CGP-36216 Drug Info IC50 = 3000 nM
3-ammoniopropane-1-sulfinate Drug Info IC50 = 60 nM
(3-Amino-1-ethyl-propyl)-methyl-phosphinic acid Drug Info IC50 = 18500 nM [533678]
4-Amino-3-(4-fluoro-phenyl)-butyric acid Drug Info IC50 = 1330 nM [528071]
4-Amino-3-thiophen-2-yl-butyric acid Drug Info IC50 = 9720 nM [528071]
CGP-34938 Drug Info IC50 = 77 nM [533678]
CGP-35582 Drug Info IC50 = 140 nM [533678]
(3-Amino-propyl)-difluoromethyl-phosphinic acid Drug Info IC50 = 89 nM [533678]
4-Amino-3-(5-bromo-thiophen-2-yl)-butyric acid Drug Info IC50 = 1860 nM [528071]
((E)-3-Amino-propenyl)-methyl-phosphinic acid Drug Info IC50 = 665 nM [533678]
GAMMA-AMINO-BUTANOIC ACID Drug Info IC50 = 40 nM [528071]
References
Ref 552296International Union of Pharmacology. XXXIII. Mammalian gamma-aminobutyric acid(B) receptors: structure and function. Pharmacol Rev. 2002 Jun;54(2):247-64.
Ref 533413J Med Chem. 1987 Apr;30(4):743-6.Synthesis and pharmacological evaluation of gamma-aminobutyric acid analogues. New ligand for GABAB sites.
Ref 533678J Med Chem. 1995 Aug 18;38(17):3297-312.Phosphinic acid analogues of GABA. 1. New potent and selective GABAB agonists.
Ref 528071J Med Chem. 1991 Aug;34(8):2557-60.3-Thienyl- and 3-furylaminobutyric acids. Synthesis and binding GABAB receptor studies.
Ref 528071J Med Chem. 1991 Aug;34(8):2557-60.3-Thienyl- and 3-furylaminobutyric acids. Synthesis and binding GABAB receptor studies.
Ref 533678J Med Chem. 1995 Aug 18;38(17):3297-312.Phosphinic acid analogues of GABA. 1. New potent and selective GABAB agonists.
Ref 528071J Med Chem. 1991 Aug;34(8):2557-60.3-Thienyl- and 3-furylaminobutyric acids. Synthesis and binding GABAB receptor studies.
Ref 552201Synthesis and biological evaluation of conformationally restricted Gabapentin analogues. Bioorg Med Chem Lett. 1999 Aug 16;9(16):2329-34.
Ref 533678J Med Chem. 1995 Aug 18;38(17):3297-312.Phosphinic acid analogues of GABA. 1. New potent and selective GABAB agonists.
Ref 525508J Med Chem. 1999 Jun 3;42(11):2053-9.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-chlorophenyl)pentanoicacid.
Ref 525508J Med Chem. 1999 Jun 3;42(11):2053-9.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-chlorophenyl)pentanoicacid.
Ref 533678J Med Chem. 1995 Aug 18;38(17):3297-312.Phosphinic acid analogues of GABA. 1. New potent and selective GABAB agonists.
Ref 528071J Med Chem. 1991 Aug;34(8):2557-60.3-Thienyl- and 3-furylaminobutyric acids. Synthesis and binding GABAB receptor studies.
Ref 528071J Med Chem. 1991 Aug;34(8):2557-60.3-Thienyl- and 3-furylaminobutyric acids. Synthesis and binding GABAB receptor studies.
Ref 533678J Med Chem. 1995 Aug 18;38(17):3297-312.Phosphinic acid analogues of GABA. 1. New potent and selective GABAB agonists.
Ref 533678J Med Chem. 1995 Aug 18;38(17):3297-312.Phosphinic acid analogues of GABA. 1. New potent and selective GABAB agonists.
Ref 533678J Med Chem. 1995 Aug 18;38(17):3297-312.Phosphinic acid analogues of GABA. 1. New potent and selective GABAB agonists.
Ref 528071J Med Chem. 1991 Aug;34(8):2557-60.3-Thienyl- and 3-furylaminobutyric acids. Synthesis and binding GABAB receptor studies.
Ref 533678J Med Chem. 1995 Aug 18;38(17):3297-312.Phosphinic acid analogues of GABA. 1. New potent and selective GABAB agonists.
Ref 528071J Med Chem. 1991 Aug;34(8):2557-60.3-Thienyl- and 3-furylaminobutyric acids. Synthesis and binding GABAB receptor studies.

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