Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T80387 Target Info
Target Name GABA(A) receptor beta-2 (GABRB2)
Synonyms
GABRB2; GABA(A) receptor subunit beta-2
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Target Type Successful Target
Gene Name GABRB2
Biochemical Class Neurotransmitter receptor
UniProt ID
GBRB2_HUMAN
Co-Targets of This Target  Top
Co-Target Name Gamma-aminobutyric acid B receptor (GABBR) Successful Target
UniProt ID GABR1_HUMAN; GABR2_HUMAN
Gene Name GABBR1; GABBR2
Synonyms
Gamma-aminobutyric acid type B receptor; GPRC3; GABABR; GABA-BR; GABA-B-R; GABA-B receptor
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Representative Drug(s) GSK683699 Drug Info IC50 = 25 nM [1]
Co-Target Name GABA transporter-3 (SLC6A11) Clinical trial Target
UniProt ID S6A11_HUMAN
Gene Name SLC6A11
Synonyms
Solute carrier family 6 member 11; Sodium- and chloride-dependent GABA transporter 3; GAT3; GAT-3; GABT3
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Representative Drug(s) GSK683699 Drug Info IC50 = 1000 nM [2]
Co-Target Name GABA(A) receptor rho1 (GABRR1) Literature-reported Target
UniProt ID GBRR1_HUMAN
Gene Name GABRR1
Synonyms
Gamma-aminobutyric acid receptor subunit rho-1; GABA(C) receptor1; GABA(A) receptor subunit rho-1
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Representative Drug(s) GSK683699 Drug Info EC50 = 269.15 nM [3]
Co-Target Name Na(+)/Cl(-) betaine/GABA transporter (SLC6A12) Literature-reported Target
UniProt ID S6A12_HUMAN
Gene Name SLC6A12
Synonyms
Solute carrier family 6 member 12; Sodium- and chloride-dependent betaine transporter; BGT-1
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Representative Drug(s) GSK683699 Drug Info IC50 = 851.14 nM [2]
Co-Target Name GABA A receptor alpha-1/beta-2/gamma-2 (GABRA1/GABRB2/GABRG2) Co-Target
UniProt ID GBRA1_HUMAN-GBRB2_HUMAN-GBRG2_HUMAN
Gene Name GABRA1-GABRB2-GABRG2
Representative Drug(s) ZK-93423 Drug Info Ki = 4.1 nM Click to Show More [4]
2 ZK-93423 Drug Info Ki = 4.1 nM [4]
Co-Target Name GABA A receptor alpha-2/beta-3/gamma-2 (GABRA2/GABRB3/GABRG2) Co-Target
UniProt ID GBRA2_HUMAN-GBRB3_HUMAN-GBRG2_HUMAN
Gene Name GABRA2-GABRB3-GABRG2
Representative Drug(s) ZK-93423 Drug Info Ki = 4.2 nM [4]
Co-Target Name GABA A receptor alpha-5/beta-3/gamma-2 (GABRA5/GABRB3/GABRG2) Co-Target
UniProt ID GBRA5_HUMAN-GBRB3_HUMAN-GBRG2_HUMAN
Gene Name GABRA5-GABRB3-GABRG2
Representative Drug(s) ZK-93423 Drug Info Ki = 4.5 nM [5]
Co-Target Name GABA A receptor alpha-3/beta-3/gamma-2 (GABRA3/GABRB3/GABRG2) Co-Target
UniProt ID GBRA3_HUMAN-GBRB3_HUMAN-GBRG2_HUMAN
Gene Name GABRA3-GABRB3-GABRG2
Representative Drug(s) ZK-93423 Drug Info Ki = 6 nM [4]
Co-Target Name GABA A receptor alpha-6/beta-3/gamma-2 (GABRA6/GABRB3/GABRG2) Co-Target
UniProt ID GBRA6_HUMAN-GBRB3_HUMAN-GBRG2_HUMAN
Gene Name GABRA6-GABRB3-GABRG2
Representative Drug(s) ZK-93423 Drug Info Ki ~ 1000 nM [5]
References  Top
REF 1 Phosphinic acid analogues of GABA. 1. New potent and selective GABAB agonists. J Med Chem. 1995 Aug 18;38(17):3297-312.
REF 2 Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/-Aminobutyric Acid Transporter 1 (BGT1). J Med Chem. 2017 Nov 9;60(21):8834-8846.
REF 3 Synthesis and biological evaluation of 4-(aminomethyl)-1-hydroxypyrazole analogues of muscimol as -aminobutyric acid(a) receptor agonists. J Med Chem. 2013 Feb 14;56(3):993-1006.
REF 4 Synthesis and evaluation of analogues of the partial agonist 6-(propyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (6-PBC) a... J Med Chem. 1998 Jul 2;41(14):2537-52.
REF 5 Pharmacophore/receptor models for GABA(A)/BzR subtypes (alpha1beta3gamma2, alpha5beta3gamma2, and alpha6beta3gamma2) via a comprehensive ligand-mapping approach. J Med Chem. 2000 Jan 13;43(1):71-95.

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