[3H]GABA [Ligand Id: 5410] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL96 (NSC-27418, Gamma-Aminobutyric Acid, .gamma.-aminobutyric acid, Aminobutyric acid)
  • BGT1/Betaine transporter in Human [ChEMBL: CHEMBL3715] [GtoPdb: 932] [UniProtKB: P48065]
  • This target only has 0 pki data point
1 CHEMBL96_lig_chart_1 Betaine transporter Human
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  • GABAA receptor α1 subunit/GABAA receptor β1 subunit/GABAA receptor β3 subunit/GABAA receptor α5 subunit/GABAA receptor α3 subunit/GABAA receptor α2 subunit/GABAA receptor β2 subunit/GABAA receptor α4 subunit/GABAA receptor α6 subunit/GABA-A receptor; agonist GABA site in Human [ChEMBL: CHEMBL2109244] [GtoPdb: 404410412408406405411407409] [UniProtKB: P14867P18505P28472P31644P34903P47869P47870P48169Q16445]
  • This target only has 0 pki data point
2 CHEMBL96_lig_chart_2 GABA-A receptor; agonist GABA site Human
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  • GABAA receptor α1 subunit/GABAA receptor β1 subunit/GABAA receptor γ2 subunit/GABA A receptor alpha-1/beta-1/gamma-2 in Human [ChEMBL: CHEMBL2111392] [GtoPdb: 404410414] [UniProtKB: P14867P18505P18507]
  • This target only has 0 pki data point
3 CHEMBL96_lig_chart_3 GABA A receptor alpha-1/beta-1/gamma-2 Human
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  • GABAA receptor α1 subunit/GABAA receptor γ2 subunit/GABAA receptor β2 subunit/GABA-A receptor; alpha-1/beta-2/gamma-2 in Human [ChEMBL: CHEMBL2095172] [GtoPdb: 404414411] [UniProtKB: P14867P18507P47870]
  • GABAA receptor γ2 subunit/GABAA receptor α1 subunit/GABAA receptor β2 subunit/GABA-A receptor; alpha-1/beta-2/gamma-2 in Rat [ChEMBL: CHEMBL2095167] [GtoPdb: 414404411] [UniProtKB: P18508P62813P63138]
  • This target only has 0 pki data point
4 CHEMBL96_lig_chart_4 GABA-A receptor; alpha-1/beta-2/gamma-2 HumanRat
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  • GABAA receptor α1 subunit/GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABA-A receptor; alpha-1/beta-3/gamma-2 in Human [ChEMBL: CHEMBL2094121] [GtoPdb: 404414412] [UniProtKB: P14867P18507P28472]
  • This target only has 0 pki data point
5 CHEMBL96_lig_chart_5 GABA-A receptor; alpha-1/beta-3/gamma-2 Human
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  • GABAA receptor γ2 subunit/GABAA receptor α2 subunit/GABAA receptor β2 subunit/GABA A receptor alpha-2/beta-2/gamma-2 in Human [ChEMBL: CHEMBL2111413] [GtoPdb: 414405411] [UniProtKB: P18507P47869P47870]
  • This target only has 0 pki data point
6 CHEMBL96_lig_chart_6 GABA A receptor alpha-2/beta-2/gamma-2 Human
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  • GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α2 subunit/GABA-A receptor; alpha-2/beta-3/gamma-2 in Human [ChEMBL: CHEMBL2094130] [GtoPdb: 414412405] [UniProtKB: P18507P28472P47869]
  • This target only has 0 pki data point
7 CHEMBL96_lig_chart_7 GABA-A receptor; alpha-2/beta-3/gamma-2 Human
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  • GABAA receptor γ2 subunit/GABAA receptor α3 subunit/GABAA receptor β2 subunit/GABA A receptor alpha-3/beta-2/gamma-2 in Human [ChEMBL: CHEMBL2111339] [GtoPdb: 414406411] [UniProtKB: P18507P34903P47870]
  • This target only has 0 pki data point
8 CHEMBL96_lig_chart_8 GABA A receptor alpha-3/beta-2/gamma-2 Human
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  • GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α3 subunit/GABA-A receptor; alpha-3/beta-3/gamma-2 in Human [ChEMBL: CHEMBL2094120] [GtoPdb: 414412406] [UniProtKB: P18507P28472P34903]
  • This target only has 0 pki data point
9 CHEMBL96_lig_chart_9 GABA-A receptor; alpha-3/beta-3/gamma-2 Human
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  • GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α4 subunit/GABA A receptor alpha-4/beta-3/gamma-2 in Human [ChEMBL: CHEMBL2111366] [GtoPdb: 414412407] [UniProtKB: P18507P28472P48169]
  • This target only has 0 pki data point
10 CHEMBL96_lig_chart_10 GABA A receptor alpha-4/beta-3/gamma-2 Human
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  • GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α5 subunit/GABA-A receptor; alpha-5/beta-3/gamma-2 in Human [ChEMBL: CHEMBL2094122] [GtoPdb: 414412408] [UniProtKB: P18507P28472P31644]
  • This target only has 0 pki data point
11 CHEMBL96_lig_chart_11 GABA-A receptor; alpha-5/beta-3/gamma-2 Human
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  • GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α6 subunit/GABA-A receptor; alpha-6/beta-3/gamma-2 in Human [ChEMBL: CHEMBL2095190] [GtoPdb: 414412409] [UniProtKB: P18507P28472Q16445]
  • This target only has 0 pki data point
12 CHEMBL96_lig_chart_12 GABA-A receptor; alpha-6/beta-3/gamma-2 Human
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13 CHEMBL96_lig_chart_13 GABA-A receptor; anion channel HumanMouseRat
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14 CHEMBL96_lig_chart_14 GABA B receptor Rat
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15 CHEMBL96_lig_chart_15 GABA-B receptor Human
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  • GABAB1/GABA-B receptor 1 in Human [ChEMBL: CHEMBL2064] [GtoPdb: 240] [UniProtKB: Q9UBS5]
  • This target only has 0 pki data point
16 CHEMBL96_lig_chart_16 GABA-B receptor 1 Human
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  • GABAA receptor ρ3 subunit/GABAA receptor ρ1 subunit/GABAA receptor ρ2 subunit/GABA-C receptor in Human [ChEMBL: CHEMBL2109242] [GtoPdb: 422420421] [UniProtKB: A8MPY1P24046P28476]
  • This target only has 0 pki data point
17 CHEMBL96_lig_chart_17 GABA-C receptor Human
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  • GABAA receptor α1 subunit/GABA receptor alpha-1 subunit in Human [ChEMBL: CHEMBL1962] [GtoPdb: 404] [UniProtKB: P14867]
  • GABAA receptor α1 subunit/GABA receptor alpha-1 subunit in Rat [ChEMBL: CHEMBL343] [GtoPdb: 404] [UniProtKB: P62813]
  • This target only has 0 pki data point
18 CHEMBL96_lig_chart_18 GABA receptor alpha-1 subunit HumanRat
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  • GABAA receptor α2 subunit/GABA receptor alpha-2 subunit in Rat [ChEMBL: CHEMBL341] [GtoPdb: 405] [UniProtKB: P23576]
  • This target only has 0 pki data point
19 CHEMBL96_lig_chart_19 GABA receptor alpha-2 subunit Rat
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  • GABAA receptor γ1 subunit/GABA receptor gamma-1 subunit in Rat [ChEMBL: CHEMBL296] [GtoPdb: 413] [UniProtKB: P23574]
  • This target only has 0 pki data point
20 CHEMBL96_lig_chart_20 GABA receptor gamma-1 subunit Rat
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  • GABAA receptor ρ1 subunit/GABA receptor rho-1 subunit in Human [ChEMBL: CHEMBL3561] [GtoPdb: 420] [UniProtKB: P24046]
  • This target only has 0 pki data point
21 CHEMBL96_lig_chart_21 GABA receptor rho-1 subunit Human
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  • GAT1/GABA transporter 1 in Human [ChEMBL: CHEMBL1903] [GtoPdb: 929] [UniProtKB: P30531]
  • GAT1/GABA transporter 1 in Mouse [ChEMBL: CHEMBL5445] [GtoPdb: 929] [UniProtKB: P31648]
  • GAT1/GABA transporter 1 in Rat [ChEMBL: CHEMBL4054] [GtoPdb: 929] [UniProtKB: P23978]
  • This target only has 0 pki data point
22 CHEMBL96_lig_chart_22 GABA transporter 1 HumanMouseRat
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  • GAT2/GABA transporter 2 in Rat [ChEMBL: CHEMBL4889] [GtoPdb: 930] [UniProtKB: P31646]
  • This target only has 0 pki data point
23 CHEMBL96_lig_chart_23 GABA transporter 2 Rat
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  • GAT3/GABA transporter 3 in Human [ChEMBL: CHEMBL5208] [GtoPdb: 931] [UniProtKB: P48066]
  • GAT2/GABA transporter 3 in Mouse [ChEMBL: CHEMBL5205] [GtoPdb: 930] [UniProtKB: P31649]
  • This target only has 0 pki data point
24 CHEMBL96_lig_chart_24 GABA transporter 3 HumanMouse
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  • GAT3/GABA transporter 4 in Mouse [ChEMBL: CHEMBL3699] [GtoPdb: 931] [UniProtKB: P31650]
  • This target only has 0 pki data point
25 CHEMBL96_lig_chart_25 GABA transporter 4 Mouse
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  • GABAA receptor β3 subunit/GABAA receptor α3 subunit/Gamma-aminobutyric acid receptor subunit alpha-3/beta-3 in Human [ChEMBL: CHEMBL3885574] [GtoPdb: 412406] [UniProtKB: P28472P34903]
  • This target only has 0 pki data point
26 CHEMBL96_lig_chart_26 Gamma-aminobutyric acid receptor subunit alpha-3/beta-3 Human
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  • GABAA receptor β3 subunit/GABAA receptor α3 subunit/GABAA receptor θ subunit/Gamma-aminobutyric acid receptor subunit alpha-3/beta-3/theta in Human [ChEMBL: CHEMBL3885575] [GtoPdb: 412406418] [UniProtKB: P28472P34903Q9UN88]
  • This target only has 0 pki data point
27 CHEMBL96_lig_chart_27 Gamma-aminobutyric acid receptor subunit alpha-3/beta-3/theta Human
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  • Proton-coupled Amino acid Transporter 1/Proton-coupled amino acid transporter 1 in Human [ChEMBL: CHEMBL1914279] [GtoPdb: 1161] [UniProtKB: Q7Z2H8]
  • This target only has 1 pki data point
28 CHEMBL96_lig_chart_28 Proton-coupled amino acid transporter 1 Human
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
BGT1/Betaine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3715] [GtoPdb: 932] [UniProtKB: P48065]
ChEMBL Inhibition of human BGT1/human GAT3 chimera B expresses in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 4.41 pIC50 39000 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human GABA transporter (hBGT-1) activity. B 4.44 pIC50 36000 nM IC50 J. Med. Chem. (1994) 37: 2334-2342 [PMID:8057281]
ChEMBL Inhibition of human BGT1/human GAT3 chimera B expresses in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 4.56 pIC50 27542.29 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human BGT1 expresses in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 4.6 pIC50 25000 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human BGT1 expresses in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 4.75 pIC50 17782.79 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human BGT1/human GAT3 chimera D expresses in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 5.05 pIC50 9000 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of human BGT1/human GAT3 chimera D expresses in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 5.41 pIC50 3890.45 nM IC50 J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
GABAA receptor α1 subunit/GABAA receptor β1 subunit/GABAA receptor β3 subunit/GABAA receptor α5 subunit/GABAA receptor α3 subunit/GABAA receptor α2 subunit/GABAA receptor β2 subunit/GABAA receptor α4 subunit/GABAA receptor α6 subunit/GABA-A receptor; agonist GABA site in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2109244] [GtoPdb: 404410412408406405411407409] [UniProtKB: P14867P18505P28472P31644P34903P47869P47870P48169Q16445]
ChEMBL Agonist activity at human alpha-1-beta-2-gamma-2L GABAA receptor expressed in Xenopus oocytes assessed as inhibition of current production by two electrode voltage clamp method F 4.68 pEC50 21100 nM EC50 J. Med. Chem. (2008) 51: 3825-3840 [PMID:18528996]
ChEMBL Agonist activity at GABAA receptor (unknown origin) B 4.78 pEC50 16500 nM EC50 ACS Med. Chem. Lett. (2013) 4: 402-407 [PMID:24900684]
ChEMBL Agonist activity at human alpha1beta2gamma2L GABAA receptor expressed in Xenopus oocytes assessed as potentiation of channel current response by two-electrode voltage clamp electrophysiology assay F 6 pEC50 990 nM EC50 J. Med. Chem. (2011) 54: 8124-8135 [PMID:22029276]
GABAA receptor α1 subunit/GABAA receptor β1 subunit/GABAA receptor γ2 subunit/GABA A receptor alpha-1/beta-1/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111392] [GtoPdb: 404410414] [UniProtKB: P14867P18505P18507]
ChEMBL Agonist activity at GABA alpha-1-beta-2-gamma-2 receptor expressed in HEK293 cells by Whole-cell patch-clamp technique F 4.37 pEC50 43000 nM EC50 J. Med. Chem. (2007) 50: 4147-4161 [PMID:17655213]
ChEMBL Agonist activity at GABA alpha-1-beta-2-gamma-2 receptor expressed in HEK293 cells by Whole-cell patch-clamp technique F 4.37 pEC50 42657.95 nM EC50 J. Med. Chem. (2007) 50: 4147-4161 [PMID:17655213]
GABAA receptor α1 subunit/GABAA receptor γ2 subunit/GABAA receptor β2 subunit/GABA-A receptor; alpha-1/beta-2/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095172] [GtoPdb: 404414411] [UniProtKB: P14867P18507P47870]
ChEMBL Activity at human GABAA alpha-1-beta-2-gamma-2 LS327A receptor in HEK293 cells expressing as-PKCepsilon assessed as evoked current response by whole cell patch clamp method B 1.52 pEC50 1.52 - logEC50 J. Biol. Chem. (2007) 282: 33052-33063 [PMID:17875639]
ChEMBL Activity at human GABAA alpha-1-beta-2-gamma-2 LS327A,S343A receptor in HEK293 cells expressing as-PKCepsilon assessed as evoked current response by whole cell patch clamp method B 1.56 pEC50 1.56 - logEC50 J. Biol. Chem. (2007) 282: 33052-33063 [PMID:17875639]
ChEMBL Partial agonist activity at GABAAalpha1beta2gamma2s receptor (unknown origin) expressed in Xenopus laevis oocytes assessed as induction of chloride current by two-microelectrode voltage-clamp method B 4.29 pEC50 51000 nM EC50 Bioorg. Med. Chem. (2015) 23: 6757-6762 [PMID:26410663]
ChEMBL Agonist activity at human GABAA alpha1beta2gamma2S receptor expressed in TSA201 cells after 1 min by FLIPR assay B 5.74 pEC50 1800 nM EC50 J. Med. Chem. (2013) 56: 993-1006 [PMID:23294161]
ChEMBL Agonist activity at human GABAAalpha1beta2gamma2S receptor expressed in tsA-201cells by FLIPR membrane potential blue assay B 5.74 pEC50 1800 nM EC50 Eur. J. Med. Chem. (2014) 84: 404-416 [PMID:25038482]
ChEMBL Agonist activity at human GABAA alpha1beta2gamma2S receptor expressed in TSA201 cells after 1 min by FLIPR assay B 5.75 pEC50 1778.28 nM EC50 J. Med. Chem. (2013) 56: 993-1006 [PMID:23294161]
ChEMBL Agonist activity at human GABAAalpha1beta2gamma2S receptor expressed in tsA-201cells by FLIPR membrane potential blue assay B 5.75 pEC50 1778.28 nM EC50 Eur. J. Med. Chem. (2014) 84: 404-416 [PMID:25038482]
GABAA receptor γ2 subunit/GABAA receptor α1 subunit/GABAA receptor β2 subunit/GABA-A receptor; alpha-1/beta-2/gamma-2 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095167] [GtoPdb: 414404411] [UniProtKB: P18508P62813P63138]
ChEMBL Agonist activity at rat GABA-A alpha1beta2gamma2 receptor expressed in human TSA201 cells by whole cell voltage-clamp method B 5.64 pEC50 2300 nM EC50 J. Med. Chem. (2013) 56: 2456-2465 [PMID:23428109]
GABAA receptor α1 subunit/GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABA-A receptor; alpha-1/beta-3/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094121] [GtoPdb: 404414412] [UniProtKB: P14867P18507P28472]
ChEMBL Effective agonist dose for human Gamma-aminobutyric acid A receptor alpha-1-beta-3-gamma-2 expressed in Xenopus oocytes F 4.1 pEC50 80000 nM EC50 Bioorg. Med. Chem. Lett. (2001) 11: 1573-1577 [PMID:11412984]
GABAA receptor γ2 subunit/GABAA receptor α2 subunit/GABAA receptor β2 subunit/GABA A receptor alpha-2/beta-2/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111413] [GtoPdb: 414405411] [UniProtKB: P18507P47869P47870]
ChEMBL Agonist activity at human GABAA alpha2beta2gamma2S receptor expressed in TSA201 cells after 1 min by FLIPR assay B 6.18 pEC50 660.69 nM EC50 J. Med. Chem. (2013) 56: 993-1006 [PMID:23294161]
ChEMBL Agonist activity at human GABAAalpha2beta2gamma2S receptor expressed in tsA-201cells by FLIPR membrane potential blue assay B 6.18 pEC50 660.69 nM EC50 Eur. J. Med. Chem. (2014) 84: 404-416 [PMID:25038482]
ChEMBL Agonist activity at human GABAA alpha2beta2gamma2S receptor expressed in TSA201 cells after 1 min by FLIPR assay B 6.19 pEC50 650 nM EC50 J. Med. Chem. (2013) 56: 993-1006 [PMID:23294161]
ChEMBL Agonist activity at human GABAAalpha2beta2gamma2S receptor expressed in tsA-201cells by FLIPR membrane potential blue assay B 6.19 pEC50 650 nM EC50 Eur. J. Med. Chem. (2014) 84: 404-416 [PMID:25038482]
GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α2 subunit/GABA-A receptor; alpha-2/beta-3/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094130] [GtoPdb: 414412405] [UniProtKB: P18507P28472P47869]
ChEMBL Agonist activity on human Gamma-aminobutyric acid A receptor alpha-2-beta-3-gamma-2 expressed in Xenopus oocytes F 4.4 pEC50 40000 nM EC50 Bioorg. Med. Chem. Lett. (2001) 11: 1573-1577 [PMID:11412984]
GABAA receptor γ2 subunit/GABAA receptor α3 subunit/GABAA receptor β2 subunit/GABA A receptor alpha-3/beta-2/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111339] [GtoPdb: 414406411] [UniProtKB: P18507P34903P47870]
ChEMBL Agonist activity at human GABAA alpha3beta2gamma2S receptor expressed in TSA201 cells after 1 min by FLIPR assay B 6.04 pEC50 920 nM EC50 J. Med. Chem. (2013) 56: 993-1006 [PMID:23294161]
ChEMBL Agonist activity at human GABAAalpha3beta2gamma2S receptor expressed in tsA-201cells by FLIPR membrane potential blue assay B 6.04 pEC50 920 nM EC50 Eur. J. Med. Chem. (2014) 84: 404-416 [PMID:25038482]
ChEMBL Agonist activity at human GABAA alpha3beta2gamma2S receptor expressed in TSA201 cells after 1 min by FLIPR assay B 6.04 pEC50 912.01 nM EC50 J. Med. Chem. (2013) 56: 993-1006 [PMID:23294161]
ChEMBL Agonist activity at human GABAAalpha3beta2gamma2S receptor expressed in tsA-201cells by FLIPR membrane potential blue assay B 6.04 pEC50 912.01 nM EC50 Eur. J. Med. Chem. (2014) 84: 404-416 [PMID:25038482]
GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α3 subunit/GABA-A receptor; alpha-3/beta-3/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094120] [GtoPdb: 414412406] [UniProtKB: P18507P28472P34903]
ChEMBL Agonist activity on human Gamma-aminobutyric acid A receptor alpha-3-beta-3-gamma-2 expressed in Xenopus oocytes F 4.55 pEC50 28000 nM EC50 Bioorg. Med. Chem. Lett. (2001) 11: 1573-1577 [PMID:11412984]
GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α4 subunit/GABA A receptor alpha-4/beta-3/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111366] [GtoPdb: 414412407] [UniProtKB: P18507P28472P48169]
ChEMBL Effective agonist dose for human Gamma-aminobutyric acid A receptor alpha-4-beta-3-gamma-2 F 4.3 pEC50 50000 nM EC50 Bioorg. Med. Chem. Lett. (2001) 11: 1573-1577 [PMID:11412984]
GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α5 subunit/GABA-A receptor; alpha-5/beta-3/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094122] [GtoPdb: 414412408] [UniProtKB: P18507P28472P31644]
ChEMBL Effective agonist dose for human Gamma-aminobutyric acid A receptor alpha-5-beta-3-gamma-2 expressed in Xenopus oocytes F 5.52 pEC50 3000 nM EC50 Bioorg. Med. Chem. Lett. (2001) 11: 1573-1577 [PMID:11412984]
GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α6 subunit/GABA-A receptor; alpha-6/beta-3/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095190] [GtoPdb: 414412409] [UniProtKB: P18507P28472Q16445]
ChEMBL Effective agonist dose for human Gamma-aminobutyric acid A receptor alpha-6-beta-3-gamma-2 F 5.82 pEC50 1500 nM EC50 Bioorg. Med. Chem. Lett. (2001) 11: 1573-1577 [PMID:11412984]
GABAA receptor π subunit/GABAA receptor δ subunit/GABAA receptor α1 subunit/GABAA receptor β1 subunit/GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α5 subunit/GABAA receptor α3 subunit/GABAA receptor α2 subunit/GABAA receptor β2 subunit/GABAA receptor α4 subunit/GABAA receptor ε subunit/GABAA receptor α6 subunit/GABAA receptor γ1 subunit/GABAA receptor γ3 subunit/GABAA receptor θ subunit/GABA-A receptor; anion channel in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2093872] [GtoPdb: 419416404410414412408406405411407417409413415418] [UniProtKB: O00591O14764P14867P18505P18507P28472P31644P34903P47869P47870P48169P78334Q16445Q8N1C3Q99928Q9UN88]
ChEMBL Displacement of [3H]gamma-amino butyric acid from Gamma-aminobutyric acid (GABA-A) receptor of human cerebellar cortex preparation B 6.7 pKi 200 nM Ki J. Med. Chem. (1980) 23: 702-704 [PMID:7392039]
ChEMBL Displacement of [3H]muscimol from GABAA receptor in SPRD rat brain synaptic membranes by scintillation counting method B 7.48 pKi 33 nM Ki Eur. J. Med. Chem. (2014) 84: 404-416 [PMID:25038482]
ChEMBL Affinity for gamma-aminobutyric-acid A receptor measured by its ability to displace [3H]gabazine antagonist from rat brain preparations. F 5.84 pIC50 1450 nM IC50 J. Med. Chem. (1992) 35: 4092-4097 [PMID:1331456]
ChEMBL Binding affinity in vivo for gamma-aminobutyric-acid A receptor measured by its ability to displace [3H]-GABA agonist from rat brain preparations after iv injection. B 7.6 pIC50 25 nM IC50 J. Med. Chem. (1992) 35: 4092-4097 [PMID:1331456]
GABAA receptor α6 subunit/GABAA receptor γ2 subunit/GABAA receptor δ subunit/GABAA receptor α2 subunit/GABAA receptor α3 subunit/GABAA receptor γ3 subunit/GABAA receptor β1 subunit/GABAA receptor α1 subunit/GABAA receptor β3 subunit/GABAA receptor α5 subunit/GABAA receptor π subunit/GABAA receptor α4 subunit/GABAA receptor θ subunit/GABAA receptor γ1 subunit/GABA-A receptor; anion channel in Mouse (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094133] [GtoPdb: 409414416405406415410404412408419407418413] [UniProtKB: A2AMW3P16305P22723P22933P26048P26049P27681P50571P62812P63080Q8BHJ7Q8QZW7Q9D6F4Q9JLF1Q9R0Y8]
ChEMBL Activation of chloride ion uptake into mouse brain synaptoneurosomes F 4.84 pEC50 14300 nM EC50 Bioorg. Med. Chem. Lett. (2002) 12: 1985-1988 [PMID:12113824]
GABAA receptor π subunit/GABAA receptor β1 subunit/GABAA receptor δ subunit/GABAA receptor γ2 subunit/GABAA receptor α5 subunit/GABAA receptor α3 subunit/GABAA receptor γ1 subunit/GABAA receptor α2 subunit/GABAA receptor α4 subunit/GABAA receptor γ3 subunit/GABAA receptor α6 subunit/GABAA receptor α1 subunit/GABAA receptor β3 subunit/GABAA receptor β2 subunit/GABAA receptor ε subunit/GABA-A receptor; anion channel in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907607] [GtoPdb: 419410416414408406413405407415409404412411417] [UniProtKB: O09028P15431P18506P18508P19969P20236P23574P23576P28471P28473P30191P62813P63079P63138Q91ZM7Q9ES14]
ChEMBL Displacement of [3H]muscimol from GABAA receptor in rat brain synaptic membranes B 7.31 pKi 49 nM Ki J. Med. Chem. (2006) 49: 4442-4446 [PMID:16821803]
ChEMBL Displacement of [3H]gamma-amino butyric acid from Gamma-aminobutyric acid (GABA-A) receptor of rat ganglion neurons B 7.6 pKi 25 nM Ki J. Med. Chem. (1980) 23: 702-704 [PMID:7392039]
ChEMBL Inhibition of 2 nM [3H]muscimol binding to Gamma-aminobutyric acid (GABA-A) receptor in rat brain crude synaptic membranes B 4.3 pIC50 50000 nM IC50 J. Med. Chem. (1982) 25: 113-116 [PMID:6276545]
ChEMBL Inhibition of [3H]muscimol binding to GABA-A receptor from rat cortex B 6.89 pIC50 128 nM IC50 J. Med. Chem. (1995) 38: 3297-3312 [PMID:7650684]
ChEMBL Inhibition of [3H]muscimol binding to gamma-aminobutyric-acid A (GABA-A) receptor B 7 pIC50 100 nM IC50 J. Med. Chem. (1991) 34: 2557-2560 [PMID:1652022]
ChEMBL In vitro affinity for GABA binding sites on purified synaptic membranes from rat brain. B 7.48 pIC50 33 nM IC50 J. Med. Chem. (1983) 26: 895-900 [PMID:6304315]
ChEMBL Inhibition of [3H]GABA binding to Gamma-aminobutyric acid receptor of rat brain synaptosomal membranes B 7.48 pIC50 33 nM IC50 J. Med. Chem. (1982) 25: 1157-1162 [PMID:6292417]
ChEMBL In vitro binding affinity against Gamma-aminobutyric acid A receptor in rat brain synaptic membranes at pH 7.1 B 7.48 pIC50 33 nM IC50 J. Med. Chem. (1990) 33: 71-77 [PMID:2153214]
ChEMBL Inhibition of [3H]GABA binding to gamma-aminobutyric-acid A (GABA-A) receptor B 7.52 pIC50 30 nM IC50 J. Med. Chem. (1991) 34: 1307-1313 [PMID:1849996]
ChEMBL Displacement of [3H]GABA from Gamma-aminobutyric acid A receptor ofrat brain membranes B 7.52 pIC50 30 nM IC50 J. Med. Chem. (1987) 30: 743-746 [PMID:3031294]
ChEMBL Displacement of [3H]- muscimol from GABA-A receptor from rat cerebellum membrane at 0.022-0.039 uM B 7.54 pIC50 29 nM IC50 J. Med. Chem. (1985) 28: 653-660 [PMID:2985785]
ChEMBL In vitro inhibition of [3H]P4S binding to Gamma-aminobutyric acid receptor of rat brain synaptic membranes B 7.6 pIC50 25 nM IC50 J. Med. Chem. (1985) 28: 1612-1617 [PMID:2999396]
ChEMBL Displacement of [3H]muscimol from GABA-A receptor in Sprague-Dawley rat cerebral cortex B 7.62 pIC50 24 nM IC50 J. Med. Chem. (2006) 49: 5571-5577 [PMID:16942030]
ChEMBL Displacement of [3H]gamma-aminobutyric acid from sodium-independent Gamma-aminobutyric acid (GABA-A) receptor synaptic membrane binding sites from rat brain tissue B 7.7 pIC50 20 nM IC50 J. Med. Chem. (1980) 23: 1142-1144 [PMID:7420361]
ChEMBL Binding affinity against Gamma-aminobutyric acid A receptor in rat cerebral cortex B 7.74 pIC50 18 nM IC50 J. Med. Chem. (1995) 38: 3287-3296 [PMID:7650683]
ChEMBL Displacement of [3H]muscimol from GABA-A receptor in Sprague-Dawley rat spinal cord B 7.82 pIC50 15 nM IC50 J. Med. Chem. (2006) 49: 5571-5577 [PMID:16942030]
ChEMBL In vitro inhibition of [3H]THIP binding to Gamma-aminobutyric acid receptor in rat brain synaptic membranes B 7.82 pIC50 15 nM IC50 J. Med. Chem. (1985) 28: 1612-1617 [PMID:2999396]
ChEMBL Inhibition of [3H]GABA binding in GABAA receptor in rat brain synaptic membranes B 7.89 pIC50 13 nM IC50 J. Med. Chem. (2006) 49: 4442-4446 [PMID:16821803]
GABAB2/GABAB1/GABA B receptor in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111474] [GtoPdb: 241240] [UniProtKB: O88871Q9Z0U4]
ChEMBL In vitro displacement of [3H]GABA from Gamma-aminobutyric acid type B receptor sites in rat brain membranes B 7.22 pIC50 60 nM IC50 Bioorg. Med. Chem. Lett. (1993) 3: 515-518
ChEMBL Inhibition of [3H]baclofen binding to rat gamma-aminobutyric acid type B receptor. B 7.4 pIC50 40 nM IC50 J. Med. Chem. (1991) 34: 2557-2560 [PMID:1652022]
ChEMBL Displacement of [3H]baclofen from Gamma-aminobutyric acid type B receptor of rat brain membranes B 7.52 pIC50 30 nM IC50 J. Med. Chem. (1987) 30: 743-746 [PMID:3031294]
ChEMBL