[3H]RY80 [Ligand Id: 4364] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL286594
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • 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]
  • GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α5 subunit in Rat [GtoPdb: 414412408] [UniProtKB: P18508P63079P19969]
There should be some charts here, you may need to enable JavaScript!
  • GABAA receptor γ2 subunit/GABAA receptor β2 subunit/GABAA receptor α6 subunit/GABA A receptor alpha-6/beta-2/gamma-2 in Human [ChEMBL: CHEMBL2111370] [GtoPdb: 414411409] [UniProtKB: P18507P47870Q16445]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • GABAA receptor α3 subunit/GABA receptor alpha-3 subunit in Human [ChEMBL: CHEMBL3026] [GtoPdb: 406] [UniProtKB: P34903]
There should be some charts here, you may need to enable JavaScript!
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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 Binding affinity for human GABA-A receptor alpha-1-beta-2-gamma-2 expressed in L(tk-) cell membranes B 7.55 pKi 28.4 nM Ki J. Med. Chem. (1996) 39: 1928-1934 [PMID:8627617]
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 Binding affinity against alpha-1-beta-3-gamma-2 GABAA/BzR receptor subtype. B 7.55 pKi 28.4 nM Ki J. Med. Chem. (1998) 41: 4130-4142 [PMID:9767648]
ChEMBL In vitro binding affinity for human GABA-A receptor alpha-1-beta-3-gamma-2 subunits expressed in L(tk-) cell membranes B 7.55 pKi 28.4 nM Ki J. Med. Chem. (2003) 46: 5567-5570 [PMID:14667209]
ChEMBL Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-1-beta-3-gamma-2 B 7.55 pKi 28.4 nM Ki J. Med. Chem. (2000) 43: 71-95 [PMID:10633039]
ChEMBL In vitro inhibition of [3H]-Ro- 15-1788 binding to human GABA-A receptor alpha-1-beta-3-gamma-2 subunits expressed in L(tk-)cells B 7.55 pKi 28.4 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 1465-1469 [PMID:15006383]
ChEMBL Displacement of [3H]flunitrazepam from human recombinant GABAA alpha-1-beta-3-gamma-2 receptor expressed in HEK293 cells B 7.55 pKi 28.4 nM Ki Bioorg. Med. Chem. (2008) 16: 8853-8862 [PMID:18790643]
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 Binding affinity for human GABA-A receptor alpha-2-beta-2-gamma-2 expressed in L(tk-) cell membranes B 7.67 pKi 21.4 nM Ki J. Med. Chem. (1996) 39: 1928-1934 [PMID:8627617]
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 Binding affinity tested against alpha-2-beta-3-gamma-2 GABAA/BzR receptor subtype. B 7.67 pKi 21.4 nM Ki J. Med. Chem. (1998) 41: 4130-4142 [PMID:9767648]
ChEMBL In vitro binding affinity for human GABA-A receptor alpha-2-beta-3-gamma-2 subunits expressed in L(tk-) cell membranes B 7.67 pKi 21.4 nM Ki J. Med. Chem. (2003) 46: 5567-5570 [PMID:14667209]
ChEMBL Binding affinity to human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-2-beta-3-gamma-2 B 7.67 pKi 21.4 nM Ki J. Med. Chem. (2000) 43: 71-95 [PMID:10633039]
ChEMBL In vitro inhibition of [3H]-Ro- 15-1788 binding to human GABA-A receptor alpha-2-beta-3-gamma-2 subunits expressed in L(tk-)cells B 7.67 pKi 21.4 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 1465-1469 [PMID:15006383]
ChEMBL Displacement of [3H]flunitrazepam from human recombinant GABAA alpha-2-beta-3-gamma-2 receptor expressed in HEK293 cells B 7.67 pKi 21.4 nM Ki Bioorg. Med. Chem. (2008) 16: 8853-8862 [PMID:18790643]
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 Binding affinity for human GABA-A receptor alpha-3-beta-2-gamma-2 expressed in L(tk-) cell membranes B 7.59 pKi 25.8 nM Ki J. Med. Chem. (1996) 39: 1928-1934 [PMID:8627617]
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 Binding affinity against alpha-3-beta-3-gamma-2 GABAA/BzR receptor subtype. B 7.59 pKi 25.8 nM Ki J. Med. Chem. (1998) 41: 4130-4142 [PMID:9767648]
ChEMBL Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-3-beta-3-gamma-2 B 7.59 pKi 25.8 nM Ki J. Med. Chem. (2000) 43: 71-95 [PMID:10633039]
ChEMBL In vitro inhibition of [3H]-Ro- 15-1788 binding to human GABA-A receptor alpha-3-beta-3-gamma-2 subunits expressed in L(tk-)cells B 7.59 pKi 25.8 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 1465-1469 [PMID:15006383]
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 In vitro binding affinity for human GABA-A receptor alpha-4-beta-3-gamma-2 subunits expressed in L(tk-) cell membranes B 7.28 pKi 53 nM Ki J. Med. Chem. (2003) 46: 5567-5570 [PMID:14667209]
ChEMBL In vitro inhibition of [3H]-Ro- 15-1788 binding to human GABA-A receptor alpha-4-beta-3-gamma-2 subunits expressed in L(tk-)cells B 7.28 pKi 53 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 1465-1469 [PMID:15006383]
ChEMBL Displacement of [3H]flunitrazepam from human recombinant GABAA alpha-4-beta-3-gamma-2 receptor expressed in HEK293 cells B 8.28 pKi 5.3 nM Ki Bioorg. Med. Chem. (2008) 16: 8853-8862 [PMID:18790643]
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 Binding affinity for Gamma-aminobutyric acid A receptor alpha-5-beta-3-gamma-2 B 9.31 pKi 0.49 nM Ki J. Med. Chem. (1998) 41: 4130-4142 [PMID:9767648]
ChEMBL In vitro binding affinity for human GABA-A receptor alpha-5-beta-3-gamma-2 subunits expressed in L(tk-) cell membranes B 9.31 pKi 0.49 nM Ki J. Med. Chem. (2003) 46: 5567-5570 [PMID:14667209]
ChEMBL Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-5-beta-3-gamma-2 B 9.31 pKi 0.49 nM Ki J. Med. Chem. (2000) 43: 71-95 [PMID:10633039]
ChEMBL In vitro inhibition of [3H]-Ro- 15-1788 binding to human GABA-A receptor alpha-5-beta-3-gamma-2 subunits expressed in L(tk-)cells B 9.31 pKi 0.49 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 1465-1469 [PMID:15006383]
ChEMBL Displacement of [3H]flunitrazepam from human recombinant GABAA alpha-5-beta-3-gamma-2 receptor expressed in HEK293 cells B 9.31 pKi 0.49 nM Ki Bioorg. Med. Chem. (2008) 16: 8853-8862 [PMID:18790643]
GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α5 subunit in Rat [GtoPdb: 414412408] [UniProtKB: P18508P63079P19969]
GtoPdb - - 9.2 pKd 0.7 nM Kd J Pharmacol Exp Ther (1997) 283: 488-93 [PMID:9353361]
GABAA receptor γ2 subunit/GABAA receptor β2 subunit/GABAA receptor α6 subunit/GABA A receptor alpha-6/beta-2/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111370] [GtoPdb: 414411409] [UniProtKB: P18507P47870Q16445]
ChEMBL Binding affinity for human GABA-A receptor alpha-6-beta-2-gamma-2 expressed in L(tk-) cell membranes B 7.54 pKi 28.8 nM Ki J. Med. Chem. (1996) 39: 1928-1934 [PMID:8627617]
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 Binding affinity against Gamma-aminobutyric acid A receptor alpha-6-beta-3-gamma-2 B 7.54 pKi 28.8 nM Ki J. Med. Chem. (1998) 41: 4130-4142 [PMID:9767648]
ChEMBL In vitro binding affinity for human GABA-A receptor alpha-6-beta-3-gamma-2 subunits expressed in L(tk-) cell membranes B 7.54 pKi 28.8 nM Ki J. Med. Chem. (2003) 46: 5567-5570 [PMID:14667209]
ChEMBL Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-6-beta-3-gamma-2 B 7.54 pKi 28.8 nM Ki J. Med. Chem. (2000) 43: 71-95 [PMID:10633039]
ChEMBL In vitro inhibition of [3H]-Ro- 15-1788 binding to human GABA-A receptor alpha-6-beta-3-gamma-2 subunits expressed in L(tk-)cells B 7.54 pKi 28.8 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 1465-1469 [PMID:15006383]
ChEMBL Displacement of [3H]flunitrazepam from human recombinant GABAA alpha-6-beta-3-gamma-2 receptor expressed in HEK293 cells B 7.54 pKi 28.8 nM Ki Bioorg. Med. Chem. (2008) 16: 8853-8862 [PMID:18790643]
GABAA receptor α3 subunit/GABA receptor alpha-3 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3026] [GtoPdb: 406] [UniProtKB: P34903]
ChEMBL Displacement of [3H]flunitrazepam from human recombinant GABAA alpha-3-beta-3-gamma-2 receptor expressed in HEK293 cells B 7.59 pKi 25.8 nM Ki Bioorg. Med. Chem. (2008) 16: 8853-8862 [PMID:18790643]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]