RY024 [Ligand Id: 4301] 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: CHEMBL58757
  • 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]
  • This target only has 1 pki data point
  • 7.57
1 CHEMBL58757_lig_chart_1 GABA-A receptor; alpha-1/beta-2/gamma-2 Human
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]
  • 7.57
2 CHEMBL58757_lig_chart_2 GABA-A receptor; alpha-1/beta-3/gamma-2 Human
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]
  • This target only has 1 pki data point
  • 7.58
3 CHEMBL58757_lig_chart_3 GABA A receptor alpha-2/beta-2/gamma-2 Human
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]
  • 7.58
4 CHEMBL58757_lig_chart_4 GABA-A receptor; alpha-2/beta-3/gamma-2 Human
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]
  • This target only has 1 pki data point
  • 7.73
5 CHEMBL58757_lig_chart_5 GABA A receptor alpha-3/beta-2/gamma-2 Human
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]
  • 7.73
6 CHEMBL58757_lig_chart_6 GABA-A receptor; alpha-3/beta-3/gamma-2 Human
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]
  • 9.4
7 CHEMBL58757_lig_chart_7 GABA-A receptor; alpha-5/beta-3/gamma-2 Human
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]
  • This target only has 1 pki data point
  • 8.29
8 CHEMBL58757_lig_chart_8 GABA A receptor alpha-6/beta-2/gamma-2 Human
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]
  • 8.29
9 CHEMBL58757_lig_chart_9 GABA-A receptor; alpha-6/beta-3/gamma-2 Human
There should be some charts here, you may need to enable JavaScript!
10 CHEMBL58757_lig_chart_10 GABA-A receptor; anion channel Rat
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]
  • This target only has 1 pki data point
  • 7.73
11 CHEMBL58757_lig_chart_11 GABA receptor alpha-3 subunit Human
There should be some charts here, you may need to enable JavaScript!
  • GABAA receptor α5 subunit/GABA receptor alpha-5 subunit in Rat [ChEMBL: CHEMBL300] [GtoPdb: 408] [UniProtKB: P19969]
  • This target only has 0 pki data point
  • 0
12 CHEMBL58757_lig_chart_12 GABA receptor alpha-5 subunit Rat
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 7.57 pKi 26.9 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 7.57 pKi 26.9 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 7.57 pKi 26.9 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 7.57 pKi 26.9 nM Ki J. Med. Chem. (2000) 43: 71-95 [PMID:10633039]
ChEMBL Binding affinity to GABAA alpha-1-beta-3-gamma-2 receptor B 7.57 pKi 26.9 nM Ki J. Med. Chem. (2008) 51: 3788-3803 [PMID:18537233]
ChEMBL Activity at GABAA alpha-1-beta-3-gamma-2 receptor expressed in Xenopus oocytes assessed as inhibition of GABA-induced current by voltage clamp assay B 4.13 pEC50 74400 nM EC50 J. Med. Chem. (2008) 51: 3788-3803 [PMID:18537233]
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 7.58 pKi 26.3 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 7.58 pKi 26.3 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 7.58 pKi 26.3 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 7.58 pKi 26.3 nM Ki J. Med. Chem. (2000) 43: 71-95 [PMID:10633039]
ChEMBL Binding affinity to GABAA alpha-2-beta-3-gamma-2 receptor B 7.58 pKi 26.3 nM Ki J. Med. Chem. (2008) 51: 3788-3803 [PMID:18537233]
ChEMBL Activity at alpha-2-beta-3-gamma-2 GABAA receptor expressed in Xenopus oocytes assessed as inhibition in GABA-induced current by voltage clamp assay B 4.02 pEC50 95500 nM EC50 J. Med. Chem. (2008) 51: 3788-3803 [PMID:18537233]
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 7.73 pKi 18.7 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 7.73 pKi 18.7 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 7.73 pKi 18.7 nM Ki J. Med. Chem. (2000) 43: 71-95 [PMID:10633039]
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 9.4 pKi 0.4 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 9.4 pKi 0.4 nM Ki J. Med. Chem. (2003) 46: 5567-5570 [PMID:14667209]
ChEMBL Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-5-beta-3-gamma-2 B 9.4 pKi 0.4 nM Ki J. Med. Chem. (2000) 43: 71-95 [PMID:10633039]
ChEMBL Binding affinity to GABAA alpha-5-beta-3-gamma-2 receptor B 9.4 pKi 0.4 nM Ki J. Med. Chem. (2008) 51: 3788-3803 [PMID:18537233]
ChEMBL Activity at alpha-5-beta-3-gamma-2 GABAA receptor expressed in Xenopus oocytes assessed as inhibition in GABA-induced current by voltage clamp assay B 5.01 pEC50 9800 nM EC50 J. Med. Chem. (2008) 51: 3788-3803 [PMID:18537233]
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 8.29 pKi 5.1 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 8.29 pKi 5.1 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 8.29 pKi 5.1 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 8.29 pKi 5.1 nM Ki J. Med. Chem. (2000) 43: 71-95 [PMID:10633039]
ChEMBL Binding affinity to GABAA alpha-6-beta-3-gamma-2 receptor B 8.29 pKi 5.1 nM Ki J. Med. Chem. (2008) 51: 3788-3803 [PMID:18537233]
ChEMBL Activity at alpha-6-beta-3-gamma-2 GABAA receptor expressed in Xenopus oocytes assessed as inhibition in GABA-induced current by voltage clamp assay B 4.29 pEC50 51700 nM EC50 J. Med. Chem. (2008) 51: 3788-3803 [PMID:18537233]
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 Inhibition of [3H]flunitrazepam binding to low affinity GABA-A receptor of rat hippocampal membranes B 7.07 pIC50 85.6 nM IC50 J. Med. Chem. (1996) 39: 1928-1934 [PMID:8627617]
ChEMBL Inhibition of [3H]flunitrazepam binding to GABA-A receptor of rat cerebral membranes B 7.1 pIC50 79.8 nM IC50 J. Med. Chem. (1996) 39: 1928-1934 [PMID:8627617]
ChEMBL Inhibition of [3H]flunitrazepam binding to low affinity GABA-A receptor of rat hippocampal membranes B 7.15 pIC50 70.7 nM IC50 J. Med. Chem. (1996) 39: 1928-1934 [PMID:8627617]
GABAA receptor α3 subunit/GABA receptor alpha-3 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3026] [GtoPdb: 406] [UniProtKB: P34903]
ChEMBL Binding affinity to GABAA alpha-3-beta-3-gamma-2 receptor B 7.73 pKi 18.7 nM Ki J. Med. Chem. (2008) 51: 3788-3803 [PMID:18537233]
GABAA receptor α5 subunit/GABA receptor alpha-5 subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL300] [GtoPdb: 408] [UniProtKB: P19969]
ChEMBL Inhibition of [3H]flunitrazepam binding to alpha5 GABA-A receptor of rat hippocampal membranes B 7.17 pIC50 67.2 nM IC50 J. Med. Chem. (1996) 39: 1928-1934 [PMID:8627617]
ChEMBL Inhibition of [3H]flunitrazepam binding to high affinity GABA-A receptor of rat hippocampal membranes B 9.22 pIC50 0.6 nM IC50 J. Med. Chem. (1996) 39: 1928-1934 [PMID:8627617]
ChEMBL Inhibition of [3H]flunitrazepam binding to alpha-5 GABA-A receptor of rat hippocampal membranes B 9.48 pIC50 0.33 nM IC50 J. Med. Chem. (1996) 39: 1928-1934 [PMID:8627617]

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]