RY024 [Ligand Id: 4301] activity data from GtoPdb and ChEMBL

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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: 404, 414, 411] [UniProtKB: P14867, P18507, P47870]
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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: 404, 414, 412] [UniProtKB: P14867, P18507, P28472]
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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: 414, 405, 411] [UniProtKB: P18507, P47869, P47870]
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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: 414, 412, 405] [UniProtKB: P18507, P28472, P47869]
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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: 414, 406, 411] [UniProtKB: P18507, P34903, P47870]
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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: 414, 412, 406] [UniProtKB: P18507, P28472, P34903]
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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: 414, 412, 408] [UniProtKB: P18507, P28472, P31644]
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  • 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: 414, 411, 409] [UniProtKB: P18507, P47870, Q16445]
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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: 414, 412, 409] [UniProtKB: P18507, P28472, Q16445]
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  • GABAA receptor α3 subunit/GABA receptor alpha-3 subunit in Human [ChEMBL: CHEMBL3026] [GtoPdb: 406] [UniProtKB: P34903]
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  • GABAA receptor α5 subunit/GABA receptor alpha-5 subunit in Rat [ChEMBL: CHEMBL300] [GtoPdb: 408] [UniProtKB: P19969]
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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: 404, 414, 411] [UniProtKB: P14867, P18507, P47870]
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: 404, 414, 412] [UniProtKB: P14867, P18507, P28472]
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: 414, 405, 411] [UniProtKB: P18507, P47869, P47870]
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: 414, 412, 405] [UniProtKB: P18507, P28472, P47869]
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: 414, 406, 411] [UniProtKB: P18507, P34903, P47870]
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: 414, 412, 406] [UniProtKB: P18507, P28472, P34903]
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: 414, 412, 408] [UniProtKB: P18507, P28472, P31644]
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: 414, 411, 409] [UniProtKB: P18507, P47870, Q16445]
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: 414, 412, 409] [UniProtKB: P18507, P28472, Q16445]
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: 419, 410, 416, 414, 408, 406, 413, 405, 407, 415, 409, 404, 412, 411, 417] [UniProtKB: O09028, P15431, P18506, P18508, P19969, P20236, P23574, P23576, P28471, P28473, P30191, P62813, P63079, P63138, Q91ZM7, Q9ES14]
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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]