[3H]Ro154513 [Ligand Id: 4365] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL6597 (Ro-154513)
  • 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]
  • 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: 414, 404, 411] [UniProtKB: P18508, P62813, P63138]
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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]
  • GABAA receptor γ2 subunit/GABAA receptor α3 subunit/GABAA receptor β2 subunit/GABA A receptor alpha-3/beta-2/gamma-2 in Rat [ChEMBL: CHEMBL2111343] [GtoPdb: 414, 406, 411] [UniProtKB: P18508, P20236, P63138]
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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]
  • GABAA receptor γ2 subunit/GABAA receptor α6 subunit/GABAA receptor β2 subunit/GABA A receptor alpha-6/beta-2/gamma-2 in Rat [ChEMBL: CHEMBL2111365] [GtoPdb: 414, 409, 411] [UniProtKB: P18508, P30191, P63138]
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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 α1 subunit/GABA receptor alpha-1 subunit in Human [ChEMBL: CHEMBL1962] [GtoPdb: 404] [UniProtKB: P14867]
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  • GABAA receptor α5 subunit/GABA receptor alpha-5 subunit in Human [ChEMBL: CHEMBL5112] [GtoPdb: 408] [UniProtKB: P31644]
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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 Displacement of [3H]Flunitrazepam from GABA-A receptor alpha-1-beta-2-gamma-2 subunits expressed in Sf9 cells B 7.82 pKi 15 nM Ki J Med Chem (1996) 39: 158-175 [PMID:8568803]
ChEMBL Binding affinity for human GABA-A receptor alpha-1-beta-2-gamma-2 expressed in L(tk-) cell membranes B 8.48 pKi 3.3 nM Ki J Med Chem (1996) 39: 1928-1934 [PMID:8627617]
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: 414, 404, 411] [UniProtKB: P18508, P62813, P63138]
ChEMBL Binding affinity for rat GABA-A receptor alpha-1-beta-2-gamma-2 subunits expressed in HEK293 cells B 7.82 pKi 15 nM Ki J Med Chem (1994) 37: 4576-4580 [PMID:7799410]
ChEMBL Binding affinity for mutant rat GABA-A receptor alpha-1-(arg)-beta-2-gamma-2 subunits expressed in HEK293 cells B 8.72 pKi 1.9 nM Ki J Med Chem (1994) 37: 4576-4580 [PMID:7799410]
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 In vitro binding affinity for human GABA-A receptor alpha-1-beta-3-gamma-2 subunits expressed in L(tk-) cell membranes B 7.48 pKi 33 nM Ki J Med Chem (2003) 46: 5567-5570 [PMID:14667209]
ChEMBL Binding affinity against alpha-1-beta-3-gamma-2 GABAA/BzR receptor subtype. B 8.48 pKi 3.3 nM Ki J Med Chem (1998) 41: 4130-4142 [PMID:9767648]
ChEMBL Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-1-beta-3-gamma-2 B 8.48 pKi 3.3 nM Ki J Med Chem (2000) 43: 71-95 [PMID:10633039]
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 8.59 pKi 2.6 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 8.59 pKi 2.6 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 8.59 pKi 2.6 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 8.59 pKi 2.6 nM Ki J Med Chem (2000) 43: 71-95 [PMID:10633039]
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 8.6 pKi 2.5 nM Ki J Med Chem (1996) 39: 1928-1934 [PMID:8627617]
GABAA receptor γ2 subunit/GABAA receptor α3 subunit/GABAA receptor β2 subunit/GABA A receptor alpha-3/beta-2/gamma-2 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111343] [GtoPdb: 414, 406, 411] [UniProtKB: P18508, P20236, P63138]
ChEMBL Binding affinity for rat GABA-A receptor alpha-3-beta-2-gamma-2 subunits expressed in HEK293 cells B 8.3 pKi 5 nM Ki J Med Chem (1994) 37: 4576-4580 [PMID:7799410]
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 8.6 pKi 2.5 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 8.6 pKi 2.5 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 In vitro binding affinity for human GABA-A receptor alpha-5-beta-3-gamma-2 subunits expressed in L(tk-) cell membranes B 9.52 pKi 0.3 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 9.52 pKi 0.3 nM Ki J Med Chem (2000) 43: 71-95 [PMID:10633039]
ChEMBL Binding affinity for Gamma-aminobutyric acid A receptor alpha-5-beta-3-gamma-2 B 9.57 pKi 0.27 nM Ki J Med Chem (1998) 41: 4130-4142 [PMID:9767648]
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 Displacement of [3H]Ro-154513 from GABA-A receptor alpha-6-beta-2-gamma-2 subunits expressed in Sf9 cells B 8.27 pKi 5.4 nM Ki J Med Chem (1996) 39: 158-175 [PMID:8568803]
ChEMBL Displacement of [3H]-Ro- 15-4513 from alpha-6-beta-2-gamma-2 GABA-A receptor subunits expressed in Sf9 cell membranes B 8.27 pKi 5.4 nM Ki J Med Chem (1994) 37: 758-768 [PMID:8145225]
ChEMBL Displacement of [3H]Ro-154513 from benzodiazepine binding site of GABAA alpha-6-beta-2-gamma-2 receptor expressed in HEK293T cells B 8.29 pKi 5.1 nM Ki J Med Chem (2008) 51: 7243-7252 [PMID:18973287]
ChEMBL Binding affinity for human GABA-A receptor alpha-6-beta-2-gamma-2 expressed in L(tk-) cell membranes B 8.42 pKi 3.8 nM Ki J Med Chem (1996) 39: 1928-1934 [PMID:8627617]
GABAA receptor γ2 subunit/GABAA receptor α6 subunit/GABAA receptor β2 subunit/GABA A receptor alpha-6/beta-2/gamma-2 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111365] [GtoPdb: 414, 409, 411] [UniProtKB: P18508, P30191, P63138]
ChEMBL Binding affinity for mutant rat GABA-A receptor alpha-6-(his,thr,gly,val)beta2gamma2 subunits expressed in HEK293 cells B 6.72 pKi 190 nM Ki J Med Chem (1994) 37: 4576-4580 [PMID:7799410]
ChEMBL Binding affinity for rat GABA-A receptor alpha-6-beta-2-gamma-2 subunits expressed in HEK293 cells B 8 pKi 10 nM Ki J Med Chem (1994) 37: 4576-4580 [PMID:7799410]
ChEMBL Binding affinity for mutant rat GABA-A receptor alpha-6-(his,thr,gly)beta2gamma2 subunits expressed in HEK293 cells B 8.1 pKi 8 nM Ki J Med Chem (1994) 37: 4576-4580 [PMID:7799410]
ChEMBL Binding affinity for mutant rat GABA-A receptor alpha-6-(his,thr)beta2gamma2 subunits expressed in HEK293 cells B 8.22 pKi 6 nM Ki J Med Chem (1994) 37: 4576-4580 [PMID:7799410]
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 8.42 pKi 3.8 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 8.42 pKi 3.8 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 8.42 pKi 3.8 nM Ki J Med Chem (2000) 43: 71-95 [PMID:10633039]
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 Displacement of [3H]flunitrazepam from diazepam-sensitive GABA-A benzodiazepine receptor of rat cerebellar membrane B 8.28 pKi 5.3 nM Ki J Med Chem (1993) 36: 479-490 [PMID:8386247]
ChEMBL Binding affinity for Diazepam-Sensitive fraction of GABA-A benzodiazepine receptors B 8.28 pKi 5.3 nM Ki J Med Chem (1993) 36: 1001-1006 [PMID:8386769]
ChEMBL Binding affinity for Diazepam sensitive (DS) isoform of the benzodiazepine (Bz) binding site on GABAA receptors B 8.28 pKi 5.3 nM Ki J Med Chem (1993) 36: 1820-1830 [PMID:8390574]
ChEMBL Binding affinity against Diazepam sensitive (DS) Gamma-aminobutyric acid A receptor in rat cerebellum. B 8.28 pKi 5.3 nM Ki J Med Chem (1995) 38: 1679-1688 [PMID:7752192]
ChEMBL Binding affinity for Diazepam insensitive (DI) isoform of the benzodiazepine (Bz) binding site on GABAA receptors B 8.51 pKi 3.1 nM Ki J Med Chem (1993) 36: 1820-1830 [PMID:8390574]
ChEMBL Binding affinity against Diazepam insensitive (DI) Gamma-aminobutyric acid A receptor B 8.51 pKi 3.1 nM Ki J Med Chem (1995) 38: 1679-1688 [PMID:7752192]
ChEMBL Displacement of [3H]flunitrazepam from diazepam-insensitive GABA-A benzodiazepine receptor of rat cerebellar membrane B 8.51 pKi 3.1 nM Ki J Med Chem (1993) 36: 479-490 [PMID:8386247]
ChEMBL Binding affinity for Diazepam-Insensitive fraction of GABA-A benzodiazepine receptors B 8.51 pKi 3.1 nM Ki J Med Chem (1993) 36: 1001-1006 [PMID:8386769]
GABAA receptor α1 subunit/GABA receptor alpha-1 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1962] [GtoPdb: 404] [UniProtKB: P14867]
ChEMBL Binding affinity to GABAA alpha-1-beta-2-gamma-2 receptor B 8.48 pKd 3.3 nM Kd J Med Chem (2008) 51: 3788-3803 [PMID:18537233]
ChEMBL Activity at rat wild type GABAA alpha-1-beta-2-gamma-2 receptor expressed in xenopus oocytes assessed as GABA-elicited response by two electrode voltage clamp method relative to control B 8.96 pEC50 1.1 nM EC50 J Biol Chem (2007) 282: 26316-26325 [PMID:17626010]
GABAA receptor α5 subunit/GABA receptor alpha-5 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5112] [GtoPdb: 408] [UniProtKB: P31644]
ChEMBL Binding affinity to GABAA alpha-5-beta-2-gamma-2 receptor B 8.42 pKd 3.8 nM Kd J Med Chem (2008) 51: 3788-3803 [PMID:18537233]
ChEMBL Displacement of [3H]Ro-151788 from benzodiazepine binding site of GABAA alpha-5-beta-2-gamma-2 receptor expressed in HEK293T cells B 8.51 pKi 3.1 nM Ki J Med Chem (2008) 51: 7243-7252 [PMID:18973287]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]