[3H]RY80 [Ligand Id: 4364] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL286594 |
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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 | 7.55 | 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: 404, 414, 412] [UniProtKB: P14867, P18507, P28472] | ||||||||
| 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: 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 | 7.67 | 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: 414, 412, 405] [UniProtKB: P18507, P28472, P47869] | ||||||||
| 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: 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 | 7.59 | 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: 414, 412, 406] [UniProtKB: P18507, P28472, P34903] | ||||||||
| 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: 414, 412, 407] [UniProtKB: P18507, P28472, P48169] | ||||||||
| 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: 414, 412, 408] [UniProtKB: P18507, P28472, P31644] | ||||||||
| 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: 414, 412, 408] [UniProtKB: P18508, P63079, P19969] | ||||||||
| 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: 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 | 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: 414, 412, 409] [UniProtKB: P18507, P28472, Q16445] | ||||||||
| 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 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]
