Ro15-4513 [Ligand Id: 4296] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL6597 (Ro-154513) |
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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 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]
