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: CHEMBL6597 (Ro-154513) |
---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
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: 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]