ganaxolone [Ligand Id: 11942] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1568698 (CCD 1042, CCD-1042, DEA NO. 2401, Ganaxolone, Ztalmy) |
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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 β1 subunit/GABAA receptor β3 subunit/GABAA receptor α5 subunit/GABAA receptor α3 subunit/GABAA receptor α2 subunit/GABAA receptor β2 subunit/GABAA receptor α4 subunit/GABAA receptor α6 subunit/GABA-A receptor; agonist GABA site in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2109244] [GtoPdb: 404, 410, 412, 408, 406, 405, 411, 407, 409] [UniProtKB: P14867, P18505, P28472, P31644, P34903, P47869, P47870, P48169, Q16445] | ||||||||
| ChEMBL | Positive allosteric modulation of recombinant alpha1beta2gamma2 GABAA receptor (unknown origin) expressed in LTK cells assessed as potentiation of GABA-induced channel current treated for 30 s prior to GABA stimulation for 2s by Q-patch assay | B | 6.58 | pEC50 | 266 | nM | EC50 | J Med Chem (2015) 58: 3500-3511 [PMID:25799373] |
| GtoPdb | Potentiation of GABA-activated currents in Xenopus oocytes expressing cloned human α1/β2/γ2L subunits of GABAA receptor | - | 6.59 | pEC50 | 260 | nM | EC50 | J Med Chem (1997) 40: 61-72 [PMID:9016329] |
| ChEMBL | Positive allosteric modulation of recombinant alpha4beta3delta GABAA receptor (unknown origin) expressed in CHO cells assessed as potentiation of GABA-induced channel current treated for 30 s prior to GABA stimulation for 2s by manual patch assay | B | 6.99 | pEC50 | 103 | nM | EC50 | J Med Chem (2015) 58: 3500-3511 [PMID:25799373] |
| 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 | Potentiation of GABA-activated currents in Xenopus oocytes expressing cloned human alpha-1-beta-2-gamma-2L subunits of GABA-A receptor | F | 6.59 | pEC50 | 260 | nM | EC50 | J Med Chem (1997) 40: 61-72 [PMID:9016329] |
| GtoPdb | Potentiation of GABA-activated currents in Xenopus oocytes expressing cloned human α1/β2/γ2L subunits of GABAA receptor | - | 6.59 | pEC50 | 260 | nM | EC50 | J Med Chem (1997) 40: 61-72 [PMID:9016329] |
| GABAA receptor π subunit/GABAA receptor δ subunit/GABAA receptor α1 subunit/GABAA receptor β1 subunit/GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α5 subunit/GABAA receptor α3 subunit/GABAA receptor α2 subunit/GABAA receptor β2 subunit/GABAA receptor α4 subunit/GABAA receptor ε subunit/GABAA receptor α6 subunit/GABAA receptor γ1 subunit/GABAA receptor γ3 subunit/GABAA receptor θ subunit/GABA-A receptor; anion channel in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2093872] [GtoPdb: 419, 416, 404, 410, 414, 412, 408, 406, 405, 411, 407, 417, 409, 413, 415, 418] [UniProtKB: O00591, O14764, P14867, P18505, P18507, P28472, P31644, P34903, P47869, P47870, P48169, P78334, Q16445, Q8N1C3, Q99928, Q9UN88] | ||||||||
| ChEMBL | Displacement of [3H]TBPS from GABAA receptor in Sprague-Dawley rat brain cortical membrane after 90 mins by liquid scintillation spectrometry | B | 7.38 | pIC50 | 42 | nM | IC50 | J Med Chem (2015) 58: 3500-3511 [PMID:25799373] |
| GtoPdb | Potentiation of GABA-activated currents in Xenopus oocytes expressing cloned human α1/β2/γ2L subunits of GABAA receptor | - | 6.59 | pEC50 | 260 | nM | EC50 | J Med Chem (1997) 40: 61-72 [PMID:9016329] |
| 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 | Ability to allosterically modulate the binding of [35S]TBPS to gamma-aminobutyric-acid A receptor in rat brain cortical P2 membranes. | B | 7.1 | pIC50 | 80 | nM | IC50 | J Med Chem (1997) 40: 61-72 [PMID:9016329] |
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]
