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] |
| ChEMBL | Positive allosteric modulation of human GABAA alpha1beta2gamma2 receptor expressed in Xenopus laevis oocytes by two-microelectrode voltage-clamp assay | B | 6.7 | pEC50 | 200 | nM | EC50 | Bioorg Med Chem Lett (2018) 28: 61-70 [PMID:29223589] |
| 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] |
| GABAA receptor β1 subunit/GABAA receptor γ2 subunit/GABAA receptor α2 subunit/Gamma-aminobutyric acid receptor subunit alpha-2/beta-1/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL5291949] [GtoPdb: 410, 414, 405] [UniProtKB: P18505, P18507, P47869] | ||||||||
| ChEMBL | Positive allosteric modulation of human GABAA alpha2beta1gamma2 receptor expressed in Xenopus laevis oocytes by two-microelectrode voltage-clamp assay | B | 7 | pEC50 | 100 | nM | EC50 | Bioorg Med Chem Lett (2018) 28: 61-70 [PMID:29223589] |
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]
