zuranolone [Ligand Id: 12858] activity data from GtoPdb and ChEMBL

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: CHEMBL4105630 (S-812217, Sage-217, SAGE-217, SGE-797, Zuranolone, Zurzuvae)
  • GABAA receptor α1 subunit/GABAA receptor γ2 subunit/GABAA receptor β2 subunit/GABA-A receptor; alpha-1/beta-2/gamma-2 in Human [ChEMBL: CHEMBL2095172] [GtoPdb: 404, 414, 411] [UniProtKB: P14867, P18507, P47870]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • GABAA receptor δ subunit/GABAA receptor β2 subunit/GABAA receptor α4 subunit/Gamma-aminobutyric acid receptor subunit alpha-4/beta-2/delta in Human [ChEMBL: CHEMBL4296046] [GtoPdb: 416, 411, 407] [UniProtKB: O14764, P47870, P48169]
There should be some charts here, you may need to enable JavaScript!
  • GABAA receptor δ subunit/GABAA receptor β3 subunit/GABAA receptor α4 subunit/Gamma-aminobutyric acid receptor subunit alpha-4/beta3/delta in Human [ChEMBL: CHEMBL3430899] [GtoPdb: 416, 412, 407] [UniProtKB: O14764, P28472, P48169]
There should be some charts here, you may need to enable JavaScript!
  • Kir2.1/Inward rectifier potassium channel 2 in Human [ChEMBL: CHEMBL1914276] [GtoPdb: 430] [UniProtKB: P63252]
There should be some charts here, you may need to enable JavaScript!
  • Kv4.3/Kv channel-interacting protein 2/Potassium voltage-gated channel subfamily D member 3 in Human [ChEMBL: CHEMBL3885598] [GtoPdb: 554] [UniProtKB: Q9NS61, Q9UK17]
There should be some charts here, you may need to enable JavaScript!
  • HCN2/Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 2 in Human [ChEMBL: CHEMBL1795172] [GtoPdb: 401] [UniProtKB: Q9UL51]
There should be some charts here, you may need to enable JavaScript!
  • Kv1.5/Potassium voltage-gated channel subfamily A member 5 in Human [ChEMBL: CHEMBL4306] [GtoPdb: 542] [UniProtKB: P22460]
There should be some charts here, you may need to enable JavaScript!
  • Nav1.5/Sodium channel protein type 5 subunit alpha in Human [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524]
There should be some charts here, you may need to enable JavaScript!
  • Cav1.2/Voltage-dependent L-type calcium channel subunit alpha-1C in Human [ChEMBL: CHEMBL1940] [GtoPdb: 529] [UniProtKB: Q13936]
There should be some charts here, you may need to enable JavaScript!
  • Kv11.1/Voltage-gated inwardly rectifying potassium channel KCNH2 in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
There should be some charts here, you may need to enable JavaScript!
  • Kv7.1/Voltage-gated potassium channel, IKs; KCNQ1(Kv7.1)/KCNE1(MinK) in Human [ChEMBL: CHEMBL2221347] [GtoPdb: 560] [UniProtKB: P15382, P51787]
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 Positive allosteric modulation of GABAA receptor alpha1beta2gamma2 (unknown origin) expressed in mouse LTK cells assessed as potentiation of GABA-mediated increase in channel current under holding potential at -80 mV preincubated for 30 secs followed by GABA stimulation for 2 secs by automated patch clamp assay B 6.43 pEC50 375 nM EC50 J Med Chem (2017) 60: 7810-7819 [PMID:28753313]
ChEMBL Positive allosteric modulation of GABAA receptor alpha1beta2gamma2 (unknown origin) B 6.43 pEC50 374 nM EC50 Bioorg Med Chem Lett (2017) 27: 3207-3218 [PMID:28606760]
ChEMBL Positive allosteric modulation of synaptic alpha1beta2gamma2 GABA-A receptor (unknown origin) transfected in LTK cells assessed as potentiation of GABA-induced peak current amplitude at -80 mV holding potential preincubated for 30 secs followed by GABA stimulation for 2 secs by Q-patch assay B 6.82 pEC50 152 nM EC50 Eur J Med Chem (2024) 276: 116602-116602 [PMID:38971049]
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 Inhibition of [35S]TBPS binding to GABA-A receptor in Sprague-Dawley rat brain cortical membrane incubated for 90 mins by liquid scintillation spectrometry B 8.15 pIC50 7 nM IC50 Eur J Med Chem (2024) 276: 116602-116602 [PMID:38971049]
GABAA receptor δ subunit/GABAA receptor β2 subunit/GABAA receptor α4 subunit/Gamma-aminobutyric acid receptor subunit alpha-4/beta-2/delta in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4296046] [GtoPdb: 416, 411, 407] [UniProtKB: O14764, P47870, P48169]
ChEMBL Positive allosteric modulation of GABAA receptor alpha4beta2delta (unknown origin) B 6.79 pEC50 163 nM EC50 Bioorg Med Chem Lett (2017) 27: 3207-3218 [PMID:28606760]
GABAA receptor δ subunit/GABAA receptor β3 subunit/GABAA receptor α4 subunit/Gamma-aminobutyric acid receptor subunit alpha-4/beta3/delta in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3430899] [GtoPdb: 416, 412, 407] [UniProtKB: O14764, P28472, P48169]
ChEMBL Positive allosteric modulation of GABAA receptor alpha4beta3delta (unknown origin) expressed in CHO cells assessed as potentiation of GABA-mediated increase in channel current under holding potential at -80 mV preincubated for 30 secs followed by GABA stimulation for 2 secs by manual patch clamp assay B 6.52 pEC50 299 nM EC50 J Med Chem (2017) 60: 7810-7819 [PMID:28753313]
ChEMBL Positive allosteric modulation of extrasynaptic alpha4beta3delta GABA-A receptor (unknown origin) transfected in CHO cells assessed as potentiation of GABA-induced peak current amplitude at -80 mV holding potential preincubated for 30 secs followed by GABA stimulation for 2 secs by manual patch assay B 6.87 pEC50 135 nM EC50 Eur J Med Chem (2024) 276: 116602-116602 [PMID:38971049]
Kir2.1/Inward rectifier potassium channel 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1914276] [GtoPdb: 430] [UniProtKB: P63252]
ChEMBL Inhibition of Kir2.1 (unknown origin) by patch clamp assay B 4.52 pIC50 >30000 nM IC50 J Med Chem (2017) 60: 7810-7819 [PMID:28753313]
Kv4.3/Kv channel-interacting protein 2/Potassium voltage-gated channel subfamily D member 3 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3885598] [GtoPdb: 554] [UniProtKB: Q9NS61, Q9UK17]
ChEMBL Inhibition of Kv4.3(unknown origin)/KChIP2.2 (unknown origin) by patch clamp assay B 4.52 pIC50 >30000 nM IC50 J Med Chem (2017) 60: 7810-7819 [PMID:28753313]
HCN2/Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795172] [GtoPdb: 401] [UniProtKB: Q9UL51]
ChEMBL Inhibition of HCN2 (unknown origin) by patch clamp assay B 4.52 pIC50 >30000 nM IC50 J Med Chem (2017) 60: 7810-7819 [PMID:28753313]
Kv1.5/Potassium voltage-gated channel subfamily A member 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4306] [GtoPdb: 542] [UniProtKB: P22460]
ChEMBL Inhibition of Kv1.5 (unknown origin) by patch clamp assay B 4.52 pIC50 >30000 nM IC50 J Med Chem (2017) 60: 7810-7819 [PMID:28753313]
Nav1.5/Sodium channel protein type 5 subunit alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524]
ChEMBL Inhibition of Nav1.5 (unknown origin) by patch clamp assay B 4.52 pIC50 >30000 nM IC50 J Med Chem (2017) 60: 7810-7819 [PMID:28753313]
Cav1.2/Voltage-dependent L-type calcium channel subunit alpha-1C in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1940] [GtoPdb: 529] [UniProtKB: Q13936]
ChEMBL Inhibition of Cav1.2 (unknown origin) by patch clamp assay B 4.52 pIC50 >30000 nM IC50 J Med Chem (2017) 60: 7810-7819 [PMID:28753313]
Kv11.1/Voltage-gated inwardly rectifying potassium channel KCNH2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG by patch clamp assay B 4.52 pIC50 >30000 nM IC50 J Med Chem (2017) 60: 7810-7819 [PMID:28753313]
Kv7.1/Voltage-gated potassium channel, IKs; KCNQ1(Kv7.1)/KCNE1(MinK) in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2221347] [GtoPdb: 560] [UniProtKB: P15382, P51787]
ChEMBL Inhibition of KCNQ1/minK (unknown origin) by patch clamp assay B 4.52 pIC50 >30000 nM IC50 J Med Chem (2017) 60: 7810-7819 [PMID:28753313]

ChEMBL data shown on this page come from version 36:

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]