zuranolone [Ligand Id: 12858] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4105630 (S-812217, Sage-217, SAGE-217, SGE-797, Zuranolone, Zurzuvae) |
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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 | 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] |
| 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] |
| Kv11.1/HERG 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] |
| 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] |
| Nav1.5/Sodium channel protein type V alpha subunit 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-gated L-type calcium channel alpha-1C subunit 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] |
| 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] |
| Kv1.5/Voltage-gated potassium channel subunit Kv1.5 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] |
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]
