eszopiclone [Ligand Id: 7429] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1522 (Estorra, Eszopiclon, Eszopiclona, Eszopiclone, Eszopiclone civ, GSK-1755165, Lunesta, (S)-Zopiclone, (S)-ZOPICLONE, Zopiclone s-form) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 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 | Displacement of [3H]Ro-151788 from benzodiazepine binding site of GABAA alpha-2-beta-2-gamma-2 receptor expressed in HEK293T cells | B | 6.94 | pKi | 114 | nM | Ki | J Med Chem (2008) 51: 7243-7252 [PMID:18973287] |
| 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 | Displacement of [3H]Ro-151788 from benzodiazepine binding site of GABAA alpha-3-beta-2-gamma-2 receptor expressed in HEK293T cells | B | 6.79 | pKi | 162 | nM | Ki | J Med Chem (2008) 51: 7243-7252 [PMID:18973287] |
| 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 benzodiazepine binding site of GABAA alpha-6-beta-2-gamma-2 receptor expressed in HEK293T cells | B | 4.82 | pKi | >15000 | nM | Ki | J Med Chem (2008) 51: 7243-7252 [PMID:18973287] |
| GABAA receptor α1 subunit/GABA receptor alpha-1 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1962] [GtoPdb: 404] [UniProtKB: P14867] | ||||||||
| ChEMBL | Displacement of [3H]Ro15-1788 from benzodiazepine binding site of GABAA alpha-1-beta-2-gamma-2 receptor expressed in HEK293T cells | B | 7.3 | pKi | 50.1 | nM | Ki | J Med Chem (2008) 51: 7243-7252 [PMID:18973287] |
| GABAA receptor α4 subunit/GABA receptor alpha-4 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2472] [GtoPdb: 407] [UniProtKB: P48169] | ||||||||
| ChEMBL | Displacement of [3H]Ro-154513 from benzodiazepine binding site of GABAA alpha-4-beta-2-gamma-2 receptor expressed in HEK293T cells | B | 6.99 | pKi | 102 | nM | Ki | J Med Chem (2008) 51: 7243-7252 [PMID:18973287] |
| GABAA receptor α5 subunit/GABA receptor alpha-5 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5112] [GtoPdb: 408] [UniProtKB: P31644] | ||||||||
| ChEMBL | Displacement of [3H]Ro-151788 from benzodiazepine binding site of GABAA alpha-5-beta-2-gamma-2 receptor expressed in HEK293T cells | B | 4.82 | pKi | >15000 | nM | Ki | J Med Chem (2008) 51: 7243-7252 [PMID:18973287] |
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]
