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ChEMBL ligand: CHEMBL1783282 (Azd7325) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α2 subunit/GABA-A receptor; alpha-2/beta-3/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094130] [GtoPdb: 414, 412, 405] [UniProtKB: P18507, P28472, P47869] | ||||||||
ChEMBL | Displacement of [3H]flunitrazepam from benzodiazepine binding site GABAA alpha2beta3gamma2 receptor expressed in Sf9 cells after 1 hr | B | 9.51 | pKi | 0.31 | nM | Ki | Bioorg Med Chem (2011) 19: 2927-2938 [PMID:21498079] |
GtoPdb | - | - | 9.52 | pKi | 0.3 | nM | Ki | AZD7325.. astrazeneca.com |
GABAA receptor α1 subunit/GABA receptor alpha-1 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1962] [GtoPdb: 404] [UniProtKB: P14867] | ||||||||
ChEMBL | Binding affinity to GABA-A alpha1 (unknown origin) | B | 9.3 | pKi | 0.5 | nM | Ki | J Med Chem (2020) 63: 3425-3446 [PMID:31738537] |
GABAA receptor α2 subunit/GABA receptor alpha-2 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4956] [GtoPdb: 405] [UniProtKB: P47869] | ||||||||
ChEMBL | Binding affinity to GABA-A alpha2 (unknown origin) | B | 9.51 | pKi | 0.31 | nM | Ki | J Med Chem (2020) 63: 3425-3446 [PMID:31738537] |
GtoPdb | - | - | 9.52 | pKi | 0.3 | nM | Ki | AZD7325.. astrazeneca.com |
ChEMBL | Binding affinity to GABA-A alpha2 (unknown origin) | B | 9.52 | pKi | 0.3 | nM | Ki | J Med Chem (2020) 63: 3425-3446 [PMID:31738537] |
GABAA receptor α3 subunit/GABA receptor alpha-3 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3026] [GtoPdb: 406] [UniProtKB: P34903] | ||||||||
ChEMBL | Binding affinity to GABA-A alpha3 (unknown origin) | B | 8.89 | pKi | 1.3 | nM | Ki | J Med Chem (2020) 63: 3425-3446 [PMID:31738537] |
GtoPdb | - | - | 8.89 | pKi | 1.3 | nM | Ki | AZD7325.. astrazeneca.com |
GABAA receptor α5 subunit/GABA receptor alpha-5 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5112] [GtoPdb: 408] [UniProtKB: P31644] | ||||||||
ChEMBL | Binding affinity to GABA-A alpha5 (unknown origin) | B | 6.64 | pKi | 230 | nM | Ki | J Med Chem (2020) 63: 3425-3446 [PMID:31738537] |
MT1 receptor in Human [GtoPdb: 287] [UniProtKB: P48039] | ||||||||
GtoPdb | - | - | 6.9 | pIC50 | 126 | nM | IC50 | AZD7325.. astrazeneca.com |
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]