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ChEMBL ligand: CHEMBL363211 |
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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 α1 subunit/GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABA-A receptor; alpha-1/beta-3/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094121] [GtoPdb: 404, 414, 412] [UniProtKB: P14867, P18507, P28472] | ||||||||
ChEMBL | Displacement of [3H]-Ro- 15-1788 from human gamma-aminobutyric-acid GABA-A receptor alpha-1-beta-3-gamma-2 expressed in L(tk-) cells | B | 9.08 | pKi | 0.83 | nM | Ki | J Med Chem (2004) 47: 5829-5832 [PMID:15537339] |
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]-Ro- 15-1788 from human gamma-aminobutyric-acid GABA-A receptor alpha-2-beta-3-gamma-2 expressed in L(tk-) cells | B | 9.07 | pKi | 0.85 | nM | Ki | J Med Chem (2004) 47: 5829-5832 [PMID:15537339] |
GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α3 subunit/GABA-A receptor; alpha-3/beta-3/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094120] [GtoPdb: 414, 412, 406] [UniProtKB: P18507, P28472, P34903] | ||||||||
ChEMBL | Displacement of [3H]-Ro- 15-1788 from human gamma-aminobutyric-acid GABA-A receptor alpha-3-beta-3-gamma-2 expressed in L(tk-) cells | B | 9.11 | pKi | 0.77 | nM | Ki | J Med Chem (2004) 47: 5829-5832 [PMID:15537339] |
GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α4 subunit/GABA A receptor alpha-4/beta-3/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111366] [GtoPdb: 414, 412, 407] [UniProtKB: P18507, P28472, P48169] | ||||||||
ChEMBL | Binding affinity towards gamma-aminobutyric-acid GABA-A receptor alpha-4-beta-3-gamma-2 | B | 6.4 | pKi | 395 | nM | Ki | J Med Chem (2004) 47: 5829-5832 [PMID:15537339] |
GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α5 subunit/GABA-A receptor; alpha-5/beta-3/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094122] [GtoPdb: 414, 412, 408] [UniProtKB: P18507, P28472, P31644] | ||||||||
ChEMBL | Inverse agonist activity at recombinant human GABA-A alpha5beta3gamma2 receptor expressed in mouse L(tk-) cells by radioligand binding assay | B | 8.52 | pKi | 3 | nM | Ki | Eur J Med Chem (2019) 171: 434-461 [PMID:30928713] |
ChEMBL | Displacement of [3H]-Ro- 15-1788 from human gamma-aminobutyric-acid GABA-A receptor alpha-5-beta-3-gamma-2 expressed in L(tk-) cells | B | 8.85 | pKi | 1.4 | nM | Ki | J Med Chem (2004) 47: 5829-5832 [PMID:15537339] |
ChEMBL | Displacement of [3H]Ro15-1788 from recombinant human GABA-A alpha5beta3gamma2 receptor expressed in mouse L(tk-) cells by radioligand binding assay | B | 8.85 | pKi | 1.4 | nM | Ki | Eur J Med Chem (2019) 171: 434-461 [PMID:30928713] |
GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α6 subunit/GABA-A receptor; alpha-6/beta-3/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095190] [GtoPdb: 414, 412, 409] [UniProtKB: P18507, P28472, Q16445] | ||||||||
ChEMBL | Binding affinity towards gamma-aminobutyric-acid GABA-A receptor alpha-6-beta-3-gamma-2 | B | 5.4 | pKi | >4000 | nM | Ki | J Med Chem (2004) 47: 5829-5832 [PMID:15537339] |
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 | 9.08 | pKi | 0.83 | nM | Ki | J Med Chem (2020) 63: 3425-3446 [PMID:31738537] |
ChEMBL | Positive allosteric modulation of GABAA alpha1 (unknown origin) | B | 9.1 | pKi | 0.8 | nM | Ki | J Med Chem (2013) 56: 593-624 [PMID:23121096] |
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 | 9.07 | pKi | 0.85 | nM | Ki | J Med Chem (2020) 63: 3425-3446 [PMID:31738537] |
ChEMBL | Positive allosteric modulation of GABAA alpha2 (unknown origin) | B | 9.1 | pKi | 0.8 | nM | Ki | J Med Chem (2013) 56: 593-624 [PMID:23121096] |
GABAA receptor α3 subunit/GABA receptor alpha-3 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3026] [GtoPdb: 406] [UniProtKB: P34903] | ||||||||
ChEMBL | Positive allosteric modulation of GABAA alpha3 (unknown origin) | B | 9.1 | pKi | 0.8 | nM | Ki | J Med Chem (2013) 56: 593-624 [PMID:23121096] |
ChEMBL | Binding affinity to GABA-A alpha3 (unknown origin) | B | 9.11 | pKi | 0.77 | nM | Ki | J Med Chem (2020) 63: 3425-3446 [PMID:31738537] |
GABAA receptor α5 subunit/GABA receptor alpha-5 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5112] [GtoPdb: 408] [UniProtKB: P31644] | ||||||||
ChEMBL | Positive allosteric modulation of GABAA alpha5 (unknown origin) | B | 8.85 | pKi | 1.4 | nM | Ki | J Med Chem (2013) 56: 593-624 [PMID:23121096] |
ChEMBL | Binding affinity to GABA-A alpha5 (unknown origin) | B | 8.85 | pKi | 1.4 | nM | Ki | J Med Chem (2020) 63: 3425-3446 [PMID:31738537] |
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]