gaboxadol [Ligand Id: 4322] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL312443 (Gaboxadol, LU 02-030, LU-02-030, LU-02030, MK-0928, NSC-759585) |
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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 | Agonist activity at human GABAA alpha1beta2gamma2S receptor expressed in TSA201 cells after 1 min by FLIPR assay | B | 4.85 | pEC50 | 14125.38 | nM | EC50 | J Med Chem (2013) 56: 993-1006 [PMID:23294161] |
| ChEMBL | Agonist activity at human GABAA alpha1beta2gamma2S receptor expressed in TSA201 cells after 1 min by FLIPR assay | B | 4.85 | pEC50 | 14000 | nM | EC50 | J Med Chem (2013) 56: 993-1006 [PMID:23294161] |
| 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 | Displacement of [3H]muscimol from GABAA receptor in rat brain synaptic membranes | B | 6.8 | pKi | 160 | nM | Ki | J Med Chem (2006) 49: 4442-4446 [PMID:16821803] |
| ChEMBL | Inhibition against Gamma-aminobutyric acid A (GABA-A) receptor | B | 6.89 | pIC50 | 130 | nM | IC50 | J Med Chem (2000) 43: 4930-4933 [PMID:11150163] |
| ChEMBL | In vitro affinity for GABA binding sites on purified synaptic membranes from rat brain. | B | 6.89 | pIC50 | 130 | nM | IC50 | J Med Chem (1983) 26: 895-900 [PMID:6304315] |
| ChEMBL | Inhibition of [3H]-GABA binding to GABA-A receptor in rat cerebral cortex homogenates | B | 7 | pIC50 | 100 | nM | IC50 | Bioorg Med Chem Lett (1991) 1: 247-248 |
| ChEMBL | Binding affinity against Gamma-aminobutyric acid A receptor in rat cerebral cortex | B | 7.04 | pIC50 | 92 | nM | IC50 | J Med Chem (1995) 38: 3287-3296 [PMID:7650683] |
| ChEMBL | Displacement of [3H]- muscimol in cerebral tissue of male rats | B | 7.5 | pIC50 | 31.5 | nM | IC50 | J Med Chem (1985) 28: 1109-1111 [PMID:2991521] |
| GABAB2/GABAB1/GABA B receptor in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111474] [GtoPdb: 241, 240] [UniProtKB: O88871, Q9Z0U4] | ||||||||
| ChEMBL | Inhibition of Gamma-aminobutyric acid type B receptor of rat cortex | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1995) 38: 3287-3296 [PMID:7650683] |
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]
