6-Methylflavone [Ligand Id: 12466] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL134291 (6-Methylflavone)
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  • TAS2R39 in Human [GtoPdb: 675] [UniProtKB: P59534]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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: 419410416414408406413405407415409404412411417] [UniProtKB: O09028P15431P18506P18508P19969P20236P23574P23576P28471P28473P30191P62813P63079P63138Q91ZM7Q9ES14]
ChEMBL Ability to inhibit [3H]-Ro- 15-1788 binding to Gamma-aminobutyric acid A receptor alpha in vitro in rat cortical membranes B 6.74 pKi 180 nM Ki J Med Chem (2002) 45: 4188-4201 [PMID:12213060]
ChEMBL In vitro affinity against Benzodiazepine receptor binding to rat cortical membranes (using [3H]- flumazenil as radioligand). B 6.9 pKi 125 nM Ki J Med Chem (1999) 42: 4343-4350 [PMID:10543878]
tankyrase/Tankyrase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6164] [GtoPdb: 3108] [UniProtKB: O95271]
ChEMBL Inhibition of human TNKS1 (1030 to 1317) using NAD+ as substrate by fluorescence assay B 5 pIC50 >10000 nM IC50 J Med Chem (2013) 56: 7880-7889 [PMID:24116873]
TAS2R39 in Human [GtoPdb: 675] [UniProtKB: P59534]
GtoPdb - - 4.66 pIC50 21960 nM IC50 PLoS One (2014) 9: e94451 [PMID:24722342]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]