scutellarein [Ligand Id: 12463] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL55415 (5,6,7,4'-Tetrahydroxyflavone, 6-Hydroxyapigenin, Scutellarein) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Fructose-1,6-bisphosphatase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3975] [UniProtKB: P09467] | ||||||||
| ChEMBL | Inhibition of human liver FBP1 incubated for 5 mins by fluorescence method | B | 4.42 | pIC50 | 38200 | nM | IC50 | J Nat Prod (2020) 83: 1541-1552 [PMID:32364726] |
| GABAA receptor π subunit/GABAA receptor δ subunit/GABAA receptor α1 subunit/GABAA receptor β1 subunit/GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α5 subunit/GABAA receptor α3 subunit/GABAA receptor α2 subunit/GABAA receptor β2 subunit/GABAA receptor α4 subunit/GABAA receptor ε subunit/GABAA receptor α6 subunit/GABAA receptor γ1 subunit/GABAA receptor γ3 subunit/GABAA receptor θ subunit/GABA-A receptor; anion channel in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2093872] [GtoPdb: 419, 416, 404, 410, 414, 412, 408, 406, 405, 411, 407, 417, 409, 413, 415, 418] [UniProtKB: O00591, O14764, P14867, P18505, P18507, P28472, P31644, P34903, P47869, P47870, P48169, P78334, Q16445, Q8N1C3, Q99928, Q9UN88] | ||||||||
| ChEMBL | Binding affinity towards benzodiazepine site in GABAA receptor | B | 4.92 | pKi | 12022.64 | nM | Ki | J Med Chem (2001) 44: 1883-1891 [PMID:11384234] |
| G protein-coupled receptor kinase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6144] [GtoPdb: 1470] [UniProtKB: P43250] | ||||||||
| ChEMBL | Inhibition of human recombinant full-length GST-tagged human GRK6 using peptide substrate peptide-216 incubated for 7 hrs | B | 5.18 | pIC50 | 6610 | nM | IC50 | US-20140309185-A1. Inhibiting G-protein coupled receptor 6 kinase polypeptides (2014) |
| enhancer of zeste 1 polycomb repressive complex 2 subunit/Histone-lysine N-methyltransferase EZH1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2189116] [GtoPdb: 2835] [UniProtKB: Q92800] | ||||||||
| ChEMBL | Inhibition of Ezh1 (unknown origin) preincubated for 15 mins followed by addition of substrate measured after 1 hr by AlphaLISA assay | B | 5.06 | pIC50 | 8770 | nM | IC50 | Bioorg Med Chem (2020) 28: 115372-115372 [PMID:32088124] |
| lysine methyltransferase 2A/Histone-lysine N-methyltransferase MLL in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293299] [GtoPdb: 2688] [UniProtKB: Q03164] | ||||||||
| ChEMBL | Inhibition of MLL1 (unknown origin) preincubated for 15 mins followed by addition of substrate measured after 1 hr by AlphaLISA assay | B | 5.53 | pIC50 | 2920 | nM | IC50 | Bioorg Med Chem (2020) 28: 115372-115372 [PMID:32088124] |
| nuclear receptor binding SET domain protein 2/Histone-lysine N-methyltransferase NSD2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3108645] [GtoPdb: 3220] [UniProtKB: O96028] | ||||||||
| ChEMBL | Inhibition of NSD2 (unknown origin) preincubated for 15 mins followed by addition of [3H]-SAM as substrate and peptide solution after 240 mins cold SAM was added measured by radioisotope assay | B | 5.58 | pIC50 | 2650 | nM | IC50 | Bioorg Med Chem (2020) 28: 115372-115372 [PMID:32088124] |
| SET domain containing 7, histone lysine methyltransferase/Histone-lysine N-methyltransferase SETD7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5523] [GtoPdb: 2703] [UniProtKB: Q8WTS6] | ||||||||
| ChEMBL | Inhibition of human SET7 overexpressed in Escherichia coli BL21 (DE3) cells preincubated for 15 mins followed by addition of SAM as substrate and biotinylated Histone H3 (1-50) peptide measured after 30 mins by AlphaLISA assay relative to control | B | 5.71 | pIC50 | 1960 | nM | IC50 | Bioorg Med Chem (2020) 28: 115372-115372 [PMID:32088124] |
| Histone-lysine N-methyltransferase SMYD3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2321643] [UniProtKB: Q9H7B4] | ||||||||
| ChEMBL | Inhibition of SMYD3 (unknown origin) preincubated for 15 mins followed by addition of [3H]-SAM as substrate and peptide solution after 240 mins cold SAM was added measured after 1 hr by radioisotope assay | B | 4.74 | pIC50 | 18230 | nM | IC50 | Bioorg Med Chem (2020) 28: 115372-115372 [PMID:32088124] |
| Neuraminidase in Influenza A virus (A/Puerto Rico/8/1934(H1N1)) (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2051] [UniProtKB: P03468] | ||||||||
| ChEMBL | Inhibition of Influenza A PR/8/34 H1N1 virus neuraminidase activity by MUN-ANA substrate based fluorimetric assay | B | 1.16 | pIC50 | 1.16 | - | logIC50 | Eur J Med Chem (2010) 45: 1724-1730 [PMID:20116898] |
| Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2459] [GtoPdb: 595] [UniProtKB: P37238] | ||||||||
| ChEMBL | Agonist activity at mouse PPARgamma expressed in HEK293 cells co-expressing with Gal4 reporter vector after 24 hrs by dual-luciferase reporter assay | B | 4.79 | pEC50 | 16400 | nM | EC50 | J Nat Prod (2014) 77: 1594-1600 [PMID:24955889] |
| pyruvate kinase M1/2/Pyruvate kinase isozymes M1/M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075189] [GtoPdb: 3006] [UniProtKB: P14618] | ||||||||
| ChEMBL | Inhibition of recombinant human N-terminal His6/SUMO-tagged PKM1 expressed in Escherichia coli BL21 using PEP as substrate incubated for 30 mins in presence of ADP by spectrophotometric based LDH enzyme coupled assay | B | 4 | pIC50 | 100000 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 5404-5408 [PMID:29157862] |
| ChEMBL | Inhibition of recombinant human N-terminal His6/SUMO-tagged PKM2 expressed in Escherichia coli BL21 using PEP as substrate incubated for 30 mins in presence of ADP by spectrophotometric based LDH enzyme coupled assay | B | 4.9 | pIC50 | 12500 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 5404-5408 [PMID:29157862] |
| RTP Type S/Receptor-type tyrosine-protein phosphatase S in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2396508] [GtoPdb: 1866] [UniProtKB: Q13332] | ||||||||
| ChEMBL | Inhibition of recombinant human PTP-sigma (residues 1367 to 1948) using para-nitrophenylphosphate as substrate for 60 mins by fluorescence analysis | B | 6.22 | pIC50 | 600 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 87-93 [PMID:26602279] |
| Salivary alpha-amylase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2478] [UniProtKB: P0DUB6] | ||||||||
| ChEMBL | Inhibition of human salivary alpha-amylase | B | 5.02 | pIC50 | 9640 | nM | IC50 | J Med Chem (2008) 51: 3555-3561 [PMID:18507367] |
| neuraminidase 2/Sialidase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3200] [GtoPdb: 3258] [UniProtKB: Q9Y3R4] | ||||||||
| ChEMBL | Inhibition of human Neu2 assessed as MuNANA substrate hydrolysis in presence of 0.1% Triton X-100 by discontinuous fluorimetric assay | B | 4.26 | pIC50 | 55000 | nM | IC50 | Bioorg Med Chem (2010) 18: 1633-1640 [PMID:20097567] |
| fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888] | ||||||||
| ChEMBL | Inhibition of recombinant FLT3 (unknown origin) by TR-FRET assay | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 1768-1770 [PMID:23411073] |
| Xanthine dehydrogenase in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3649] [UniProtKB: P80457] | ||||||||
| ChEMBL | Inhibition of cow milk xanthine oxidase | B | 4.9 | pIC50 | 12600 | nM | IC50 | J Nat Prod (1988) 51: 345-348 [PMID:3379415] |
| TRPM8 in Human [GtoPdb: 500] [UniProtKB: Q7Z2W7] | ||||||||
| GtoPdb | - | - | 5.77 | pIC50 | 1700 | nM | IC50 | J Nat Med (2021) 75: 717-725 [PMID:33877504] |
| TAS2R39 in Human [GtoPdb: 675] [UniProtKB: P59534] | ||||||||
| GtoPdb | - | - | 4.39 | pEC50 | 40300 | nM | EC50 | J Agric Food Chem (2013) 61: 10454-66 [PMID:24117141] |
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]
