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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  • G protein-coupled receptor kinase 6 in Human [ChEMBL: CHEMBL6144] [GtoPdb: 1470] [UniProtKB: P43250]
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  • enhancer of zeste 1 polycomb repressive complex 2 subunit/Histone-lysine N-methyltransferase EZH1 in Human [ChEMBL: CHEMBL2189116] [GtoPdb: 2835] [UniProtKB: Q92800]
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  • lysine methyltransferase 2A/Histone-lysine N-methyltransferase MLL in Human [ChEMBL: CHEMBL1293299] [GtoPdb: 2688] [UniProtKB: Q03164]
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  • nuclear receptor binding SET domain protein 2/Histone-lysine N-methyltransferase NSD2 in Human [ChEMBL: CHEMBL3108645] [GtoPdb: 3220] [UniProtKB: O96028]
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  • SET domain containing 7, histone lysine methyltransferase/Histone-lysine N-methyltransferase SETD7 in Human [ChEMBL: CHEMBL5523] [GtoPdb: 2703] [UniProtKB: Q8WTS6]
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  • Histone-lysine N-methyltransferase SMYD3 in Human [ChEMBL: CHEMBL2321643] [UniProtKB: Q9H7B4]
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  • Neuraminidase in Influenza A virus (A/Puerto Rico/8/1934(H1N1)) [ChEMBL: CHEMBL2051] [UniProtKB: P03468]
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  • Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Mouse [ChEMBL: CHEMBL2459] [GtoPdb: 595] [UniProtKB: P37238]
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  • pyruvate kinase M1/2/Pyruvate kinase isozymes M1/M2 in Human [ChEMBL: CHEMBL1075189] [GtoPdb: 3006] [UniProtKB: P14618]
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  • RTP Type S/Receptor-type tyrosine-protein phosphatase S in Human [ChEMBL: CHEMBL2396508] [GtoPdb: 1866] [UniProtKB: Q13332]
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  • CoV Replicase polyprotein 1ab/CoV RNA-dependent RNA polymerase/CoV Non-structural protein 15/CoV Non-structural protein 13 in SARS-CoV-2 [GtoPdb: 3125, 3139, 3206, 3261] [UniProtKB: P0DTD1, P0DTD1, P0DTD1, P0DTD1]
  • CoV Replicase polyprotein 1ab/CoV RNA-dependent RNA polymerase/CoV Non-structural protein 15/CoV Non-structural protein 13/Replicase polyprotein 1ab in Severe acute respiratory syndrome coronavirus 2 [ChEMBL: CHEMBL4523582] [GtoPdb: 3125, 3139, 3206, 3261] [UniProtKB: P0DTD1]
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  • OATP2B1/Solute carrier organic anion transporter family member 2B1 in Human [ChEMBL: CHEMBL1743124] [GtoPdb: 1224] [UniProtKB: O94956]
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  • fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
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  • TRPM8 in Human [GtoPdb: 500] [UniProtKB: Q7Z2W7]
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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
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]
ChEMBL Inhibition of PKM2 (unknown origin) Lys207, Hie78, Asp177, Asn75, Thr129, Gly128, Arg73 residues B 4.9 pIC50 12500 nM IC50 J Med Chem (2022) 65: 1171-1205 [PMID:34726055]
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]
CoV Replicase polyprotein 1ab/CoV RNA-dependent RNA polymerase/CoV Non-structural protein 15/CoV Non-structural protein 13 in SARS-CoV-2 [GtoPdb: 3125, 3139, 3206, 3261] [UniProtKB: P0DTD1, P0DTD1, P0DTD1, P0DTD1]
GtoPdb Inhibition of dsRNA unwinding activity; wildtype nsp13 - 5.52 pIC50 3000 nM IC50 SLAS Discov (2024) 29: 100145 [PMID:38301954]
CoV Replicase polyprotein 1ab/CoV RNA-dependent RNA polymerase/CoV Non-structural protein 15/CoV Non-structural protein 13/Replicase polyprotein 1ab in Severe acute respiratory syndrome coronavirus 2 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523582] [GtoPdb: 3125, 3139, 3206, 3261] [UniProtKB: P0DTD1]
ChEMBL Inhibition of N-terminal full length GST-tagged SARS-CoV-2 3CLpro expressed in Escherichia coli BL21 (DE3) by using MCA-AVLQSGFR-Lys(Dnp)-Lys-NH as fluorogenic substrate preincubated with compound for 10 mins followed by substrate addition by FRET assay B 5.24 pIC50 5800 nM IC50 Eur J Med Chem (2023) 257: 115491-115491 [PMID:37244162]
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]
OATP2B1/Solute carrier organic anion transporter family member 2B1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743124] [GtoPdb: 1224] [UniProtKB: O94956]
ChEMBL Inhibition of human OATP2B1 expressed in Flp-In-CHO cells assessed as inhibition of OATP2B1 mediated DBF uptake using DBF as fluorescent substrate incubated for 2 mins by BCA assay B 6.46 pIC50 350 nM IC50 RSC Med Chem (2023) 14: 890-898 [PMID:37252098]
ChEMBL Inhibition of human OATP2B1 expressed in Flp-In-CHO cells assessed as inhibition of OATP2B1 mediated DBF uptake using DBF as fluorescent substrate incubated for 2 mins by BCA assay B 6.46 pIC50 346.74 nM IC50 RSC Med Chem (2023) 14: 890-898 [PMID:37252098]
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 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]