baicalein [Ligand Id: 5144] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL8260 (Baicalein, Noroxylin, NSC-661431)
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  • 12S-LOX/Arachidonate 12-lipoxygenase in Human [ChEMBL: CHEMBL3687] [GtoPdb: 1387] [UniProtKB: P18054]
  • 15-LOX-1/Arachidonate 12-lipoxygenase in Rat [ChEMBL: CHEMBL2741] [GtoPdb: 1388] [UniProtKB: Q02759]
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  • 15-LOX-1/Arachidonate 15-lipoxygenase in Human [ChEMBL: CHEMBL2903] [GtoPdb: 1388] [UniProtKB: P16050]
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  • 15-LOX-2/Arachidonate 15-lipoxygenase, type II in Human [ChEMBL: CHEMBL2457] [GtoPdb: 1389] [UniProtKB: O15296]
  • 15-LOX-2/Arachidonate 15-lipoxygenase, type II in Rat [ChEMBL: CHEMBL3289] [GtoPdb: 1389] [UniProtKB: Q8K4F2]
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  • 5-LOX/Arachidonate 5-lipoxygenase in Rat [ChEMBL: CHEMBL312] [GtoPdb: 1385] [UniProtKB: P12527]
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  • G protein-coupled receptor kinase 6 in Human [ChEMBL: CHEMBL6144] [GtoPdb: 1470] [UniProtKB: P43250]
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  • histone deacetylase 6/Histone deacetylase 6 in Human [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7]
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  • Human immunodeficiency virus type 1 integrase in Human immunodeficiency virus 1 [ChEMBL: CHEMBL3471] [UniProtKB: Q7ZJM1]
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  • lysine demethylase 4E/Lysine-specific demethylase 4D-like in Human [ChEMBL: CHEMBL1293226] [GtoPdb: 2679] [UniProtKB: B2RXH2]
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  • lysine demethylase 1A/Lysine-specific histone demethylase 1 in Human [ChEMBL: CHEMBL6136] [GtoPdb: 2669] [UniProtKB: O60341]
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  • prolyl endopeptidase/Prolyl endopeptidase in Human [ChEMBL: CHEMBL3202] [GtoPdb: 2395] [UniProtKB: P48147]
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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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  • Replicase polyprotein 1ab in Middle East respiratory syndrome-related coronavirus (isolate UnitedKingdom/H123990006/2012) (Betacoronavirus England 1) (Humancoronavirus EMC) [ChEMBL: CHEMBL4295557] [UniProtKB: K9N7C7]
  • 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: 3125313932063261] [UniProtKB: P0DTD1]
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  • polo like kinase 1/Serine/threonine-protein kinase PLK1 in Human [ChEMBL: CHEMBL3024] [GtoPdb: 2168] [UniProtKB: P53350]
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  • polo like kinase 3/Serine/threonine-protein kinase PLK3 in Human [ChEMBL: CHEMBL4897] [GtoPdb: 2170] [UniProtKB: Q9H4B4]
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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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  • YES proto-oncogene 1, Src family tyrosine kinase/Tyrosine-protein kinase YES in Human [ChEMBL: CHEMBL2073] [GtoPdb: 2284] [UniProtKB: P07947]
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  • Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Rat [ChEMBL: CHEMBL3762] [GtoPdb: 529] [UniProtKB: P22002]
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  • xanthine dehydrogenase/Xanthine dehydrogenase in Human [ChEMBL: CHEMBL1929] [GtoPdb: 2646] [UniProtKB: P47989]
  • Xanthine dehydrogenase in Bovine [ChEMBL: CHEMBL3649] [UniProtKB: P80457]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
synuclein alpha/Alpha-synuclein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6152] [GtoPdb: 3285] [UniProtKB: P37840]
ChEMBL Inhibition of human alpha-synuclein filament formation expressed in Escherichia coli BL21(DE3) cells incubated for 72 hrs by thioflavin S based fluorescence assay B 5.09 pIC50 8200 nM IC50 Eur J Med Chem (2019) 167: 10-36 [PMID:30743095]
12S-LOX/Arachidonate 12-lipoxygenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3687] [GtoPdb: 1387] [UniProtKB: P18054]
ChEMBL Inhibition of human platelet-type 12-lipoxygenase B 5.8 pKi 1600 nM Ki J Med Chem (2011) 54: 5485-5497 [PMID:21739938]
ChEMBL Inhibition of 12-hLO B 6.07 pIC50 860 nM IC50 Bioorg Med Chem (2007) 15: 7408-7425 [PMID:17869117]
15-LOX-1/Arachidonate 12-lipoxygenase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2741] [GtoPdb: 1388] [UniProtKB: Q02759]
ChEMBL Inhibitory activity against 12-lipoxygenase in rat platelet rich plasma B 7.82 pIC50 15 nM IC50 J Med Chem (1991) 34: 1503-1505 [PMID:2016727]
15-LOX-1/Arachidonate 15-lipoxygenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2903] [GtoPdb: 1388] [UniProtKB: P16050]
ChEMBL Inhibition of human 15-lipoxygenase B 6.22 pKi 600 nM Ki J Med Chem (2011) 54: 5485-5497 [PMID:21739938]
ChEMBL Inhibition of 15-hLO1 B 5.04 pIC50 9100 nM IC50 Bioorg Med Chem (2007) 15: 7408-7425 [PMID:17869117]
15-LOX-2/Arachidonate 15-lipoxygenase, type II in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2457] [GtoPdb: 1389] [UniProtKB: O15296]
ChEMBL Inhibition of 15-hLO2 B 4 pIC50 >100000 nM IC50 Bioorg Med Chem (2007) 15: 7408-7425 [PMID:17869117]
15-LOX-2/Arachidonate 15-lipoxygenase, type II in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3289] [GtoPdb: 1389] [UniProtKB: Q8K4F2]
ChEMBL Inhibitory activity against 15-lipoxygenase in rat polymorphonuclear leukocytes B 6.59 pIC50 260 nM IC50 J Med Chem (1991) 34: 1503-1505 [PMID:2016727]
5-LOX/Arachidonate 5-lipoxygenase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL312] [GtoPdb: 1385] [UniProtKB: P12527]
ChEMBL In vitro inhibition of LTB4 production was measured in rat blood F 5 pIC50 10000 nM IC50 J Med Chem (1991) 34: 1028-1036 [PMID:1848292]
ChEMBL Inhibitory activity against 5-lipoxygenase in rat polymorphonuclear leukocytes B 5 pIC50 >10000 nM IC50 J Med Chem (1991) 34: 1503-1505 [PMID:2016727]
cyclin dependent kinase 1/Cyclin-dependent kinase 1/cyclin B1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907602] [GtoPdb: 1961] [UniProtKB: P06493P14635]
ChEMBL Inhibition of Cdk1/cyclin B B 5.19 pIC50 6530 nM IC50 Bioorg Med Chem (2008) 16: 7128-7133 [PMID:18639462]
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 4.54 pIC50 29000 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: 419416404410414412408406405411407417409413415418] [UniProtKB: O00591O14764P14867P18505P18507P28472P31644P34903P47869P47870P48169P78334Q16445Q8N1C3Q99928Q9UN88]
ChEMBL Binding affinity towards benzodiazepine site in GABAA receptor B 5.25 pKi 5623.41 nM Ki J Med Chem (2001) 44: 1883-1891 [PMID:11384234]
Glucocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2034] [GtoPdb: 625] [UniProtKB: P04150]
ChEMBL Competitive inhibition of glucocorticoid receptor (unknown origin) by fluorescence polarization based competition assay B 4.72 pIC50 19000 nM IC50 J Nat Prod (2022) 85: 237-247 [PMID:34935393]
Glyoxalase I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2424] [UniProtKB: Q04760]
ChEMBL Inhibition of human recombinant His-tagged Glyoxalase 1 expressed in Sf21-Baculovirus system B 4.96 pIC50 11000 nM IC50 Bioorg Med Chem (2008) 16: 3969-3975 [PMID:18258440]
GPR35/G-protein coupled receptor 35 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293267] [GtoPdb: 102] [UniProtKB: Q9HC97]
ChEMBL Desensitization of GPR35 receptor in human HT-29 cells assessed as inhibition of zaprinast-induced dynamic mass redistribution after 10 mins B 4.55 pIC50 28200 nM IC50 ACS Med Chem Lett (2012) 3: 165-169 [PMID:24900447]
ChEMBL Agonist activity at GPR35 receptor in human U2OS cells coexpressing Gal4-VP16-TEV assessed as beta arrestin translocation after 5 hrs by beta lactamase reporter gene assay F 4.64 pEC50 22700 nM EC50 ACS Med Chem Lett (2012) 3: 165-169 [PMID:24900447]
ChEMBL Agonist activity at GPR35 receptor in human HT-29 cells after 10 mins by dynamic mass redistribution assay F 4.99 pEC50 10300 nM EC50 ACS Med Chem Lett (2012) 3: 165-169 [PMID:24900447]
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 5.06 pIC50 8700 nM IC50 US-20140309185-A1. Inhibiting G-protein coupled receptor 6 kinase polypeptides (2014)
histone deacetylase 6/Histone deacetylase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7]
ChEMBL Determination of IC50 values for inhibition of enzymatic assay of human HDAC6 with custom peptide substrate B 5.92 pIC50 1204 nM IC50 HDAC6 screening dataset using tau-based substrate in an enzymatic assay yields selective inhibitors and activators
Human immunodeficiency virus type 1 integrase in Human immunodeficiency virus 1 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3471] [UniProtKB: Q7ZJM1]
ChEMBL Inhibition of recombinant HIV-1 integrase 3'-processing activity using 32P 5' end-labeled linear 21'mer as substrate preincubated for 30 mins prior to substrate challenge by phosphorimaging analysis B 5.12 pIC50 7500 nM IC50 Bioorg Med Chem (2014) 22: 3146-3158 [PMID:24794743]
ChEMBL IC50 was measured as concentration required to inhibit 50% of HIV-integrase integration B 5.37 pIC50 4300 nM IC50 J Med Chem (1995) 38: 890-897 [PMID:7699704]
ChEMBL Inhibition of His6-tagged HIV-1 integrase assessed as decrease in integrase-Flag-LEDGF/p75 interaction preincubated with enzyme for 30 mins followed by addition of Flag-LEDGF/p75 for 1 hr by AlphaScreen assay B 5.57 pIC50 2700 nM IC50 Bioorg Med Chem (2014) 22: 3146-3158 [PMID:24794743]
ChEMBL IC50 was measured as concentration required to inhibit 50% of HIV-integrase cleavage B 5.92 pIC50 1200 nM IC50 J Med Chem (1995) 38: 890-897 [PMID:7699704]
ChEMBL Inhibition of recombinant HIV-1 integrase strand transfer activity using 32P 5' end-labeled linear 21'mer as substrate preincubated for 30 mins prior to substrate challenge by phosphorimaging analysis B 6.11 pIC50 780 nM IC50 Bioorg Med Chem (2014) 22: 3146-3158 [PMID:24794743]
lysine demethylase 4E/Lysine-specific demethylase 4D-like in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293226] [GtoPdb: 2679] [UniProtKB: B2RXH2]
ChEMBL Non-competitive inhibition of JMJD2E relative to alpha-ketoglutarate B 5.36 pKi 4330 nM Ki Bioorg Med Chem (2011) 19: 3625-3636 [PMID:21596573]
ChEMBL Inhibition of JMJD2E B 5.52 pIC50 3000 nM IC50 Bioorg Med Chem (2011) 19: 3625-3636 [PMID:21596573]
ChEMBL Inhibition of N-terminal His-6-tagged human JMJD2E (1 to 337 residues) expressed in Escherichia coli by MALDI-TOF/MS analysis B 5.52 pIC50 3000 nM IC50 Medchemcomm (2012) 3: 135-161
lysine demethylase 1A/Lysine-specific histone demethylase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6136] [GtoPdb: 2669] [UniProtKB: O60341]
ChEMBL Inhibition of LSD1 (unknown origin) B 4.9 pIC50 12500 nM IC50 Bioorg Med Chem (2019) 27: 370-374 [PMID:30552007]
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
ChEMBL TP_TRANSPORTER: increase in Vinblastine intracellular accumulation in KB/MDR cells F 4.39 pIC50 41000 nM IC50 J Med Chem (2004) 47: 5555-5566 [PMID:15481991]
Progesterone receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL208] [GtoPdb: 627] [UniProtKB: P06401]
ChEMBL Competitive inhibition of progesterone receptor (unknown origin) by fluorescence polarization based competition assay B 4.82 pIC50 15000 nM IC50 J Nat Prod (2022) 85: 237-247 [PMID:34935393]
prolyl endopeptidase/Prolyl endopeptidase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3202] [GtoPdb: 2395] [UniProtKB: P48147]
ChEMBL Inhibition of human brain prolyl oligopeptidase expressed in Escherichia coli B 4.44 pIC50 36000 nM IC50 Bioorg Med Chem (2008) 16: 7516-7524 [PMID:18650094]
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 4.99 pIC50 10300 nM IC50 Bioorg Med Chem Lett (2016) 26: 87-93 [PMID:26602279]
Replicase polyprotein 1ab in Middle East respiratory syndrome-related coronavirus (isolate UnitedKingdom/H123990006/2012) (Betacoronavirus England 1) (Humancoronavirus EMC) (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4295557] [UniProtKB: K9N7C7]
ChEMBL MERS_3CL Pro protease inhibition IC50 by FRET kind of response from peptide substrate F 5 pIC50 >10000 nM IC50 Identification of inhibitors of SARS-Cov2 M-Pro enzymatic activity using a small molecule repurposing screen
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: 3125313932063261] [UniProtKB: P0DTD1]
ChEMBL Binding affinity to SARS-CoV-2 3CL protease at 1.875 to 50 uM by SPR assay B 4.5 pKd 31300 nM Kd J Nat Prod (2022) 85: 327-336 [PMID:35084181]
ChEMBL Binding affinity to C-terminal GST-tagged full length SARS CoV-2 3CL protease expressed in Escherichia coli BL21 (DE3) cells incubated for 1 hr by ESI-MS assay B 4.91 pKd 12400 nM Kd J Med Chem (2022) 65: 2716-2746 [PMID:33186044]
ChEMBL Binding affinity to C-terminal GST-tagged full length SARS CoV-2 3CL protease expressed in Escherichia coli BL21 (DE3) cells by isothermal titration calorimetry assay B 4.94 pKd 11500 nM Kd J Med Chem (2022) 65: 2716-2746 [PMID:33186044]
ChEMBL Inhibition of 6his/TEV-fused GST tagged SARS-CoV-2 MPro (1 to 306 residues) expressed in Escherichia coli RIL cells using 5-FAM-AVLQSGFR-Lys-(Dabcyl)-K-amide as substrate assessed as substrate cleavage preincubated for 30 mins followed by substrate addition and measured every 30 sec for 60 cycles by FRET based assay B 4.3 pIC50 50600 nM IC50 J Nat Prod (2023) 86: 264-275 [PMID:36651644]
ChEMBL Inhibition of SARS-CoV-2 MPro using Dabcyl-KTSAVLQSGFRKME-Edans as substrate preincubated for 5 mins followed by substrate addition and measured after 10 mins by fluorescence based assay B 5.29 pIC50 5160 nM IC50 J Nat Prod (2023) 86: 264-275 [PMID:36651644]
ChEMBL Inhibition of SARS-CoV-2 3CL protease using MCA-AVLQSGFR-Lys(Dnp)-Lys-NH2 as flurogenic substrate pre-incubated with compound for 10 mins followed by substrate addition measured after 10 mins by FRET assay B 5.29 pIC50 5100 nM IC50 J Nat Prod (2022) 85: 327-336 [PMID:35084181]
ChEMBL Inhibition of C-terminal GST-tagged full length SARS CoV 3CL protease expressed in Escherichia coli BL21 (DE3) cells using MCA-AVLQSGFR-Lys(Dnp)-Lys-NH as substrate incubated for 10 mins by FRET assay B 5.96 pIC50 1100 nM IC50 J Med Chem (2022) 65: 2716-2746 [PMID:33186044]
ChEMBL Inhibition of SARS-CoV-2 MPro B 6.01 pIC50 980 nM IC50 J Nat Prod (2023) 86: 264-275 [PMID:36651644]
ChEMBL Inhibition of C-terminal GST-tagged full length SARS CoV-2 3CL protease expressed in Escherichia coli BL21 (DE3) cells using MCA-AVLQSGFR-Lys(Dnp)-Lys-NH as substrate incubated for 10 mins by FRET assay B 6.03 pIC50 940 nM IC50 J Med Chem (2022) 65: 2716-2746 [PMID:33186044]
ChEMBL Inhibition of SARS-CoV-2 main protease B 6.03 pIC50 940 nM IC50 Eur J Med Chem (2020) 201: 112559-112559 [PMID:32563814]
ChEMBL Inhibition of N-terminal MBP-tagged SARS CoV-2 Main protease by fluorescence based analysis B 6.03 pIC50 940 nM IC50 J Med Chem (2021) 64: 16922-16955 [PMID:34798775]
ChEMBL Inhibition of GST-tagged SARS-CoV-2 main protease expressed in Escherichia coli BL21 (De3) using MCA-AVLQSGFR-Lys(Dnp)-Lys-NH2 as substrate preincubated for 10 mins followed by substrate addition and measured for 3.5 mins by FRET analysis B 6.03 pIC50 940 nM IC50 Eur J Med Chem (2022) 238: 114508-114508 [PMID:35688005]
ChEMBL Inhibition of SARS-CoV-2 MPro B 6.03 pIC50 940 nM IC50 Bioorg Med Chem (2021) 29: 115860-115860 [PMID:33191083]
ChEMBL Inhibition of SARS-CoV-2 (BetaCoV/Wuhan/WIV04/2019) MPro expressed in Escherichia coli using FRET susbtrate measured after 1 hr B 6.03 pIC50 940 nM IC50 Bioorg Med Chem (2021) 29: 115860-115860 [PMID:33191083]
ChEMBL Inhibition of SARS-CoV-2 MPro B 6.03 pIC50 939.72 nM IC50 Bioorg Med Chem (2021) 29: 115860-115860 [PMID:33191083]
ChEMBL Inhibition of C-terminal His6-tagged full length SARS CoV-2 3CL protease expressed in Escherichia coli BL21 (DE3) cells using Thr-Ser-Ala-Val-Leu-Gln-pNA substrate preincubated for 30 mins followed by substrate addition by microplate reader analysis B 6.47 pIC50 340 nM IC50 J Med Chem (2022) 65: 2716-2746 [PMID:33186044]
ChEMBL SARS-CoV-2 3CL-Pro protease inhibition IC50 determined by FRET kind of response from peptide substrate F 7.7 pIC50 20 nM IC50 Identification of inhibitors of SARS-Cov2 M-Pro enzymatic activity using a small molecule repurposing screen
ChEMBL Inhibition of C-terminal GST-tagged full length SARS CoV-2 3CL protease expressed in Escherichia coli BL21 (DE3) cells measured after 48 hrs by qRT-PCR analysis B 5.77 pEC50 1690 nM EC50 J Med Chem (2022) 65: 2716-2746 [PMID:33186044]
polo like kinase 1/Serine/threonine-protein kinase PLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3024] [GtoPdb: 2168] [UniProtKB: P53350]
ChEMBL Inhibition of PLK1 (unknown origin) in the presence of ATP by ADP-Glo-kinase assay B 5.05 pIC50 9000 nM IC50 J Med Chem (2022) 65: 10133-10160 [PMID:35878418]
polo like kinase 3/Serine/threonine-protein kinase PLK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4897] [GtoPdb: 2170] [UniProtKB: Q9H4B4]
ChEMBL Inhibition of PLK3 (unknown origin) in the presence of ATP by ADP-Glo-kinase assay B 4.4 pIC50 40000 nM IC50 J Med Chem (2022) 65: 10133-10160 [PMID:35878418]
Sucrase-isomaltase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2748] [UniProtKB: P14410]
ChEMBL Inhibition of sucrase B 4.28 pIC50 52000 nM IC50 Bioorg Med Chem Lett (2008) 18: 1659-1662 [PMID:18255289]
ChEMBL Inhibition of human intestinal sucrase in human Caco-2 cell membrane B 4.46 pIC50 35000 nM IC50 J Nat Prod (1998) 61: 1413-1415 [PMID:9834167]
Sucrase-isomaltase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3114] [UniProtKB: P23739]
ChEMBL Inhibition of rat intestinal sucrase B 4.28 pIC50 52000 nM IC50 Bioorg Med Chem Lett (2008) 18: 812-815 [PMID:18039578]
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]
YES proto-oncogene 1, Src family tyrosine kinase/Tyrosine-protein kinase YES in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073] [GtoPdb: 2284] [UniProtKB: P07947]
ChEMBL Inhibition of YES (unknown origin) B 5.48 pIC50 3300 nM IC50 Eur J Med Chem (2019) 166: 186-196 [PMID:30769179]
Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3762] [GtoPdb: 529] [UniProtKB: P22002]
ChEMBL Inhibition of Cav1.2 calcium current measured using whole cell patch clamp in rat Artery myocytes F 4.07 pIC50 85100 nM IC50 IC50 data for the L-type calcium channel extracted from a set of literature articles
xanthine dehydrogenase/Xanthine dehydrogenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1929] [GtoPdb: 2646] [UniProtKB: P47989]
ChEMBL Inhibition of xanthine oxidase assessed as decrease in uric acid production by spectrophotometry B 5.55 pIC50 2790 nM IC50 J Nat Prod (1998) 61: 71-76 [PMID:9461655]
Xanthine dehydrogenase in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3649] [UniProtKB: P80457]
ChEMBL Inhibition of bovine milk xanthine oxidase assessed using xanthine as substrate after 10 mins by fluorometric assay B 4.15 pIC50 71500 nM IC50 Eur J Med Chem (2017) 135: 491-516 [PMID:28478180]
ChEMBL Inhibition of cow milk xanthine oxidase B 5.48 pIC50 3300 nM IC50 J Nat Prod (1988) 51: 345-348 [PMID:3379415]

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]