epicatechin gallate [Ligand Id: 12462] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL36327 ((-)-Epicatechin Gallate, Epicatechin Gallate) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 3-oxoacyl-acyl-carrier protein reductase in Plasmodium falciparum (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4513] [UniProtKB: Q965D6] | ||||||||
| ChEMBL | Inhibition of FabG | B | 6 | pIC50 | 1000 | nM | IC50 | J Med Chem (2006) 49: 3345-3353 [PMID:16722653] |
| 6-phosphogluconate dehydrogenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3404] [UniProtKB: P52209] | ||||||||
| ChEMBL | Inhibition of 6PGD | B | 6.68 | pIC50 | 210 | nM | IC50 | Bioorg Med Chem (2008) 16: 3580-3586 [PMID:18313308] |
| ADAMTS4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2318] [GtoPdb: 1677] [UniProtKB: O75173] | ||||||||
| ChEMBL | Inhibition of ADAMTS-4 (unknown origin) | B | 7 | pIC50 | 100 | nM | IC50 | J Med Chem (2022) 65: 13505-13532 [PMID:36250680] |
| ADAMTS5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2285] [GtoPdb: 1678] [UniProtKB: Q9UNA0] | ||||||||
| ChEMBL | Inhibition of ADAMTS-5 (unknown origin) | B | 7 | pIC50 | 100 | nM | IC50 | J Med Chem (2022) 65: 13505-13532 [PMID:36250680] |
| 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 | 5.01 | pIC50 | 9800 | nM | IC50 | Eur J Med Chem (2019) 167: 10-36 [PMID:30743095] |
| BCL2 apoptosis regulator/Apoptosis regulator Bcl-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4860] [GtoPdb: 2844] [UniProtKB: P10415] | ||||||||
| ChEMBL | Displacement of NLWAAQRYGRELRRMSD-K(FITC)-FVD from Bcl-2 (unknown origin) by fluorescence polarization assay | B | 6.4 | pKi | 400 | nM | Ki | Med Chem Res (2010) 19: 817-835 |
| ChEMBL | Binding affinity to BCL2 | B | 6.64 | pKi | 229.09 | nM | Ki | Proc Natl Acad Sci U S A (2007) 104: 19512-19517 [PMID:18040043] |
| CB1 receptor/Cannabinoid CB1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554] | ||||||||
| ChEMBL | Displacement of [3H]-CP55940 from CB1 receptor (unknown origin) | B | 4.33 | pKi | 47300 | nM | Ki | J Nat Prod (2019) 82: 636-646 [PMID:30816712] |
| CB2 receptor/Cannabinoid CB2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972] | ||||||||
| ChEMBL | Displacement of [3H]-CP55940 from CB2 receptor (unknown origin) | B | 4.02 | pKi | 95600 | nM | Ki | J Nat Prod (2019) 82: 636-646 [PMID:30816712] |
| DNA repair protein RAD52 homolog in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2362978] [UniProtKB: P43351] | ||||||||
| ChEMBL | Inhibition of RAD52 (unknown origin) assessed as effect on RAD52-mediated annealing of complementary oligonucleotides using T-28 ssDNA substrate by FRET assay | B | 4.7 | pIC50 | 20000 | nM | IC50 | US-20180209956-A1. HTS Assay for Identifying Small Molecule Inhibitors of RAD52 and Uses of Identified Small Molecule Inhibitors for Treatment and Prevention of BRCA-Deficient Malignancies (2018) |
| ChEMBL | Inhibition of RAD52 (unknown origin) assessed as reduction in RAD52-ssDNA interaction using Cy3-dT30-Cy5 ssDNA by FRET assay | B | 6.59 | pIC50 | 255 | nM | IC50 | US-20180209956-A1. HTS Assay for Identifying Small Molecule Inhibitors of RAD52 and Uses of Identified Small Molecule Inhibitors for Treatment and Prevention of BRCA-Deficient Malignancies (2018) |
| dual specificity tyrosine phosphorylation regulated kinase 1A/Dual-specificity tyrosine-phosphorylation regulated kinase 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2292] [GtoPdb: 2009] [UniProtKB: Q13627] | ||||||||
| ChEMBL | Inhibition of DYRK1A (unknown origin) using HT-497 as substrate preincubated with compound followed by substrate addition and measured after 30 mins in the presence of ATP by ELISA analysis | B | 6.28 | pIC50 | 523 | nM | IC50 | Bioorg Med Chem Lett (2022) 64: 128675-128675 [PMID:35292341] |
| ELAV-like protein 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105924] [UniProtKB: Q14576] | ||||||||
| ChEMBL | Inhibition of ELAV3 (unknown origin)-artificial ARE complex formation after 30 mins in the presence of biotin-labeled RNA probe by chemiluminescence nucleic acid detection method | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (2017) 60: 8257-8267 [PMID:28587461] |
| Enoyl-[acyl-carrier-protein] reductase in Escherichia coli (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1857] [UniProtKB: P0AEK4] | ||||||||
| ChEMBL | Inhibition of Escherichia coli ENR | B | 5 | pIC50 | 10000 | nM | IC50 | J Med Chem (2007) 50: 765-775 [PMID:17263522] |
| Enoyl-acyl-carrier protein reductase in Plasmodium falciparum (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4150] [UniProtKB: Q965D5] | ||||||||
| ChEMBL | Inhibition of Plasmodium falciparum ENR using NADH substrate | B | 6.54 | pKi | 291 | nM | Ki | J Med Chem (2007) 50: 765-775 [PMID:17263522] |
| ChEMBL | Inhibition of Plasmodium falciparum ENR using crotonyl-CoA substrate | B | 6.99 | pKi | 102 | nM | Ki | J Med Chem (2007) 50: 765-775 [PMID:17263522] |
| ChEMBL | Inhibition of Plasmodium falciparum ENR in presence of triclosan | B | 7.8 | pKi | 16 | nM | Ki | J Med Chem (2007) 50: 765-775 [PMID:17263522] |
| ChEMBL | Inhibition of Plasmodium falciparum ENR | B | 6.3 | pIC50 | 500 | nM | IC50 | J Med Chem (2007) 50: 765-775 [PMID:17263522] |
| ChEMBL | Inhibition of FabI | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (2006) 49: 3345-3353 [PMID:16722653] |
| Fatty acid synthase in Plasmodium falciparum (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4512] [UniProtKB: Q965D7] | ||||||||
| ChEMBL | Inhibition of FabZ | B | 6.4 | pIC50 | 400 | nM | IC50 | J Med Chem (2006) 49: 3345-3353 [PMID:16722653] |
| Fatty acid synthase in Chicken (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795136] [UniProtKB: P12276] | ||||||||
| ChEMBL | Inhibition of chicken liver FASN ketoreductase activity | B | 4.17 | pIC50 | 68000 | nM | IC50 | J Med Chem (2011) 54: 5615-5638 [PMID:21726077] |
| ChEMBL | Inhibition of chicken liver FASN after 3 hrs | B | 4.38 | pIC50 | 42000 | nM | IC50 | J Med Chem (2011) 54: 5615-5638 [PMID:21726077] |
| Genome polyprotein in Zika virus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523954] [UniProtKB: A0A024AXB9] | ||||||||
| ChEMBL | Inhibition of Zika virus NS2B (1421 to 1469 residues) - NS3 (1503 to 1688 residues) expressed in Escherichia coli BL21(DE3) cells using Dabcyl-KTSAVLQSGFRKME-Edans as substrate after 11 mins by FRET assay | B | 4.05 | pIC50 | 89000 | nM | IC50 | J Med Chem (2020) 63: 470-489 [PMID:31549836] |
| Glucose-6-phosphate 1-dehydrogenase in Saccharomyces cerevisiae S288c (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075249] [UniProtKB: P11412] | ||||||||
| ChEMBL | Inhibition of yeast G6PD | B | 6.74 | pIC50 | 180 | nM | IC50 | Bioorg Med Chem (2008) 16: 3580-3586 [PMID:18313308] |
| MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581] | ||||||||
| ChEMBL | Inhibition of MET kinase | B | 5 | pIC50 | 10000 | nM | IC50 | J Med Chem (2009) 52: 6543-6545 [PMID:19839593] |
| Human immunodeficiency virus type 1 reverse transcriptase in Human immunodeficiency virus 1 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL247] [UniProtKB: Q72547] | ||||||||
| ChEMBL | Inhibition of polymerization in wild type HIV-1 RT with poly rC/dG12-18 template primer and [3H]dGTP | B | 6.12 | pIC50 | 760 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 2763-2767 [PMID:11591519] |
| mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539] | ||||||||
| ChEMBL | Inhibition of p38alpha after 1 hr by ELISA | B | 5.83 | pIC50 | 1470 | nM | IC50 | J Nat Prod (2010) 73: 2035-2041 [PMID:21080642] |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum NF54 | F | 4.4 | pIC50 | 40000 | nM | IC50 | J Med Chem (2006) 49: 3345-3353 [PMID:16722653] |
| ChEMBL | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 | F | 4.95 | pIC50 | 11300 | nM | IC50 | J Med Chem (2006) 49: 3345-3353 [PMID:16722653] |
| proteasome 20S subunit beta 5/Proteasome Macropain subunit MB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4662] [GtoPdb: 2406] [UniProtKB: P28074] | ||||||||
| ChEMBL | Inhibition of chymotrypsin-like activity of purified human 20S proteasome assessed as decrease in AMC hydrolysis using Suc-Leu-Leu-Val-Tyr-AMC as substrate incubated for 30 mins by fluorometric analysis | B | 6.71 | pIC50 | 194 | nM | IC50 | Eur J Med Chem (2019) 167: 291-311 [PMID:30776692] |
| 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 | 4.33 | pIC50 | 47200 | 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 | 4.33 | pIC50 | 46773.51 | nM | IC50 | RSC Med Chem (2023) 14: 890-898 [PMID:37252098] |
| SYNJ1/Synaptojanin-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523136] [GtoPdb: 1461] [UniProtKB: O43426] | ||||||||
| ChEMBL | Inhibition of C-Myc/DDK-tagged human recombinant SYNJ1 expressed in HEK293T cells assessed as reduction in 5'-phosphatase activity incubated for 8 mins using fluorescently-labeled PI(3,4)P2 probe and Tapp1 PH-domain as detector protein by fluorescence polarization competitive assay | B | 4.8 | pIC50 | <=15900 | nM | IC50 | US-20170042857-A1. Synaptojanin-2 inhibitors for use in the treatment of cancer (2017) |
| ChEMBL | Inhibition of C-Myc/DDK-tagged human recombinant SYNJ1 expressed in HEK293T cells assessed as reduction in 5'-phosphatase activity incubated for 8 mins using fluorescently-labeled PI(3,4)P2 probe and Tapp1 PH-domain as detector protein by fluorescence polarization competitive assay | B | 4.8 | pIC50 | <=15900 | nM | IC50 | WO-2015079413-A2. Synaptojanin-2 inhibitors and uses thereof (2015) |
| SYNJ2/Synaptojanin-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523129] [GtoPdb: 1462] [UniProtKB: O15056] | ||||||||
| ChEMBL | Inhibition of C-Myc/DDK-tagged human recombinant SYNJ2 expressed in HEK293T cells assessed as reduction in 5'-phosphatase activity incubated for 8 mins using fluorescently-labeled PI(3,4)P2 probe and Tapp1 PH-domain as detector protein by fluorescence polarization competitive assay | B | 5.54 | pIC50 | 2880 | nM | IC50 | US-20170042857-A1. Synaptojanin-2 inhibitors for use in the treatment of cancer (2017) |
| ChEMBL | Inhibition of C-Myc/DDK-tagged human recombinant SYNJ2 expressed in HEK293T cells assessed as reduction in 5'-phosphatase activity incubated for 8 mins using fluorescently-labeled PI(3,4)P2 probe and Tapp1 PH-domain as detector protein by fluorescence polarization competitive assay | B | 5.54 | pIC50 | 2880 | nM | IC50 | WO-2015079413-A2. Synaptojanin-2 inhibitors and uses thereof (2015) |
| ChEMBL | Inhibition of recombinant full length C-Myc/DDK-tagged human SYNJ2 expressed in HEK293T cells using PI(3,4,5)P3 as substrate incubated for 8 mins assessed as hydrolysis of PI(3,4,5)P3 to PI(3,4)P2 by fluorescence polarization assay | B | 5.54 | pIC50 | 2880 | nM | IC50 | US-20170165285-A1. Methods of preventing tumor metastasis, treating and prognosing cancer and identifying agents which are putative metastasis inhibitors (2017) |
| TAS2R39 in Human [GtoPdb: 675] [UniProtKB: P59534] | ||||||||
| GtoPdb | - | - | 4.67 | pEC50 | 21300 | nM | EC50 | Biosci Biotechnol Biochem (2014) 78: 1753-6 [PMID:25273142] |
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]
