phloretin [Ligand Id: 4285] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL45068 (2',4,4',6'-Tetrahydroxydihydrochalcone, 2',4,4',6'-Tetrahydroxy-Dihydrochalcone, Phloretin)
  • Estrogen receptor-α/Estrogen receptor alpha in Human [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372]
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  • Glucose transporter 1/Glucose transporter in Human [ChEMBL: CHEMBL2535] [GtoPdb: 875] [UniProtKB: P11166]
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  • Sodium/glucose cotransporter 1 in Human [ChEMBL: CHEMBL4979] [GtoPdb: 915] [UniProtKB: P13866]
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  • Sodium/glucose cotransporter 2 in Human [ChEMBL: CHEMBL3884] [GtoPdb: 916] [UniProtKB: P31639]
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  • Solute carrier family 28 member 3 in Human [ChEMBL: CHEMBL5707] [GtoPdb: 1116] [UniProtKB: Q9HAS3]
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  • TAS2R14 in Human [GtoPdb: 668] [UniProtKB: Q9NYV8]
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  • TAS2R39 in Human [GtoPdb: 675] [UniProtKB: P59534]
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  • ClC-3 in Human [GtoPdb: 702] [UniProtKB: P51790]
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  • Sodium-dependent vitamin C transporter 1 in Human [GtoPdb: 1041] [UniProtKB: Q9UHI7]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Estrogen receptor-α/Estrogen receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372]
ChEMBL Binding affinity to human estrogen receptor assessed as decrease in estradiol-dependent beta-galactosidase activity B 6.52 pIC50 300 nM IC50 Bioorg Med Chem Lett (2013) 23: 6923-6927 [PMID:24200808]
Glucose transporter 1/Glucose transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2535] [GtoPdb: 875] [UniProtKB: P11166]
ChEMBL Inhibition of GLUT1 in human H1299 cells assessed as inhibition of 2-deoxy-D-[3H]-glucose uptake incubated for 15 mins prior to 2-deoxy-D-[3H]-glucose addition measured after 30 mins by liquid scintillation counting analysis B 4.67 pIC50 21400 nM IC50 Bioorg Med Chem Lett (2013) 23: 6923-6927 [PMID:24200808]
Monocarboxylate transporter 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073709] [GtoPdb: 988] [UniProtKB: P53987]
ChEMBL TP_TRANSPORTER: inhibition of lactate uptake in Xenopus laevis oocytes F 4.55 pIC50 28000 nM IC50 Biochem J (1999) 341: 529-535 [PMID:10417314]
Monocarboxylate transporter 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073718] [GtoPdb: 990] [UniProtKB: Q63344]
ChEMBL TP_TRANSPORTER: inhibition of lactate uptake in Xenopus laevis oocytes F 4.85 pIC50 14000 nM IC50 Biochem J (1999) 341: 529-535 [PMID:10417314]
Monocarboxylate transporter 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073663] [GtoPdb: 989] [UniProtKB: O15427]
ChEMBL TP_TRANSPORTER: inhibition of L-Lactate uptake (L-Lactate:30mM) in Xenopus laevis oocytes F 4.39 pIC50 41000 nM IC50 J Physiol (2000) 529: 285-293 [PMID:11101640]
Nuclear factor NF-kappa-B complex in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094258] [UniProtKB: P19838, Q00653, Q04206]
ChEMBL Inhibition of NF-kappaB transactivation in TNF-alpha-stimulated human K562 cells preincubated for 2 hrs followed by TNF-alpha challenge measured after 6 hrs by dual luciferase reporter gene assay B 4.39 pIC50 41000 nM IC50 Bioorg Med Chem (2014) 22: 3008-3015 [PMID:24775915]
Pancreatic triacylglycerol lipase in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1687677] [UniProtKB: P00591]
ChEMBL Inhibition of porcine pancreatic lipase using p-nitrophenyl butyrate as substrate pretreated for 15 mins followed by substrate addition measured after 15 mins by spectrophotometric method B 4.3 pIC50 50400 nM IC50 Bioorg Med Chem Lett (2017) 27: 4889-4892 [PMID:28958622]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay F 4.8 pIC50 15848.93 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay F 4.8 pIC50 15848.93 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
Sodium/glucose cotransporter 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4979] [GtoPdb: 915] [UniProtKB: P13866]
ChEMBL Binding affinity against Sodium/glucose co-transporter of isolated renal brush border membranes. B 4.07 pKi 86000 nM Ki J Med Chem (2000) 43: 1692-1698 [PMID:10794686]
Sodium/glucose cotransporter 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3884] [GtoPdb: 916] [UniProtKB: P31639]
ChEMBL Inhibition of human SGLT2 expressed in HEK293 cells assessed as reduction in 2-deoxyglucose uptake pretreated for 10 mins followed by 2-deoxyglucose addition in presence of sodium buffer measured after 1 hr by resazurin dye based fluorescence assay B 4.74 pIC50 18300 nM IC50 J Med Chem (2017) 60: 568-579 [PMID:28098449]
Solute carrier family 28 member 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5707] [GtoPdb: 1116] [UniProtKB: Q9HAS3]
ChEMBL Binding affinity to human recombinant CNT3 expressed in pig PK15NTD cells assessed as [3H]uridine uptake by beta-scintillation counter B 4.49 pKi 32280 nM Ki Bioorg Med Chem Lett (2009) 19: 917-921 [PMID:19097778]
transthyretin/Transthyretin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3194] [GtoPdb: 2851] [UniProtKB: P02766]
ChEMBL Stabilization of TTR V30M mutant (unknown origin) assessed as inhibition of protein-mediated amyloid fibril formation B 5.09 pKd 8100 nM Kd J Med Chem (2020) 63: 14228-14242 [PMID:32914975]
TAS2R14 in Human [GtoPdb: 668] [UniProtKB: Q9NYV8]
GtoPdb - - 4.52 pEC50 30200 nM EC50 J Agric Food Chem (2013) 61: 10454-66 [PMID:24117141]
TAS2R39 in Human [GtoPdb: 675] [UniProtKB: P59534]
GtoPdb - - 4.38 pEC50 41300 nM EC50 J Agric Food Chem (2013) 61: 10454-66 [PMID:24117141]
ClC-3 in Human [GtoPdb: 702] [UniProtKB: P51790]
GtoPdb - - 4.5 pIC50 30000 nM IC50
Sodium-dependent vitamin C transporter 1 in Human [GtoPdb: 1041] [UniProtKB: Q9UHI7]
GtoPdb - - 4.19 pKi 65000 nM Ki Nature (1999) 399: 70-5 [PMID:10331392]

ChEMBL data shown on this page come from version 32:

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]