phlorizin [Ligand Id: 4757] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL245067 (Phloridzin)
  • epoxide hydrolase 2/Epoxide hydratase in Human [ChEMBL: CHEMBL2409] [GtoPdb: 2970] [UniProtKB: P34913]
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  • Low affinity sodium-glucose cotransporter in Human [ChEMBL: CHEMBL1770047] [GtoPdb: 917] [UniProtKB: Q9NY91]
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  • Sodium/nucleoside cotransporter 2 in Human [ChEMBL: CHEMBL5780] [GtoPdb: 1115] [UniProtKB: O43868]
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  • Solute carrier family 28 member 3 in Human [ChEMBL: CHEMBL5707] [GtoPdb: 1116] [UniProtKB: Q9HAS3]
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  • SGLT6 in Human [GtoPdb: 925] [UniProtKB: Q8WWX8]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
epoxide hydrolase 2/Epoxide hydratase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2409] [GtoPdb: 2970] [UniProtKB: P34913]
ChEMBL Inhibition of sEH (unknown origin) assessed as substrate PHOME hydrolysis after 1 hr by fluorescence method B 4.38 pIC50 41720 nM IC50 Bioorg. Med. Chem. Lett. (2014) 24: 1895-1900 [PMID:24679441]
Low affinity sodium-glucose cotransporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1770047] [GtoPdb: 917] [UniProtKB: Q9NY91]
ChEMBL Inhibition of human SGLT2 expressed in CHO cells assessed as [14C]AMG uptake after 45 mins B 7.8 pIC50 16 nM IC50 Bioorg. Med. Chem. (2011) 19: 5334-5341 [PMID:21873071]
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 6.74 pKi 180 nM Ki J. Med. Chem. (2000) 43: 1692-1698 [PMID:10794686]
ChEMBL Inhibition of human SGLT1 expressed in COS7 cells assessed as reduction of [14C]-AMG uptake B 6.27 pIC50 536 nM IC50 Bioorg. Med. Chem. (2012) 20: 6598-6612 [PMID:23062824]
ChEMBL Inhibition of SGLT1 B 6.48 pIC50 330 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 2472-2475 [PMID:21398124]
ChEMBL Inhibition of human SGLT1 expressed in CHOK1 cells assessed as inhibition of glucose uptake B 6.61 pIC50 246 nM IC50 J. Med. Chem. (2010) 53: 3247-3261 [PMID:20302302]
ChEMBL Inhibition of human SGLT1 expressed in HEK293 cells assessed as inhibition of [14C]alpha-methylglucopyranoside uptake B 6.68 pIC50 210 nM IC50 J. Med. Chem. (2009) 52: 6201-6204 [PMID:19785435]
ChEMBL Inhibition of human SGLT1 B 6.68 pIC50 210 nM IC50 Eur J Med Chem (2019) 184: 111773-111773 [PMID:31630053]
ChEMBL Inhibition of human SGLT1 expressed in COS1 cells assessed as [14C]methyl-alpha-D-glucopyranoside uptake B 6.7 pIC50 200 nM IC50 Bioorg. Med. Chem. (2007) 15: 3445-3449 [PMID:17374486]
ChEMBL Inhibition of human SGLT1 expressed in CHO-K1 cells by [14C]AMG uptake assay B 6.72 pIC50 190 nM IC50 Bioorg. Med. Chem. (2012) 20: 4117-4127 [PMID:22652255]
ChEMBL Inhibition of human SGLT1 expressed in CHO cells assessed as [14C]AMG uptake after 45 mins B 6.72 pIC50 190 nM IC50 Bioorg. Med. Chem. (2011) 19: 5334-5341 [PMID:21873071]
ChEMBL Inhibition of human SGLT1 expressed in CHO cells assessed as inhibition of sodium-dependent [14C]methyl-alpha-D-glucopyranoside uptake after 45 mins B 6.73 pIC50 185 nM IC50 J. Med. Chem. (2012) 55: 7828-7840 [PMID:22889351]
ChEMBL Inhibition of SGLT1 (unknown origin) expressed in HEK293 cells using 2-NBDG as substrate incubated for 30 mins prior to substrate addition measured after 30 mins by nonradioactive fluorescence glucose uptake assay B 7.22 pIC50 60.7 nM IC50 Bioorg. Med. Chem. Lett. (2014) 24: 1528-1531 [PMID:24556379]
ChEMBL Inhibition of human SGLT1 expressed in CHO cells assessed as inhibition of [14C]AMG accumulation B 6.48 pEC50 330 nM EC50 J. Med. Chem. (2008) 51: 1145-1149 [PMID:18260618]
ChEMBL Inhibition of human SGLT1 expressed in CHO cells assessed as sodium-dependent [14C]-alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counting B 6.7 pEC50 197.4 nM EC50 J. Med. Chem. (2011) 54: 166-178 [PMID:21128592]
ChEMBL Inhibition of human SGLT1 expressed in CHO-K1 cells assessed as reduction in [14C]AMG uptake after 120 mins by scintillation counting method B 6.82 pEC50 153 nM EC50 Bioorg. Med. Chem. (2016) 24: 2242-2250 [PMID:27075813]
ChEMBL Inhibition of human SGLT1 expressed in CHO-K1 cells assessed as inhibition of [14C]-AMG uptake up to 120 mins by scintillation counting method B 6.92 pEC50 120 nM EC50 Bioorg. Med. Chem. (2013) 21: 6282-6291 [PMID:24071445]
Sodium/glucose cotransporter 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5374] [GtoPdb: 915] [UniProtKB: P53790]
ChEMBL Inhibition of rat SGLT1 expressed in COS7 cells assessed as reduction of [14C]-AMG uptake B 6.46 pIC50 350 nM IC50 Bioorg. Med. Chem. (2012) 20: 6598-6612 [PMID:23062824]
Sodium/glucose cotransporter 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3884] [GtoPdb: 916] [UniProtKB: P31639]
ChEMBL Inhibition of human kidney SGLT2 assessed as renal glucose reabsorption B 7.73 pKi 18.6 nM Ki J. Med. Chem. (2009) 52: 1785-1794 [PMID:19243175]
ChEMBL Inhibition of alpha-D-[U-14C]glucopyranoside uptake at human SGLT2 expressed in african green monkey COS1 cells after 30 mins by liquid scintillation counting B 4 pIC50 100000 nM IC50 Bioorg. Med. Chem. (2010) 18: 2152-2158 [PMID:20189404]
ChEMBL Inhibition of human SGLT2 expressed in CHO cells assessed as [14C]alpha-methyl-D-glucopyranoside uptake by fluorescence polarization assay B 6.12 pIC50 752 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 4944-4947 [PMID:18755586]
ChEMBL Inhibition of human SGLT2 expressed in Xenopus oocytes assessed as reduction in [14C]AMG uptake after 1 hr by liquid scintillation counting method B 6.8 pIC50 160 nM IC50 J Med Chem (2020) 63: 3834-3867 [PMID:31774679]
ChEMBL Inhibition of human SGLT2 expressed in COS1 cells assessed as [14C]methyl-alpha-D-glucopyranoside uptake B 7 pIC50 100 nM IC50 Bioorg. Med. Chem. (2007) 15: 3445-3449 [PMID:17374486]
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 7.17 pIC50 67.3 nM IC50 J Med Chem (2017) 60: 568-579 [PMID:28098449]
ChEMBL Inhibition of SGLT2 (unknown origin) expressed in HEK293 cells using 2-NBDG as substrate incubated for 30 mins prior to substrate addition measured after 30 mins by nonradioactive fluorescence glucose uptake assay B 7.23 pIC50 58.6 nM IC50 Bioorg. Med. Chem. Lett. (2014) 24: 1528-1531 [PMID:24556379]
ChEMBL Inhibition of human SGLT2 expressed in COS7 cells assessed as reduction of [14C]-AMG uptake B 7.42 pIC50 38 nM IC50 Bioorg. Med. Chem. (2012) 20: 6598-6612 [PMID:23062824]
ChEMBL Inhibition of SGLT2 B 7.44 pIC50 36 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 2472-2475 [PMID:21398124]
ChEMBL Inhibition of human SGLT2 B 7.46 pIC50 34.6 nM IC50 Eur J Med Chem (2019) 184: 111773-111773 [PMID:31630053]
ChEMBL Inhibition of human SGLT2 expressed in CHOK1 cells assessed as inhibition of glucose uptake B 7.56 pIC50 27.8 nM IC50 J. Med. Chem. (2010) 53: 3247-3261 [PMID:20302302]
ChEMBL Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of sodium-dependent [14C]methyl-alpha-D-glucopyranoside uptake after 45 mins B 7.79 pIC50 16.4 nM IC50 J. Med. Chem. (2012) 55: 7828-7840 [PMID:22889351]
ChEMBL Inhibition of human SGLT2 expressed in CHO-K1 cells by [14C]AMG uptake assay B 7.8 pIC50 16 nM IC50 Bioorg. Med. Chem. (2012) 20: 4117-4127 [PMID:22652255]
ChEMBL Inhibition of human SGLT2 expressed in Xenopus oocyte assessed as [14C]alpha-methyl glucopyranoside uptake B 6.8 pEC50 160 nM EC50 Bioorg. Med. Chem. Lett. (2008) 18: 4770-4773 [PMID:18707880]
ChEMBL Inhibition of human SGLT2 expressed in CHO-K1 cells assessed as reduction in [14C]AMG uptake after 120 mins by scintillation counting method B 6.91 pEC50 123 nM EC50 Bioorg. Med. Chem. (2016) 24: 2242-2250 [PMID:27075813]
ChEMBL Inhibition of human SGLT2 expressed in CHO cells assessed as sodium-dependent [14C]-alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counting B 6.97 pEC50 108 nM EC50 J. Med. Chem. (2011) 54: 166-178 [PMID:21128592]
ChEMBL Inhibition of human SGLT2 expressed in CHO cells assessed as reduction in [14C]AMG uptake after 1 hr by microbeta counting method B 7.1 pEC50 79 nM EC50 Eur J Med Chem (2018) 143: 611-620 [PMID:29216560]
ChEMBL Inhibition of human SGLT2 expressed in CHO-K1 cells assessed as inhibition of [14C]-AMG uptake up to 120 mins by scintillation counting method B 7.11 pEC50 77 nM EC50 Bioorg. Med. Chem. (2013) 21: 6282-6291 [PMID:24071445]
ChEMBL Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of [14C]AMG accumulation B 7.45 pEC50 35.6 nM EC50 J. Med. Chem. (2008) 51: 1145-1149 [PMID:18260618]
ChEMBL Inhibition of human SGLT2 expressed in CHO cells assessed as intracellular accumulation of [14C]alpha-methyl glucopyranoside B 7.46 pEC50 35 nM EC50 Bioorg. Med. Chem. Lett. (2008) 18: 4770-4773 [PMID:18707880]
ChEMBL Inhibition of human kidney SGLT2 assessed as renal glucose reabsorption B 7.46 pEC50 35 nM EC50 J. Med. Chem. (2009) 52: 1785-1794 [PMID:19243175]
Sodium/glucose cotransporter 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4316] [GtoPdb: 916] [UniProtKB: P53792]
ChEMBL Inhibition of rat SGLT2 expressed in COS7 cells assessed as reduction of [14C]-AMG uptake B 7.02 pIC50 96 nM IC50 Bioorg. Med. Chem. (2012) 20: 6598-6612 [PMID:23062824]
Sodium/nucleoside cotransporter 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5780] [GtoPdb: 1115] [UniProtKB: O43868]
ChEMBL Inhibition of human CNT2 B 4 pIC50 100000 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 917-921 [PMID:19097778]
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 4.8 pKi 16000 nM Ki Bioorg. Med. Chem. Lett. (2009) 19: 917-921 [PMID:19097778]
SGLT6 in Human [GtoPdb: 925] [UniProtKB: Q8WWX8]
GtoPdb - - 4.1 pKi 76000 nM Ki J Biol Chem (2002) 277: 35219-24 [PMID:12133831]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]