phlorizin [Ligand Id: 4757] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL245067 (Phloridzin) |
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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 alpha-D-[U-14C]glucopyranoside uptake at human SGLT1 expressed in african green monkey COS1 cells after 30 mins by liquid scintillation counting | B | 3.7 | pIC50 | 200000 | nM | IC50 | Bioorg Med Chem (2010) 18: 2152-2158 [PMID:20189404] |
| 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 SGLT1 (unknown origin) | B | 6.68 | pIC50 | 210 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127387-127387 [PMID:32738984] |
| 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 SGLT1 (unknown origin) | B | 6.72 | pIC50 | 190 | nM | IC50 | J Med Chem (2023) 66: 12536-12543 [PMID:37608596] |
| 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-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 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 SGLT2 (unknown origin) | B | 7.46 | pIC50 | 34.6 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127387-127387 [PMID:32738984] |
| 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 SGLT2 (unknown origin) | B | 7.68 | pIC50 | 21 | nM | IC50 | J Med Chem (2023) 66: 12536-12543 [PMID:37608596] |
| 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 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]
