phlorizin [Ligand Id: 4757] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL245067 (Phloridzin) |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
|
There should be some charts here, you may need to enable JavaScript!
|
| 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 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 | 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 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 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 33:
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]
