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) |
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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 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]
