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 |
|---|---|---|---|---|---|---|---|---|
| CYP19A1/Cytochrome P450 19A1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1978] [GtoPdb: 1362] [UniProtKB: P11511] | ||||||||
| ChEMBL | Inhibition of human aromatase using ASD as substrate pre-incubated for 5 mins followed by substrate addition and measured after 16 hrs by UV/vis-spectrophotometry | B | 5.58 | pIC50 | 2600.16 | nM | IC50 | Eur J Med Chem (2017) 137: 365-438 [PMID:28622580] |
| 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 kappa B subunit 1/nuclear factor kappa B subunit 2/RELA proto-oncogene, NF-kB subunit/Nuclear factor NF-kappa-B complex in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094258] [GtoPdb: 3281, 3282, 3280] [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 9 member B2/Sodium/hydrogen exchanger 9B2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5209631] [GtoPdb: 2575] [UniProtKB: Q86UD5] | ||||||||
| ChEMBL | Inhibition of the Sodium/Hydrogen Exchanger-Like Domain-Containing Protein 2 (NHA2, SLC9B2) as assessed by a sensor pH-sensitive genetically encoded fluorescent sensor (pHAxensor) in HEK-293 cells stably transfected with SLC9B2 (PubChem AID: 1794821) | F | 4.05 | pIC50 | 90000 | nM | IC50 | pH biosensor based assay for SLC9B2 using HEK-293 SLC9B2 OE cells |
| 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 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]
