ChEMBL ligand: CHEMBL45068 (2',4,4',6'-Tetrahydroxydihydrochalcone, 2',4,4',6'-Tetrahydroxy-Dihydrochalcone, Phloretin)
Estrogen receptor-α/Estrogen receptor alpha in Human [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372] There should be some charts here, you may need to enable JavaScript!
Glucose transporter 1/Glucose transporter in Human [ChEMBL: CHEMBL2535] [GtoPdb: 875] [UniProtKB: P11166] There should be some charts here, you may need to enable JavaScript!
Monocarboxylate transporter 1 in Rat [ChEMBL: CHEMBL2073709] [GtoPdb: 988] [UniProtKB: P53987] There should be some charts here, you may need to enable JavaScript!
Monocarboxylate transporter 2 in Rat [ChEMBL: CHEMBL2073718] [GtoPdb: 990] [UniProtKB: Q63344] There should be some charts here, you may need to enable JavaScript!
Monocarboxylate transporter 4 in Human [ChEMBL: CHEMBL2073663] [GtoPdb: 989] [UniProtKB: O15427] There should be some charts here, you may need to enable JavaScript!
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 [ChEMBL: CHEMBL2094258] [GtoPdb: 3281, 3282, 3280] [UniProtKB: P19838, Q00653, Q04206] There should be some charts here, you may need to enable JavaScript!
Pancreatic triacylglycerol lipase in Pig [ChEMBL: CHEMBL1687677] [UniProtKB: P00591] There should be some charts here, you may need to enable JavaScript!
Plasmodium falciparum [ChEMBL: CHEMBL364] There should be some charts here, you may need to enable JavaScript!
Sodium/glucose cotransporter 1 in Human [ChEMBL: CHEMBL4979] [GtoPdb: 915] [UniProtKB: P13866] There should be some charts here, you may need to enable JavaScript!
Sodium/glucose cotransporter 2 in Human [ChEMBL: CHEMBL3884] [GtoPdb: 916] [UniProtKB: P31639] There should be some charts here, you may need to enable JavaScript!
solute carrier family 9 member B2/Sodium/hydrogen exchanger 9B2 in Human [ChEMBL: CHEMBL5209631] [GtoPdb: 2575] [UniProtKB: Q86UD5] There should be some charts here, you may need to enable JavaScript!
Solute carrier family 28 member 3 in Human [ChEMBL: CHEMBL5707] [GtoPdb: 1116] [UniProtKB: Q9HAS3] There should be some charts here, you may need to enable JavaScript!
transthyretin/Transthyretin in Human [ChEMBL: CHEMBL3194] [GtoPdb: 2851] [UniProtKB: P02766] There should be some charts here, you may need to enable JavaScript!
TAS2R14 in Human [GtoPdb: 668] [UniProtKB: Q9NYV8] There should be some charts here, you may need to enable JavaScript!
TAS2R39 in Human [GtoPdb: 675] [UniProtKB: P59534] There should be some charts here, you may need to enable JavaScript!
ClC-3 in Human [GtoPdb: 702] [UniProtKB: P51790] There should be some charts here, you may need to enable JavaScript!
Sodium-dependent vitamin C transporter 1 in Human [GtoPdb: 1041] [UniProtKB: Q9UHI7] 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
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]