ChEMBL ligand: CHEMBL429910 (BMS-512148, Dapagliflozin, LYN-045)
Low affinity sodium-glucose cotransporter in Human [ChEMBL: CHEMBL1770047] [GtoPdb: 917] [UniProtKB: Q9NY91] 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] Sodium/glucose cotransporter 2 in Rat [ChEMBL: CHEMBL4316] [GtoPdb: 916] [UniProtKB: P53792] There should be some charts here, you may need to enable JavaScript!
SGLT6/Sodium/myo-inositol cotransporter 2 in Human [ChEMBL: CHEMBL1744524] [GtoPdb: 925] [UniProtKB: Q8WWX8] 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
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 using methyl-alpha-D-glucopyranoside by liquid scintillation counting	B	8.87	pIC50	1.35	nM	IC50	Bioorg Med Chem Lett (2011) 21: 3759-3763 [PMID:21592794]
Sodium/glucose cotransporter 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4979] [GtoPdb: 915] [UniProtKB: P13866]
ChEMBL	Inhibition of human full length SGLT1 expressed in NIH3T3 cells measured after 1 hr in presence of [14C]-methyl-alpha -D-glucopyranoside by scintillation counter method	B	4.91	pIC50	12300	nM	IC50	Eur J Med Chem (2019) 180: 398-416 [PMID:31325786]
ChEMBL	Inhibition of full length human SGLT1 assessed as methyl-alpha-D-[U-14C]glucopyranoside uptake after 2 hrs by cell-based topcount scintillation counting analysis	B	5.5	pIC50	3140	nM	IC50	J Med Chem (2014) 57: 1236-1251 [PMID:24456245]
ChEMBL	Inhibition of human SGLT1 expressed in human 293 cells assessed as inhibition of [14C]-methyl-alpha-D-glucopyranoside uptake after 1.5 hrs by scintillation counting in presence of 25 % human plasma	B	5.51	pIC50	3100	nM	IC50	Bioorg Med Chem Lett (2011) 21: 4465-4470 [PMID:21737266]
ChEMBL	Inhibition of human SGLT1 expressed in HEK293 cells assessed as decrease in [14C]-AMG uptake preincubated for 10 mins followed by [14C]-AMG addition and measured after 2 hrs by liquid scintillation counting method	B	5.74	pIC50	1830	nM	IC50	Bioorg Med Chem (2018) 26: 3947-3952 [PMID:29954682]
ChEMBL	Inhibition of human SGLT1	B	5.86	pIC50	1391	nM	IC50	Eur J Med Chem (2019) 184: 111773-111773 [PMID:31630053]
ChEMBL	Inhibition of human SGLT1 expressed in CHO cells assessed as inhibition of sodium-dependent methyl-alpha-D-[U-14C]glucopyranoside uptake after 2 hrs	B	5.92	pIC50	1200	nM	IC50	Bioorg Med Chem Lett (2010) 20: 1569-1572 [PMID:20149653]
ChEMBL	Inhibition of human SGLT1 expressed in CHOK1 cells assessed as inhibition of [14C]-AMG uptake after 3 hrs by microbeta scintillation counting analysis	B	6.05	pIC50	891	nM	IC50	Bioorg Med Chem (2014) 22: 3414-3422 [PMID:24842618]
ChEMBL	Inhibition of human SGLT1 transfected in COS-7 cells assessed as AMG uptake after 2 hrs by scintillation counting	B	6.05	pIC50	890	nM	IC50	Bioorg Med Chem Lett (2009) 19: 6877-6881 [PMID:19896374]
ChEMBL	Inhibition of human SGLT1 expressed in african green monkey COS7 cells assessed as inhibition of [14C]alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counting	B	6.05	pIC50	890	nM	IC50	Bioorg Med Chem (2010) 18: 4422-4432 [PMID:20576578]
ChEMBL	Inhibition of human SGLT1 expressed in african green monkey COS7 cells assessed as methyl-alpha-D-[U-14C]glucopyranoside uptake by scintillation counting	B	6.05	pIC50	885	nM	IC50	Bioorg Med Chem Lett (2009) 19: 5632-5635 [PMID:19700318]
ChEMBL	Inhibition of human SGLT1 expressed in HEK293 cells assessed as inhibition of [14C]alpha-methylglucopyranoside uptake	B	6.09	pIC50	810	nM	IC50	J Med Chem (2009) 52: 6201-6204 [PMID:19785435]
ChEMBL	Uptake Assay: A cDNA clone expressing human SGLT1/SGLT2 was bought from GenerScript. Having the sequence information, it was built into pcDNA5 carrier by using traditional molecular biology methods, and then the expression plasmids were transfected into Flp-in CHO cells by using Lipofetamin 200 liposomal transfection method. The transfected cells were screened for hygromycin resistance, and the single-cell clone was screened out through the process of gradient dilution. Having obtained the single-cell clone, the uptake assay of 14C-AMG in FLP-in CHO cells stably expressing SGLT1/SGLT2 was evaluated.Cells were seeded at a density of 3x104 cells per well, uptake assay was carried out after adherent cells were cultured overnight. At least 12 hours later of culture, cells were washed once by 150 microliters per well of the absorption solution KRH-NMG (120 mM NMG, 4.7 mM KCl, 1.2 mM MgCl2, 2.2 mM CaCl2, 10 mM HEPES, pH 7.4 with HCl). To every well that was cleaned with buffer KRH-Na+ and KRH-NMG.	B	6.1	pIC50	803	nM	IC50	US-8980829-B2. Aryl glycoside compound, preparation method and use thereof (2015)
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	6.1	pIC50	800	nM	IC50	J Med Chem (2012) 55: 7828-7840 [PMID:22889351]
ChEMBL	Inhibition of human SGLT1 expressed in CHO-K1 cells by [14C]AMG uptake assay	B	6.1	pIC50	800	nM	IC50	Bioorg Med Chem (2012) 20: 4117-4127 [PMID:22652255]
ChEMBL	Inhibition of human SGLT1 expressed in CHO cells assessed as decrease in uptake of [14C]AMG after 120 mins by TopCount method	B	6.2	pIC50	629	nM	IC50	J Med Chem (2017) 60: 4173-4184 [PMID:28447791]
GtoPdb	-	-	6.4	pIC50	370	nM	IC50	Bioorg Med Chem Lett (2011) 21: 2472-5 [PMID:21398124]
ChEMBL	Inhibition of human SGLT1	B	6.41	pIC50	392	nM	IC50	J Med Chem (2021) 64: 9786-9874 [PMID:34213340]
ChEMBL	Inhibition of human SGLT1 expressed in CHO cells assessed as inhibition of [14C]-alpha-methyl-D-glucopyranoside transport after 60 mins by scintillation counting	B	6.43	pIC50	370	nM	IC50	Bioorg Med Chem Lett (2011) 21: 2472-2475 [PMID:21398124]
ChEMBL	Inhibition of SGLT1 (unknown origin)	B	5.85	pEC50	1400	nM	EC50	J Med Chem (2020) 63: 5031-5073 [PMID:31930920]
ChEMBL	Inhibition of human SGLT1 expressed in CHO cells assessed as inhibition of [14C]AMG accumulation	B	5.86	pEC50	1390	nM	EC50	J Med Chem (2008) 51: 1145-1149 [PMID:18260618]
ChEMBL	Inhibition of human SGLT1 expressed in CHO-K1 cells incubated for 120 mins at 37 degC by [14C]-AMG uptake assay	B	6.23	pEC50	593	nM	EC50	Eur J Med Chem (2012) 55: 32-38 [PMID:22818040]
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	6.37	pEC50	428.5	nM	EC50	J Med Chem (2011) 54: 166-178 [PMID:21128592]
Sodium/glucose cotransporter 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3884] [GtoPdb: 916] [UniProtKB: P31639]
ChEMBL	Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of [14C]-alpha-methyl-D-glucopyranoside transport after 60 mins by scintillation counting in presence of 100% plasma	B	7.66	pIC50	22	nM	IC50	Bioorg Med Chem Lett (2011) 21: 2472-2475 [PMID:21398124]
ChEMBL	Inhibition of human full length SGLT2 expressed in NIH3T3 cells measured after 1 hr in presence of [14C]-methyl-alpha -D-glucopyranoside by scintillation counter method	B	8.08	pIC50	8.3	nM	IC50	Eur J Med Chem (2019) 180: 398-416 [PMID:31325786]
ChEMBL	Inhibition of human SGLT2 expressed in HEK293.ETN cells assessed as methyl-alpha-D-[U-14C]glucopyranoside uptake by scintillation counting	B	8.17	pIC50	6.7	nM	IC50	Bioorg Med Chem Lett (2009) 19: 5632-5635 [PMID:19700318]
ChEMBL	Inhibition of human SGLT2 expressed in HEK293 cells assessed as inhibition of [14C]alpha-methyl-D-glucopyranoside uptake after 1.5 hrs by liquid scintillation counting	B	8.17	pIC50	6.7	nM	IC50	Bioorg Med Chem (2010) 18: 4422-4432 [PMID:20576578]
ChEMBL	Inhibition of human SGLT2 transfected in HEK293.ETN cells assessed as AMG uptake after 1.5 hrs by scintillation counting	B	8.17	pIC50	6.7	nM	IC50	Bioorg Med Chem Lett (2009) 19: 6877-6881 [PMID:19896374]
ChEMBL	Competitive inhibition of full-length human SGLT2 expressed in CHO cells assessed as inhibition of sodium-dependent [14C]-alpha-methyl-D-glucopyranoside uptake after 2 hrs by scintillation counting	B	8.3	pIC50	5	nM	IC50	Bioorg Med Chem Lett (2015) 25: 993-997 [PMID:25650254]
ChEMBL	Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of [14C]-alpha-methyl-D-glucopyranoside transport after 60 mins by scintillation counting	B	8.4	pIC50	4	nM	IC50	Bioorg Med Chem Lett (2011) 21: 2472-2475 [PMID:21398124]
ChEMBL	Inhibition of full length human SGLT2 assessed as methyl-alpha-D-[U-14C]glucopyranoside uptake after 1.5 hrs by cell-based topcount scintillation counting analysis	B	8.49	pIC50	3.2	nM	IC50	J Med Chem (2014) 57: 1236-1251 [PMID:24456245]
ChEMBL	Inhibition of human SGLT2 expressed in african green monkey COS7 cells assessed as inhibition of [14C]-methyl-alpha-D-glucopyranoside uptake after 2 hrs by scintillation counting in presence of 25 % human plasma	B	8.49	pIC50	3.2	nM	IC50	Bioorg Med Chem Lett (2011) 21: 4465-4470 [PMID:21737266]
ChEMBL	Uptake Assay: A cDNA clone expressing human SGLT1/SGLT2 was bought from GenerScript. Having the sequence information, it was built into pcDNA5 carrier by using traditional molecular biology methods, and then the expression plasmids were transfected into Flp-in CHO cells by using Lipofetamin 200 liposomal transfection method. The transfected cells were screened for hygromycin resistance, and the single-cell clone was screened out through the process of gradient dilution. Having obtained the single-cell clone, the uptake assay of 14C-AMG in FLP-in CHO cells stably expressing SGLT1/SGLT2 was evaluated.Cells were seeded at a density of 3x104 cells per well, uptake assay was carried out after adherent cells were cultured overnight. At least 12 hours later of culture, cells were washed once by 150 microliters per well of the absorption solution KRH-NMG (120 mM NMG, 4.7 mM KCl, 1.2 mM MgCl2, 2.2 mM CaCl2, 10 mM HEPES, pH 7.4 with HCl). To every well that was cleaned with buffer KRH-Na+ and KRH-NMG.	B	8.52	pIC50	3	nM	IC50	US-8980829-B2. Aryl glycoside compound, preparation method and use thereof (2015)
ChEMBL	Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of [14C]-Glucose uptake using [14C]-methyl glucopyranoside after 60 mins by microbeta plate counting	B	8.52	pIC50	3	nM	IC50	Bioorg Med Chem Lett (2011) 21: 3774-3779 [PMID:21565497]
ChEMBL	Inhibition of human SGLT2	B	8.62	pIC50	2.4	nM	IC50	J Med Chem (2021) 64: 9786-9874 [PMID:34213340]
ChEMBL	Inhibition of human SGLT2 expressed in CHO cells assessed as decrease in uptake of [14C]AMG after 120 mins by TopCount method	B	8.82	pIC50	1.5	nM	IC50	J Med Chem (2017) 60: 4173-4184 [PMID:28447791]
ChEMBL	Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of sodium-dependent methyl-alpha-D-[U-14C]glucopyranoside uptake after 2 hrs	B	8.85	pIC50	1.4	nM	IC50	Bioorg Med Chem Lett (2010) 20: 1569-1572 [PMID:20149653]
ChEMBL	Inhibition of human SGLT2 expressed in HEK293 cells assessed as decrease in [14C]-AMG uptake preincubated for 10 mins followed by [14C]-AMG addition and measured after 2 hrs by liquid scintillation counting method	B	8.85	pIC50	1.4	nM	IC50	Bioorg Med Chem (2018) 26: 3947-3952 [PMID:29954682]
ChEMBL	Inhibition of human SGLT2 expressed in CHO cells assessed as reduction of [14C]-labeled AMG after 2 hrs by liquid scintillation counting	B	8.87	pIC50	1.35	nM	IC50	Bioorg Med Chem (2011) 19: 5468-5479 [PMID:21868239]
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	8.89	pIC50	1.3	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	8.89	pIC50	1.3	nM	IC50	Bioorg Med Chem (2012) 20: 4117-4127 [PMID:22652255]
ChEMBL	Inhibition of human SGLT2	B	8.94	pIC50	1.16	nM	IC50	Bioorg Med Chem Lett (2014) 24: 1528-1531 [PMID:24556379]
ChEMBL	Inhibition of human SGLT2	B	8.95	pIC50	1.12	nM	IC50	Eur J Med Chem (2019) 184: 111773-111773 [PMID:31630053]
ChEMBL	Inhibition of SGLT2 (unknown origin)	B	8.96	pIC50	1.1	nM	IC50	Bioorg Med Chem (2018) 26: 3947-3952 [PMID:29954682]
ChEMBL	Inhibition of full-length human SGLT2 expressed in CHO cells assessed as decrease in [14C]-methyl alpha-D-glucopyranoside uptake after 1 hr by liquid scintillation counting method	B	8.98	pIC50	1.05	nM	IC50	Bioorg Med Chem Lett (2018) 28: 2201-2205 [PMID:29764742]
ChEMBL	Inhibition of human SGLT2 expressed in CHOK1 cells assessed as inhibition of [14C]-AMG uptake after 3 hrs by microbeta scintillation counting analysis	B	9	pIC50	1	nM	IC50	Bioorg Med Chem (2014) 22: 3414-3422 [PMID:24842618]
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	9.1	pIC50	0.8	nM	IC50	J Med Chem (2017) 60: 568-579 [PMID:28098449]
GtoPdb	-	-	9.3	pIC50	0.49	nM	IC50	Bioorg Med Chem (2010) 18: 6069-79 [PMID:20637636]
ChEMBL	Inhibition of human recombinant SGLT2 expressed in CHO cells by liquid scintillation counting	B	9.31	pIC50	0.49	nM	IC50	Bioorg Med Chem (2010) 18: 2178-2194 [PMID:20181486]
ChEMBL	Inhibition of human SGLT2 expressed in CHO cells assessed as [14C]-alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counter	B	9.31	pIC50	0.49	nM	IC50	Eur J Med Chem (2011) 46: 2662-2675 [PMID:21514014]
ChEMBL	Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of [14C]alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counting	B	9.31	pIC50	0.49	nM	IC50	Bioorg Med Chem Lett (2011) 21: 742-746 [PMID:21193308]
ChEMBL	Inhibition of human SGLT2 expressed in CHO cells assessed as [14C]-alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counting	B	9.31	pIC50	0.49	nM	IC50	Bioorg Med Chem (2011) 19: 5813-5832 [PMID:21906953]
ChEMBL	Inhibition of human SGLT2 assessed as inhibition of methyl-alpha-D-glucopyranoside uptake by cell based assay	B	9.31	pIC50	0.49	nM	IC50	Bioorg Med Chem Lett (2010) 20: 7046-7049 [PMID:20952196]
ChEMBL	Inhibition of human SGLT2	B	9.31	pIC50	0.49	nM	IC50	Bioorg Med Chem (2010) 18: 6069-6079 [PMID:20637636]
ChEMBL	Inhibition of human SGLT2 expressed in CHO cells assessed as [14C]alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counting	B	9.31	pIC50	0.49	nM	IC50	Bioorg Med Chem Lett (2010) 20: 3420-3425 [PMID:20434909]
ChEMBL	Inhibition of human SGLT2 expressed in CHO cells by methyl-alpha-D-glucopyranoside assay	B	9.31	pIC50	0.49	nM	IC50	Bioorg Med Chem Lett (2022) 56: 128466-128466 [PMID:34813882]
ChEMBL	Inhibition of human SGLT2 expressed in CHO cells assessed as [14C]-alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counting	B	9.31	pIC50	0.49	nM	IC50	ACS Med Chem Lett (2011) 2: 182-187 [PMID:24900297]
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	8.52	pEC50	3	nM	EC50	J Med Chem (2011) 54: 166-178 [PMID:21128592]
ChEMBL	Inhibition of human SGLT2 expressed in CHO-K1 cells incubated for 120 mins at 37 degC by [14C]-AMG uptake assay	B	8.62	pEC50	2.4	nM	EC50	Eur J Med Chem (2012) 55: 32-38 [PMID:22818040]
ChEMBL	Inhibition of human SGLT2 expressed in CHO cells assessed as reduction in [14C]AMG uptake after 1 hr by microbeta counting method	B	8.7	pEC50	2	nM	EC50	Eur J Med Chem (2018) 143: 611-620 [PMID:29216560]
ChEMBL	Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of [14C]AMG accumulation	B	8.96	pEC50	1.1	nM	EC50	J Med Chem (2008) 51: 1145-1149 [PMID:18260618]
ChEMBL	Inhibition of human kidney SGLT2 assessed as renal glucose reabsorption	B	8.96	pEC50	1.1	nM	EC50	J Med Chem (2009) 52: 1785-1794 [PMID:19243175]
ChEMBL	Inhibition of SGLT2 (unknown origin)	B	8.96	pEC50	1.1	nM	EC50	J Med Chem (2020) 63: 5031-5073 [PMID:31930920]
Sodium/glucose cotransporter 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4316] [GtoPdb: 916] [UniProtKB: P53792]
ChEMBL	Inhibition of rat SGLT2 expressed in CHO cells assessed as inhibition of [14C]AMG accumulation	B	8.52	pEC50	3	nM	EC50	J Med Chem (2008) 51: 1145-1149 [PMID:18260618]
ChEMBL	Inhibition of rat SGLT2	B	8.52	pEC50	3	nM	EC50	J Med Chem (2009) 52: 1785-1794 [PMID:19243175]
SGLT6/Sodium/myo-inositol cotransporter 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1744524] [GtoPdb: 925] [UniProtKB: Q8WWX8]
ChEMBL	Inhibition of SGLT6 expressed in CHO cells assessed as inhibition of [14C]-alpha-methyl-D-glucopyranoside transport after 60 mins by scintillation counting	B	6.42	pIC50	380	nM	IC50	Bioorg Med Chem Lett (2011) 21: 2472-2475 [PMID:21398124]

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]