ChEMBL ligand: CHEMBL2048484 (Canagliflozin anhydrous, JNJ-28431754, TA-7284)
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!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
Sodium/glucose cotransporter 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4979] [GtoPdb: 915] [UniProtKB: P13866]
ChEMBL	Inhibition of human SGLT1 expressed in CHO-K1 cells by [14C]AMG uptake assay	B	5.72	pIC50	1900	nM	IC50	Bioorg Med Chem (2012) 20: 4117-4127 [PMID:22652255]
ChEMBL	Inhibition of SGLT1 (unknown origin)	B	6.15	pIC50	710	nM	IC50	J Med Chem (2023) 66: 12536-12543 [PMID:37608596]
ChEMBL	Inhibition of human SGLT1	B	6.16	pIC50	684	nM	IC50	Eur J Med Chem (2019) 184: 111773-111773 [PMID:31630053]
GtoPdb	-	-	6.2	pIC50	684	nM	IC50	PLoS ONE (2012) 7: e30555 [PMID:22355316]
ChEMBL	SGLT1/2 in-vitro assay: To analyze a sodium-dependent glucose transport, cells for expressing hSGLT1 and hSGLT2 were seeded at 1×105 cells per well into a 96-well culture plate, after which resulting cells were cultured in an RPMI 1640 medium containing 10% fetal bovine serum (FBS). In 1 day after culture, the resulting cells were cultured in a pre-treatment buffer solution (10 mM HEPES, 5 mM tris, 140 mM choline chloride, 2 mM KCl, 1 mM CaCl2 and 1 mM MgCl2, pH 7.4) under 37° C./5% CO2 conditions for 10 minutes. Then, the resulting cells were cultured in a uptake buffer solution (10 mM HEPES, 5 mM tris, 140 mM NaCl, 2 mM KCl, 1 mM CaCl2, 1 mM MgCl2 and 1 mM AMGS pH 7.4) containing 14C-AMG (8 μM) and a compound of the present disclosure or a dimethyl sulfoxide (DMSO) vehicle under 37° C./5% CO2 conditions for 2 hours. After culture, the cells were washed twice with a washing buffer solution (a pre-treatment buffer solution containing 10 mM AMG at room temperature), after which a radiation thereof was measured by using a liquid scintillation counter. IC50 of each compound was measured according to a non-linear regression analysis by using SigmaPlot (Document Analytical Biochemistry 429: 70-75, Molecular and Cellular Biochemistry 280: 91-98, 2005).	B	6.26	pIC50	550	nM	IC50	US-10752604-B2. C-glucoside derivative containing fused phenyl ring or pharmaceutically acceptable salt thereof, process for preparing same, and pharmaceutical composition comprising same (2020)
ChEMBL	Inhibition of human SGLT1 expressed in CHO cells assessed as decrease in uptake of [14C]AMG after 120 mins by TopCount method	B	6.58	pIC50	265	nM	IC50	J Med Chem (2017) 60: 4173-4184 [PMID:28447791]
ChEMBL	Inhibition of SGLT1 (unknown origin)	B	6.04	pEC50	910	nM	EC50	J Med Chem (2020) 63: 5031-5073 [PMID:31930920]
Sodium/glucose cotransporter 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3884] [GtoPdb: 916] [UniProtKB: P31639]
ChEMBL	Inhibition of human SGLT2 expressed in CHO-K1 cells by [14C]AMG uptake assay	B	8.17	pIC50	6.7	nM	IC50	Bioorg Med Chem (2012) 20: 4117-4127 [PMID:22652255]
ChEMBL	SGLT1/2 in-vitro assay: To analyze a sodium-dependent glucose transport, cells for expressing hSGLT1 and hSGLT2 were seeded at 1×105 cells per well into a 96-well culture plate, after which resulting cells were cultured in an RPMI 1640 medium containing 10% fetal bovine serum (FBS). In 1 day after culture, the resulting cells were cultured in a pre-treatment buffer solution (10 mM HEPES, 5 mM tris, 140 mM choline chloride, 2 mM KCl, 1 mM CaCl2 and 1 mM MgCl2, pH 7.4) under 37° C./5% CO2 conditions for 10 minutes. Then, the resulting cells were cultured in a uptake buffer solution (10 mM HEPES, 5 mM tris, 140 mM NaCl, 2 mM KCl, 1 mM CaCl2, 1 mM MgCl2 and 1 mM AMGS pH 7.4) containing 14C-AMG (8 μM) and a compound of the present disclosure or a dimethyl sulfoxide (DMSO) vehicle under 37° C./5% CO2 conditions for 2 hours. After culture, the cells were washed twice with a washing buffer solution (a pre-treatment buffer solution containing 10 mM AMG at room temperature), after which a radiation thereof was measured by using a liquid scintillation counter. IC50 of each compound was measured according to a non-linear regression analysis by using SigmaPlot (Document Analytical Biochemistry 429: 70-75, Molecular and Cellular Biochemistry 280: 91-98, 2005).	B	8.31	pIC50	4.9	nM	IC50	US-10752604-B2. C-glucoside derivative containing fused phenyl ring or pharmaceutically acceptable salt thereof, process for preparing same, and pharmaceutical composition comprising same (2020)
ChEMBL	Inhibition of human SGLT2	B	8.36	pIC50	4.4	nM	IC50	Eur J Med Chem (2019) 184: 111773-111773 [PMID:31630053]
GtoPdb	-	-	8.4	pIC50	4.4	nM	IC50	PLoS ONE (2012) 7: e30555 [PMID:22355316]
ChEMBL	Inhibition of SGLT2 (unknown origin)	B	8.62	pIC50	2.4	nM	IC50	J Med Chem (2023) 66: 12536-12543 [PMID:37608596]
ChEMBL	Inhibition of SGLT2 (unknown origin)	B	8.66	pIC50	2.2	nM	IC50	Bioorg Med Chem (2018) 26: 3947-3952 [PMID:29954682]
ChEMBL	Inhibition of human SGLT2 by liquid scintillation counter analysis	B	8.66	pIC50	2.2	nM	IC50	J Med Chem (2023) 66: 991-1010 [PMID:36584305]
ChEMBL	Inhibition of human SGLT2 expressed in CHO cells assessed as decrease in uptake of [14C]AMG after 120 mins by TopCount method	B	8.66	pIC50	2.2	nM	IC50	J Med Chem (2017) 60: 4173-4184 [PMID:28447791]
ChEMBL	Inhibition of SGLT2 (unknown origin)	B	8.66	pEC50	2.2	nM	EC50	J Med Chem (2020) 63: 5031-5073 [PMID:31930920]

ChEMBL data shown on this page come from version 36:

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]