dapagliflozin [Ligand Id: 4594] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL429910 (Dapagliflozin, BMS-512148, BMS-512148-05, Forxiga)
  • Low affinity sodium-glucose cotransporter in Human [ChEMBL: CHEMBL1770047] [GtoPdb: 917] [UniProtKB: Q9NY91]
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  • Sodium/glucose cotransporter 1 in Human [ChEMBL: CHEMBL4979] [GtoPdb: 915] [UniProtKB: P13866]
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  • SGLT6/Sodium/myo-inositol cotransporter 2 in Human [ChEMBL: CHEMBL1744524] [GtoPdb: 925] [UniProtKB: Q8WWX8]
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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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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-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 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 B 8.94 pIC50 1.16 nM IC50 Bioorg. Med. Chem. Lett. (2014) 24: 1528-1531 [PMID:24556379]
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]
GtoPdb - - 9.3 pIC50 0.49 nM IC50 Bioorg. Med. Chem. (2010) 18: 6069-79 [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 B 9.31 pIC50 0.49 nM IC50 Bioorg. Med. Chem. (2010) 18: 6069-6079 [PMID:20637636]
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 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 ACS Med. Chem. Lett. (2011) 2: 182-187 [PMID:24900297]
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 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 counting B 9.31 pIC50 0.49 nM IC50 Bioorg. Med. Chem. (2011) 19: 5813-5832 [PMID:21906953]
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]
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 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]