Pharos : Ligand Details - dapagliflozin

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an Sodium-glucose cotransporter 2 (SGLT2) inhibitor, SGLT2 expressed in the proximal renal tubules, is responsible for the majority of the reabsorption of filtered glucose from the tubular lumen, by inhibiting SGLT2, dapagliflozin reduces reabsorption of filtered glucose and lowers the renal threshold for glucose, and thereby increases urinary glucose excretion

Ligand Summary

Ligand Structure

chemical structure image

Synonyms & Links

UNII: 1ULL0QJ8UC

PubChem: 9887712

Guide to Pharmacology: 4594

ChEMBL: CHEMBL429910

DrugCentral: 4304

LyCHI: 2NSHZBU641RM

Target Activities

SLC5A2

Tclin

Sodium/glucose cotransporter 2

30 Activities

Items per page:

1 – 10 of 30

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)
IC50	7.66		Bioorg. Med. Chem. Lett., (2011) 21:8:2472	21398124

IC50	8.17		Bioorg. Med. Chem. Lett., (2009) 19:19:5632	19700318

IC50	8.17		Bioorg. Med. Chem. Lett., (2009) 19:24:6877	19896374

IC50	8.17		Bioorg. Med. Chem., (2010) 18:12:4422	20576578

IC50	8.3		Bioorg. Med. Chem. Lett., (2015) 25:5:993	25650254

IC50	8.4		Bioorg. Med. Chem. Lett., (2011) 21:8:2472	21398124

IC50	8.49		J. Med. Chem., (2014) 57:4:1236	24456245

IC50	8.52		None, (2015) None:None:None

IC50	8.52		None, (2015) None:None:None

EC50	8.52		J. Med. Chem., (2011) 54:1:166	21128592

SLC5A1

Tclin

Sodium/glucose cotransporter 1

14 Activities

Items per page:

1 – 10 of 14

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)
IC50	6.05		Bioorg. Med. Chem. Lett., (2009) 19:19:5632	19700318

IC50	6.05		Bioorg. Med. Chem. Lett., (2009) 19:24:6877	19896374

IC50	6.05		Bioorg. Med. Chem., (2010) 18:12:4422	20576578

IC50	6.05		Bioorg. Med. Chem., (2014) 22:13:3414	24842618

IC50	6.09		None, (2015) None:None:None

IC50	6.09		None, (2015) None:None:None

IC50	6.09		J. Med. Chem., (2009) 52:20:6201	19785435

IC50	6.1		Bioorg. Med. Chem., (2012) 20:13:4117	22652255

IC50	6.1		J. Med. Chem., (2012) 55:17:7828	22889351

EC50	6.23		Eur. J. Med. Chem., (2012) 55:None:32	22818040

SLC5A4

Tchem

Solute carrier family 5 member 4

2 Activities

Items per page:

1 – 2 of 2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)
IC50	8.87		Bioorg. Med. Chem. Lett., (2011) 21:12:3759	21592794

IC50	8.87		https://www.ebi.ac.uk/chembl/compound/inspect/CHEMBL429910

SLC5A11

Tchem

Sodium/myo-inositol cotransporter 2

2 Activities

Items per page:

1 – 2 of 2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)
IC50	6.42		Bioorg. Med. Chem. Lett., (2011) 21:8:2472	21398124

IC50	6.42		https://www.ebi.ac.uk/chembl/compound/inspect/CHEMBL429910