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

Rendered image for the query structure

Synonyms & Links

UNII: 1ULL0QJ8UC

PubChem: 9887712

Guide to Pharmacology: 4594

ChEMBL: CHEMBL429910

DrugCentral: 4304

LyCHI: 2NSHZBU641RM

Target Activities

Explore Associated and Predicted Targets

SLC5A2

Tclin

Sodium/glucose cotransporter 2

38 Activities

Items per page:

1 – 10 of 38

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)
IC50	9.3			20637636

IC50	9.31		Bioorg. Med. Chem., (2010) 18:6:2178	20181486

IC50	9.31		Bioorg. Med. Chem. Lett., (2010) 20:11:3420	20434909

IC50	9.31		Bioorg. Med. Chem., (2010) 18:16:6069	20637636

IC50	9.31		Bioorg. Med. Chem. Lett., (2010) 20:23:7046	20952196

IC50	9.31		Bioorg. Med. Chem. Lett., (2011) 21:2:742	21193308

IC50	9.31		ACS Med. Chem. Lett., (2011) 2:2:182	24900297

IC50	9.31		Eur. J. Med. Chem., (2011) 46:7:2662	21514014

IC50	9.31		Bioorg. Med. Chem., (2011) 19:19:5813	21906953

IC50	9.1		J Med Chem, (2017) 60:2:568	28098449

SLC5A1

Tclin

Sodium/glucose cotransporter 1

15 Activities

Items per page:

1 – 10 of 15

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)
IC50	6.4			21398124

IC50	8.49		Bioorg. Med. Chem. Lett., (2011) 21:15:4465	21737266

IC50	6.43		Bioorg. Med. Chem. Lett., (2011) 21:8:2472	21398124

EC50	6.37		J. Med. Chem., (2011) 54:1:166	21128592

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

IC50	6.2		J Med Chem, (2017) 60:10:4173	28447791

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

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

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

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

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

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