Pharos : Ligand Details - rosiglitazone

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A thiazolidinedione that functions as a selective agonist for PPAR GAMMA. It improves INSULIN SENSITIVITY in adipose tissue, skeletal muscle, and the liver of patients with TYPE 2 DIABETES MELLITUS.

Ligand Summary

Ligand Structure

Rendered image for the query structure

Synonyms & Links

UNII: 05V02F2KDG

PubChem: 77999

PubChem: 5281055

Guide to Pharmacology: 1056

ChEMBL: CHEMBL121

ChEMBL: CHEMBL843

DrugCentral: 2405

LyCHI: M55WRV5WU2U6

Target Activities

Explore Associated and Predicted Targets

PPARG

Tclin

Peroxisome proliferator-activated receptor gamma

113 Activities

Items per page:

1 – 10 of 113

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)
Ki	6.92			11720854

-	7.4			9836620 9013583 9454824

EC50	9		None, (2016) None:None:None

Kd	8.92		Eur J Med Chem, (2017) 127:None:379	28076827

EC50	8.62		J. Med. Chem., (2012) 55:11:4978	22582973

EC50	8.57		J. Biol. Chem., (2007) 282:23:17314	17403688

EC50	8.42		J. Biol. Chem., (2007) 282:23:17314	17403688

EC50	8.4		Bioorg. Med. Chem. Lett., (2005) 15:20:4421	16137885

EC50	8.4		J. Med. Chem., (2013) 56:4:1535	23286787

EC50	8.4		Eur J Med Chem, (2017) 137:None:310	28609708

CISD1

Tchem

CDGSH iron-sulfur domain-containing protein 1

3 Activities

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1 – 3 of 3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)
Ki	7.51		Bioorg Med Chem Lett, (2016) 26:21:5350	27687671

IC50	6.14		Bioorg Med Chem Lett, (2016) 26:21:5350	27687671

Ki	7.51		https://www.ebi.ac.uk/chembl/compound/inspect/CHEMBL121

PPARA

Tclin

Peroxisome proliferator-activated receptor alpha

2 Activities

Items per page:

1 – 2 of 2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)
EC50	8.4		Bioorg. Med. Chem. Lett., (2008) 18:5:1617	18255290

EC50	7.41		Bioorg. Med. Chem., (2008) 16:21:9498	18835719

FFAR1

Tchem

Free fatty acid receptor 1

1 Activities

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1 – 1 of 1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)
	5.6			12565875

TRPC5

Tchem

Short transient receptor potential channel 5

1 Activities

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1 – 1 of 1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)
-	4.51			21406603

MAOB

Tclin

Amine oxidase [flavin-containing] B

1 Activities

Items per page:

1 – 1 of 1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)
IC50	6.08		Bioorg. Med. Chem. Lett., (2010) 20:17:5295	20650633