Pharos : Ligand Details - diethylstilbestrol

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A synthetic nonsteroidal estrogen used in the treatment of menopausal and postmenopausal disorders. It was also used formerly as a growth promoter in animals. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), diethylstilbestrol has been listed as a known carcinogen. (Merck, 11th ed)

Ligand Summary

Ligand Structure

Rendered image for the query structure

Synonyms & Links

UNII: 731DCA35BT

PubChem: 448537

Guide to Pharmacology: 2801

ChEMBL: CHEMBL411

DrugCentral: 875

LyCHI: G6MP2G77G9WR

Target Activities

Explore Associated and Predicted Targets

ESR1

Tclin

Estrogen receptor

13 Activities

Items per page:

1 – 10 of 13

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)
-	10.4			9048584

EC50	10.22		J. Med. Chem., (2002) 45:7:1399	11906280

EC50	9.96		Bioorg Med Chem, (2019) 27:10:1952	30940565

EC50	9.7		Bioorg Med Chem, (2019) 27:10:1952	30940565

Ki	9.66		Bioorg. Med. Chem. Lett., (2013) 23:6:1834	23403082

Ki	9.58		None, None:None:None

IC50	9.48		Bioorg. Med. Chem. Lett., (2002) 12:9:1283	11965371

Ki	9.31		J. Med. Chem., (2003) 46:8:1408	12672240

IC50	9.11		Bioorg. Med. Chem. Lett., (2013) 23:6:1834	23403082

IC50	9.04		None, None:None:None

ESR2

Tclin

Estrogen receptor beta

5 Activities

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1 – 5 of 5

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)
-	9.8			9048584

EC50	10.7		J. Med. Chem., (2002) 45:7:1399	11906280

Ki	9.2		J. Med. Chem., (2003) 46:8:1408	12672240

IC50	8.4		J. Med. Chem., (2001) 44:11:1654	11356100

EC50	8.05		J. Med. Chem., (2002) 45:7:1399	11906280

SLC6A3

Tclin

Sodium-dependent dopamine transporter

1 Activities

Items per page:

1 – 1 of 1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)
Ki	6.07		None, None:None:None

ABCG2

Tchem

ATP-binding cassette sub-family G member 2

1 Activities

Items per page:

1 – 1 of 1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)
IC50	6.3		Mol. Cancer Ther., (2003) 2:1:105	12533678

AOX1

Tchem

Aldehyde oxidase

1 Activities

Items per page:

1 – 1 of 1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)
IC50	6.34		J. Med. Chem., (2010) 53:24:8441	20853847