Pharos : Ligand Details - estrone

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An aromatized C18 steroid with a 3-hydroxyl group and a 17-ketone, a major mammalian estrogen. It is converted from ANDROSTENEDIONE directly, or from TESTOSTERONE via ESTRADIOL. In humans, it is produced primarily by the cyclic ovaries, PLACENTA, and the ADIPOSE TISSUE of men and postmenopausal women.

Ligand Summary

Ligand Structure

Rendered image for the query structure

Synonyms & Links

UNII: 2DI9HA706A

PubChem: 5870

Guide to Pharmacology: 2818

ChEMBL: CHEMBL1405

DrugCentral: 3188

LyCHI: M3SWMTZ32PK9

Target Activities

Explore Associated and Predicted Targets

ESR1

Tclin

Estrogen receptor

8 Activities

Items per page:

1 – 8 of 8

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)
-	8.5			9048584

EC50	9.15		J. Med. Chem., (2002) 45:7:1399	11906280

Ki	8.66		None, None:None:None

EC50	8.15		J. Med. Chem., (2009) 52:21:6660	19824648

IC50	8.12		None, None:None:None

IC50	7.54		J. Med. Chem., (2006) 49:8:2440	16610787

IC50	7.02		Bioorg. Med. Chem. Lett., (2009) 19:23:6740	19836949

EC50	9.15	AGONIST	https://www.ebi.ac.uk/chembl/compound/inspect/CHEMBL1405

HSD17B1

Tchem

Estradiol 17-beta-dehydrogenase 1

7 Activities

Items per page:

1 – 7 of 7

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)
Ki	8.52		Eur. J. Med. Chem., (2008) 43:11:2298	18372081

IC50	6.96		Bioorg. Med. Chem. Lett., (2009) 19:23:6740	19836949

IC50	6.66		Bioorg. Med. Chem., (2008) 16:4:1849	18035543

IC50	6.48		J. Med. Chem., (2006) 49:4:1325	16480268

IC50	6.22		Eur. J. Med. Chem., (2008) 43:11:2298	18372081

IC50	6.09		Eur. J. Med. Chem., (2008) 43:11:2298	18372081

Ki	8.52		https://www.ebi.ac.uk/chembl/compound/inspect/CHEMBL1405

ESR2

Tclin

Estrogen receptor beta

5 Activities

Items per page:

1 – 5 of 5

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)
	7.93			9048584

EC50	8.68		J. Med. Chem., (2002) 45:7:1399	11906280

EC50	8.1		J. Med. Chem., (2009) 52:21:6660	19824648

EC50	7.58		J. Med. Chem., (2006) 49:8:2440	16610787

IC50	7.51		J. Med. Chem., (2006) 49:8:2440	16610787

SHBG

Tchem

Sex hormone-binding globulin

2 Activities

Items per page:

1 – 2 of 2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)
Kd	8.18		J. Med. Chem., (2008) 51:7:2047	18330978

Kd	8.18		https://www.ebi.ac.uk/chembl/compound/inspect/CHEMBL1405