Target family: CYP11, CYP17, CYP19, CYP20 and CYP21 families (type: enzyme)
Target: CYP19A1

Ligand: (2S,4S)-ketoconazole (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.400000095367432 pIC50
Reference (Journal): Stereoisomers of ketoconazole: preparation and biological activity.
Published in: J Med Chem

Ligand: aminoglutethimide (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1980)
Primary target: yes
Median affinity:  -
Reference (Journal): In vitro kinetic properties of the Thr201Met variant of human aromatase gene CYP19A1: functional responses to substrate and product inhibition and enzyme inhibitors.
Published in: J Clin Endocrinol Metab

Ligand: anastrozole (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1995)
Primary target: yes
Median affinity: 7.820000171661377 pIC50
Reference (Journal): The preclinical pharmacology of &quot;Arimidex&quot; (anastrozole; ZD1033)--a potent, selective aromatase inhibitor.
Published in: J Steroid Biochem Mol Biol

Ligand: azalanstat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.119999885559082 pKi
Reference (Journal): Selective inhibition of mammalian lanosterol 14 alpha-demethylase: a possible strategy for cholesterol lowering.
Published in: J Med Chem

Ligand: endoxifen (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.400000095367432 pKi
Reference (Journal): Tamoxifen metabolites as active inhibitors of aromatase in the treatment of breast cancer.
Published in: Breast Cancer Res Treat

Ligand: endoxifen (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.21999979019165 pIC50
Reference (Journal): The tamoxifen metabolite norendoxifen is a potent and selective inhibitor of aromatase (CYP19) and a potential lead compound for novel therapeutic agents.
Published in: Breast Cancer Res Treat

Ligand: exemestane (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1999)
Primary target: yes
Median affinity: 7.400000095367432 pIC50
Reference (Journal): 6-Methylenandrosta-1,4-diene-3,17-dione (FCE 24304): a new irreversible aromatase inhibitor.
Published in: J Steroid Biochem

Ligand: exemestane (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1999)
Primary target: no
Median affinity: 7.599999904632568 pKi
Reference (Journal): 6-Methylenandrosta-1,4-diene-3,17-dione (FCE 24304): a new irreversible aromatase inhibitor.
Published in: J Steroid Biochem

Ligand: fadrozole (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: Japan only
Primary target: yes
Median affinity: 8.350000381469727 pIC50
Reference (Journal): Fadrozole hydrochloride: a potent, selective, nonsteroidal inhibitor of aromatase for the treatment of estrogen-dependent disease.
Published in: J Med Chem

Ligand: letrozole (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1997)
Primary target: no
Median affinity: 7.900000095367432 pIC50
Reference (Journal): Highly selective inhibition of estrogen biosynthesis by CGS 20267, a new non-steroidal aromatase inhibitor.
Published in: J Steroid Biochem Mol Biol

Ligand: letrozole (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1997)
Primary target: yes
Median affinity: 10.699999809265137 pKi
Reference (Journal): Optimization of the aromatase inhibitory activities of pyridylthiazole analogues of resveratrol.
Published in: Bioorg Med Chem

Ligand: norendoxifen (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.349999904632568 pKi
Reference (Journal): Synthesis of mixed (E,Z)-, (E)-, and (Z)-norendoxifen with dual aromatase inhibitory and estrogen receptor modulatory activities.
Published in: J Med Chem

Ligand: testolactone (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1969)
Primary target: yes
Median affinity: 4.460000038146973 pKi
Reference (Journal): A new hypothesis based on suicide substrate inhibitor studies for the mechanism of action of aromatase.
Published in: Cancer Res