General Information of Xenobiotics (ID: XEO00470)
Xenobiotics Name
Flufenamic acid
Xenobiotics Type
Pharmaceutical Agent(s)
Classification
Approved/Marketed Drug
Structure
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3D MOL 2D MOL
PubChem CID
3371
DME(s) Modulated by This Xenobiotics
DME(s) Inhibited by This Xenobiotics
Aldo-keto reductase 1C1 (AKR1C1) DME Info Homo sapiens [1], [2]
Aldo-keto reductase 1C2 (AKR1C2) DME Info Homo sapiens [3]
Aldo-keto reductase 1C3 (AKR1C3) DME Info Homo sapiens [3]
Aldo-keto reductase 1C4 (AKR1C4) DME Info Homo sapiens [4], [5]
DME(s) Induced by This Xenobiotics
Prostaglandin G/H synthase 2 (COX-2) DME Info Homo sapiens [6]
Xenobiotics-DME Activity Data
Xenobiotics-DME Activity Data Aldo-keto reductase 1C1 (AKR1C1) DME Info IC50 = 0.98 microM [1], [2]
Aldo-keto reductase 1C2 (AKR1C2) DME Info IC50 = 0.37 microM [3]
Aldo-keto reductase 1C3 (AKR1C3) DME Info IC50 = 0.05 microM [3]
Aldo-keto reductase 1C4 (AKR1C4) DME Info IC50 > 100 microM [4], [5]
References
1 Relationship of human liver dihydrodiol dehydrogenases to hepatic bile-acid-binding protein and an oxidoreductase of human colon cells. Biochem J. 1996 Jan 15;313 ( Pt 2)(Pt 2):373-6.
2 Selective and potent inhibitors of human 20alpha-hydroxysteroid dehydrogenase (AKR1C1) that metabolizes neurosteroids derived from progesterone. Chem Biol Interact. 2003 Feb 1;143-144:503-13.
3 Development of potent and selective inhibitors of aldo-keto reductase 1C3 (type 5 17beta-hydroxysteroid dehydrogenase) based on N-phenyl-aminobenzoates and their structure-activity relationships. J Med Chem. 2012 Mar 8;55(5):2311-23.
4 3-(3,4-Dihydroisoquinolin-2(1H)-ylsulfonyl)benzoic Acids: Highly Potent and Selective Inhibitors of the Type 5 17-beta-hydroxysteroid Dehydrogenase AKR1C3 J Med Chem. 2012 Sep 13;55(17):7746-58.
5 Synthesis and structure-activity relationships for 1-(4-(piperidin-1-ylsulfonyl)phenyl)pyrrolidin-2-ones as novel non-carboxylate inhibitors of the aldo-keto reductase enzyme AKR1C3. Eur J Med Chem. 2013 Apr;62:738-44.
6 Two opposing effects of non-steroidal anti-inflammatory drugs on the expression of the inducible cyclooxygenaseMediation through different signaling pathways. J Biol Chem. 2000 Sep 8;275(36):28173-9.

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