General Information of DFM (ID: F08104)
Name	Fentanyl 0.4 mg tablet
Company	Cephalon
Active Pharmaceutical Ingredient (API)	Fentanyl		API Info click to show the detail info of this API
	Anaesthesia		ICD-11: 8E22	Approved
Drug Inactive Ingredient (DIGs)
	DIG ID	DIG Info	DIG Name	DIG Functional Class
	E0DB2E	DIG Info	Carbonic acid disodium salt	Alkalizing agent ...
	E0F6AN	DIG Info	Kyselina citronova	Acidulant ...
	E01UTP	DIG Info	Magnesium stearate	lubricant
	E0Q6DQ	DIG Info	Mannitol	Diluent ...
	E0G1YW	DIG Info	Sodium bicarbonate	Alkalizing agent ...

Full List of Biological Targets of DIG (DBTs) Regulated by DIG(s) in This DFM
Oxidoreductase (ORase)
DBT Name: N1-methyl adenine demethylase (FTO)				Click to Show/Hide
Detailed Information	DBT Info click to show the detail info of this DBT
Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
Interacting DIG	Kyselina citronova
Biological Activity	IC50 = 300000 nM (tested by experiment)					[1]
Tested Species	Homo sapiens (Human)
UniProt ID	FTO_HUMAN
DBT Name: RNA demethylase ALKBH5 (ALKB5)				Click to Show/Hide
Detailed Information	DBT Info click to show the detail info of this DBT
Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
Interacting DIG	Kyselina citronova
Biological Activity	IC50 = 488000 nM (tested by experiment)					[2]
Tested Species	Homo sapiens (Human)
UniProt ID	ALKB5_HUMAN
DBT Name: Albendazole monooxygenase (CYP3A4)				Click to Show/Hide
Detailed Information	DBT Info click to show the detail info of this DBT
Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
Interacting DIG	Magnesium stearate
Biological Activity	Protein expression downregulation (tested by experiment)					[3]
Tested Species	Homo sapiens (Human)
UniProt ID	CP3A4_HUMAN
Transmembrane channel/porin (TC/P)
DBT Name: Glycine receptor alpha-1 (GLRA1)				Click to Show/Hide
Detailed Information	DBT Info click to show the detail info of this DBT
Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
Interacting DIG	Mannitol
Biological Activity	EC50 = 12589.25 nM (estimated based on the structural similarity with CHEMBL604608 )					[4]
Structural Similarity	Tanimoto coefficient = 0.804878049
Tested Species	Homo sapiens (Human)
UniProt ID	GLRA1_HUMAN
Nuclear receptor (NR)
DBT Name: Factor HNF-4-alpha (HNF4A)				Click to Show/Hide
Detailed Information	DBT Info click to show the detail info of this DBT
Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
Interacting DIG	Kyselina citronova
Biological Activity	IC50 = 39869 nM (tested by experiment)					[5]
Tested Species	Homo sapiens (Human)
UniProt ID	HNF4A_HUMAN
Other protein families (OPF)
DBT Name: Perilipin-1 (PLIN1)				Click to Show/Hide
Detailed Information	DBT Info click to show the detail info of this DBT
Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
Interacting DIG	Kyselina citronova
Biological Activity	IC50 = 3708 nM (tested by experiment)					[5]
Tested Species	Homo sapiens (Human)
UniProt ID	PLIN1_HUMAN

References
1	Structural basis for inhibition of the fat mass and obesity associated protein (FTO). J Med Chem. 2013 May 9; 56(9):3680-8.
2	Repair of methyl lesions in RNA by oxidative demethylation. Med Chem Comm. (2014) 5:1797-1803.
3	Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
4	Pharmacological property optimization for allosteric ligands: A medicinal chemistry perspective. Bioorg Med Chem Lett. 2017 Jun 1; 27(11):2239-2258.
5	PubChem BioAssay data set.

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