General Information of DFM (ID: F13397)
Name	Methenamine 1000 mg tablet
Company	Leading Pharma
Active Pharmaceutical Ingredient (API)	Methenamine		API Info click to show the detail info of this API
	Urinary tract infection		ICD-11: GC08	Approved
Drug Inactive Ingredient (DIGs)
	DIG ID	DIG Info	DIG Name	DIG Functional Class
	E08XEK	DIG Info	Hydrazine yellow	Colorant
	E01UTP	DIG Info	Magnesium stearate	lubricant

Full List of Biological Targets of DIG (DBTs) Regulated by DIG(s) in This DFM
G-protein coupled receptor (GPCR)
DBT Name: Opioid receptor mu (OPRM1)				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	Hydrazine yellow
Biological Activity	IC50 = 16 uM (tested by experiment)					[1]
Tested Species	Homo sapiens (Human)
UniProt ID	OPRM_HUMAN
DBT Name: Dopamine D1 receptor (DRD1)				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	Hydrazine yellow
Biological Activity	IC50 = 23 uM (tested by experiment)					[1]
Tested Species	Homo sapiens (Human)
UniProt ID	DRD1_HUMAN
Oxidoreductase (ORase)
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)					[2]
Tested Species	Homo sapiens (Human)
UniProt ID	CP3A4_HUMAN
Hydrolase (HDase)
DBT Name: Tyrosyl-DNA phosphodiesterase 2 (TDP2)				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	Hydrazine yellow
Biological Activity	IC50 = 3500 nM (estimated based on the structural similarity with CHEMBL3813826 )					[3]
Structural Similarity	Tanimoto coefficient = 0.777777778
Tested Species	Homo sapiens (Human)
UniProt ID	TYDP2_HUMAN
Transmembrane channel/porin (TC/P)
DBT Name: GABA(A) receptor alpha-1 (GABRA1)				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	Hydrazine yellow
Biological Activity	IC50 = 13 uM (tested by experiment)					[1]
Tested Species	Homo sapiens (Human)
UniProt ID	GBRA1_HUMAN

References
1	The activities of drug inactive ingredients on biological targets. Science. 2020 Jul 24;369(6502):403-413.
2	Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
3	Discovery of selective inhibitors of tyrosyl-DNA phosphodiesterase 2 by targeting the enzyme DNA-binding cleft. Bioorg Med Chem Lett. 2016 Jul 15; 26(14):3232-3236.

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