General Information of DFM (ID: F21087)
Name	Tiagabine 4 mg tablet
Company	Sun Pharmaceutical Industries
Active Pharmaceutical Ingredient (API)	Tiagabine		API Info click to show the detail info of this API
	Epilepsy		ICD-11: 8A60	Approved
Drug Inactive Ingredient (DIGs)
	DIG ID	DIG Info	DIG Name	DIG Functional Class
	E0SJ4H	DIG Info	Beta-D-lactose	Diluent ...
	E0QV6C	DIG Info	Butylhydroxyanisole	Antimicrobial preservative ...
	E0PE9M	DIG Info	Crospovidone	Disintegrant
	E00DHW	DIG Info	Lactose monohydrate	Binding agent ...
	E0H6BT	DIG Info	Quinoline yellow WS	Colorant
	E01UTV	DIG Info	Silicon dioxide	Anticaking agent ...
	E0QY1F	DIG Info	Talc	Anticaking agent ...
	E05BSD	DIG Info	Titanium dioxide	Coating agent ...

Full List of Biological Targets of DIG (DBTs) Regulated by DIG(s) in This DFM
G-protein coupled receptor (GPCR)
DBT Name: Muscarinic receptor M1 (ACM1)				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	Butylhydroxyanisole
Biological Activity	IC50 = 19 uM (tested by experiment)					[1]
Tested Species	Homo sapiens (Human)
UniProt ID	ACM1_HUMAN
DBT Name: Alpha-1A adrenoceptor (ADA1A)				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	Butylhydroxyanisole
Biological Activity	IC50 = 19 uM (tested by experiment)					[1]
Tested Species	Homo sapiens (Human)
UniProt ID	ADA1A_HUMAN
DBT Name: Alpha-2A adrenoceptor (ADA2A)				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	Quinoline yellow WS
Biological Activity	IC50 = 28 uM (tested by experiment)					[1]
Tested Species	Homo sapiens (Human)
UniProt ID	ADA2A_HUMAN
DBT Name: Dopamine D3 receptor (DRD3)				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	Quinoline yellow WS
Biological Activity	IC50 = 26 uM (tested by experiment)					[1]
Tested Species	Homo sapiens (Human)
UniProt ID	DRD3_HUMAN
Oxidoreductase (ORase)
DBT Name: Prostaglandin G/H synthase 2 (COX-2)				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	Butylhydroxyanisole
Biological Activity	IC50 = 2.6 uM (tested by experiment)					[1]
Tested Species	Homo sapiens (Human)
UniProt ID	PGH2_HUMAN
DBT Name: Albendazole monooxygenase (CYP3A4)				Click to Show/Hide
Detailed Information	DBT Info click to show the detail info of this DBT
Experiment (1) for Assessing the Biological Activity of the Studied DIG on This DBT
Interacting DIG	Crospovidone
Biological Activity	Protein expression downregulation (tested by experiment)					[2]
Tested Species	Homo sapiens (Human)
UniProt ID	CP3A4_HUMAN
Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
Interacting DIG	Silicon dioxide
Biological Activity	Protein expression downregulation (tested by experiment)					[2]
Tested Species	Homo sapiens (Human)
UniProt ID	CP3A4_HUMAN
Hydrolase (HDase)
DBT Name: Acetylcholinesterase (ACHE)				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	Quinoline yellow WS
Biological Activity	IC50 > 10 uM (tested by experiment)					[1]
Tested Species	Homo sapiens (Human)
UniProt ID	ACES_HUMAN
Potential-driven transporter (PDT)
DBT Name: Dopamine transporter (DAT)				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	Quinoline yellow WS
Biological Activity	IC50 = 29 uM (tested by experiment)					[1]
Tested Species	Homo sapiens (Human)
UniProt ID	SC6A3_HUMAN
Nuclear receptor (NR)
DBT Name: Estrogen receptor alpha (ESR1)				Click to Show/Hide
Detailed Information	DBT Info click to show the detail info of this DBT
Experiment (1) for Assessing the Biological Activity of the Studied DIG on This DBT
Interacting DIG	Quinoline yellow WS
Biological Activity	EC50 = 13156.33 nM (estimated based on the structural similarity with CHEMBL1417293 )					[3]
Structural Similarity	Tanimoto coefficient = 0.828729282
Tested Species	Homo sapiens (Human)
UniProt ID	ESR1_HUMAN
Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
Interacting DIG	Quinoline yellow WS
Biological Activity	IC50 = 18 uM (tested by experiment)					[1]
Tested Species	Homo sapiens (Human)
UniProt ID	ESR1_HUMAN
DBT Name: Progesterone receptor (PGR)				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	Butylhydroxyanisole
Biological Activity	IC50 = 29 uM (tested by experiment)					[1]
Tested Species	Homo sapiens (Human)
UniProt ID	PRGR_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	PubChem BioAssay data set.

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