General Information of DFM (ID: F09508)
Name	Guanfacine 3 mg tablet
Company	Sun Pharmaceutical Industries
Active Pharmaceutical Ingredient (API)	Guanfacine		API Info click to show the detail info of this API
	Attention deficit hyperactivity disorder		ICD-11: 6A05	Approved
Drug Inactive Ingredient (DIGs)
	DIG ID	DIG Info	DIG Name	DIG Functional Class
	E0L3MB	DIG Info	FD&C blue no. 2	Colorant
	E0M0IE	DIG Info	Ferric hydroxide oxide yellow	Colorant
	E09ZKW	DIG Info	Fumaric acid	Acidulant ...
	E0EI2M	DIG Info	Glyceryl dibehenate	Binding agent ...
	E00DHW	DIG Info	Lactose monohydrate	Binding agent ...
	E01UTV	DIG Info	Silicon dioxide	Anticaking agent ...

Full List of Biological Targets of DIG (DBTs) Regulated by DIG(s) in This DFM
G-protein coupled receptor (GPCR)
DBT Name: Adenosine receptor A3 (AA3R)				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	FD&C blue no. 2
Biological Activity	IC50 = 1 uM (tested by experiment)					[1]
Tested Species	Homo sapiens (Human)
UniProt ID	AA3R_HUMAN
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	Fumaric acid
Biological Activity	IC50 = 150000 nM (tested by experiment)					[2]
Tested Species	Homo sapiens (Human)
UniProt ID	FTO_HUMAN
DBT Name: HIF-prolyl hydroxylase 2 (EGLN1)				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	Fumaric acid
Biological Activity	IC50 = 19000 nM (tested by experiment)					[3]
Tested Species	Homo sapiens (Human)
UniProt ID	EGLN1_HUMAN
DBT Name: Monoamine oxidase A (MAO-A)				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	FD&C blue no. 2
Biological Activity	IC50 > 3 uM (tested by experiment)					[1]
Tested Species	Homo sapiens (Human)
UniProt ID	AOFA_HUMAN
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	FD&C blue no. 2
Biological Activity	IC50 = 24 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 for Assessing the Biological Activity of the Studied DIG on This DBT
Interacting DIG	Silicon dioxide
Biological Activity	Protein expression downregulation (tested by experiment)					[4]
Tested Species	Homo sapiens (Human)
UniProt ID	CP3A4_HUMAN
Transferase (TFase)
DBT Name: VEGF-2 receptor (KDR)				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	FD&C blue no. 2
Biological Activity	IC50 = 3.1 uM (tested by experiment)					[1]
Tested Species	Homo sapiens (Human)
UniProt ID	VGFR2_HUMAN
Hydrolase (HDase)
DBT Name: Protein-tyrosine phosphatase 1D (PTPN11)				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	FD&C blue no. 2
Biological Activity	IC50 = 7940 nM (estimated based on the structural similarity with CHEMBL3692077 )					[5]
Structural Similarity	Tanimoto coefficient = 0.822222222
Tested Species	Homo sapiens (Human)
UniProt ID	PTN11_HUMAN
Potential-driven transporter (PDT)
DBT Name: Solute carrier SLCO2B1 (OATPB)				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	FD&C blue no. 2
Biological Activity	Inhibition ratio = 26 % (tested by experiment)					[6]
Tested Species	Homo sapiens (Human)
UniProt ID	SO2B1_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 for Assessing the Biological Activity of the Studied DIG on This DBT
Interacting DIG	FD&C blue no. 2
Biological Activity	IC50 > 10 uM (tested by experiment)					[1]
Tested Species	Homo sapiens (Human)
UniProt ID	ESR1_HUMAN

References
1	The activities of drug inactive ingredients on biological targets. Science. 2020 Jul 24;369(6502):403-413.
2	Structural basis for inhibition of the fat mass and obesity associated protein (FTO). J Med Chem. 2013 May 9; 56(9):3680-8.
3	Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases. J Med Chem. 2008 Nov 27; 51(22):7053-6.
4	Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
5	US patent application no. 8987474B2, Inhibition of Shp2/PTPN11 Protein Tyrosine Phosphatase by NSC-87877, NSC-117199 and Their Analogs.
6	Bacterial metabolism rescues the inhibition of intestinal drug absorption by food and drug additives. Proc Natl Acad Sci U S A. 2020 Jul 7;117(27):16009-16018.

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