Details of the Drug Combination

General Information of Drug Combination (ID: DCO1CGT)

Drug Combination Name

(-)-englerin A Eltanexor oral

Indication

Disease Entry	Status	REF
Ewing sarcoma	Investigative	[1]

Component Drugs

(-)-englerin A DMPQBWY

Eltanexor oral DM7CLEZ

Small molecular drug

N.A.

2D MOL

3D MOL is unavailable

3D MOL

High-throughput Screening Result

Testing Cell Line: TC-71

Zero Interaction Potency (ZIP) Score: 9.599

Bliss Independence Score: 7.536

Loewe Additivity Score: 13.946

LHighest Single Agent (HSA) Score: 5.736

Molecular Interaction Atlas of This Drug Combination

Molecular Interaction Atlas (MIA)

Indication(s) of (-)-englerin A

Disease Entry	ICD 11	Status	REF
Discovery agent	N.A.	Investigative	[2]

(-)-englerin A Interacts with 2 DTT Molecule(s)

DTT Name	DTT ID	UniProt ID	Mode of Action	REF
Short transient receptor potential channel 5 (TRPC5)	TT32NQ1	TRPC5_HUMAN	Agonist	[4]
Short transient receptor potential channel 4 (TRPC4)	TTX0H5W	TRPC4_HUMAN	Agonist	[4]
------------------------------------------------------------------------------------

Indication(s) of Eltanexor oral

Disease Entry	ICD 11	Status	REF
Colorectal cancer	2B91.Z	Phase 1/2	[3]
Myelodysplastic syndrome	2A37	Phase 1/2	[3]
Prostate cancer	2C82.0	Phase 1/2	[3]

Eltanexor oral Interacts with 1 DTT Molecule(s)

DTT Name	DTT ID	UniProt ID	Mode of Action	REF
Exportin-1 (XPO1)	TTCJUR4	XPO1_HUMAN	Inhibitor	[3]
------------------------------------------------------------------------------------

References

1	Recurrent recessive mutation in deoxyguanosine kinase causes idiopathic noncirrhotic portal hypertension.Hepatology. 2016 Jun;63(6):1977-86. doi: 10.1002/hep.28499. Epub 2016 Mar 31.
2	Enantioselective synthesis of (-)-englerins A and B. Angew Chem Int Ed Engl. 2010 May 3;49(20):3517-9.
3	Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
4	(-)-Englerin is a potent and selective activator of TRPC4 and TRPC5 calcium channels. Angew Chem Int Ed Engl. 2015 Mar 16;54(12):3787-91.