Details of the Drug Combination

General Information of Drug Combination (ID: DCSPJJD)

• Drug Combination Name: Exherin + (-)-englerin A
• Indication: Ewing sarcoma; Status: Investigative [1]
• Component Drugs:
  Exherin (DMC1I56): Small molecular drug
  (-)-englerin A (DMPQBWY): Small molecular drug
• High-throughput Screening Result:
  Testing Cell Line: TC-71
  Zero Interaction Potency (ZIP) Score: 5.396
  Bliss Independence Score: 1.317
  Loewe Additivity Score: 0.358
  LHighest Single Agent (HSA) Score: 6.363

Molecular Interaction Atlas of This Drug Combination

Indication(s) of Exherin

Disease Entry	ICD 11	Status	REF
Solid tumour/cancer	2A00-2F9Z	Phase 2	[2]

Exherin Interacts with 1 DTT Molecule(s)

DTT Name	DTT ID	UniProt ID	Mode of Action	REF
Neural cadherin (CDH2)	TT1WS0T	CADH2_HUMAN	Binder	[4]

Indication(s) of (-)-englerin A

Disease Entry	ICD 11	Status	REF
Discovery agent	N.A.	Investigative	[3]

(-)-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	[5]
Short transient receptor potential channel 4 (TRPC4)	TTX0H5W	TRPC4_HUMAN	Agonist	[5]

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] ClinicalTrials.gov (NCT00264433) A Study of the Safety and Effects of ADH-1 Given Intravenously as a Single Agent. U.S. National Institutes of Health.
• [3] Enantioselective synthesis of (-)-englerins A and B. Angew Chem Int Ed Engl. 2010 May 3;49(20):3517-9.
• [4] Clinical and pharmacological phase I evaluation of Exherin (ADH-1), a selective anti-N-cadherin peptide in patients with N-cadherin-expressing soli... Ann Oncol. 2009 Apr;20(4):741-5.
• [5] (-)-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.