Details of the Drug Combination

General Information of Drug Combination (ID: DC9XF10)

• Drug Combination Name: (-)-englerin A + AZD8055
• Indication: Ewing sarcoma; Status: Investigative [1]
• Component Drugs:
  (-)-englerin A (DMPQBWY): Small molecular drug
  AZD8055 (DM7L8SG): Small molecular drug
• High-throughput Screening Result:
  Testing Cell Line: TC-71
  Zero Interaction Potency (ZIP) Score: 2.824
  Bliss Independence Score: 1.865
  Loewe Additivity Score: 6.453
  LHighest Single Agent (HSA) Score: 8.586

Molecular Interaction Atlas of This Drug Combination

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 AZD8055

Disease Entry	ICD 11	Status	REF
Solid tumour/cancer	2A00-2F9Z	Discontinued in Phase 1/2	[3]

AZD8055 Interacts with 1 DTT Molecule(s)

DTT Name	DTT ID	UniProt ID	Mode of Action	REF
Serine/threonine-protein kinase mTOR (mTOR)	TTCJG29	MTOR_HUMAN	Inhibitor	[5]

References

• [1] CheMBL Affinity Phenotypic Cellular Interaction Assay ID: CHEMBL1125966
• [2] Enantioselective synthesis of (-)-englerins A and B. Angew Chem Int Ed Engl. 2010 May 3;49(20):3517-9.
• [3] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7714).
• [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.
• [5] Clinical pipeline report, company report or official report of AstraZeneca (2009).