Details of the Drug Combination

General Information of Drug Combination (ID: DCIMDPG)

• Drug Combination Name: PHA848125 + THZ1
• Indication: Diffuse intrinsic pontine glioma; Status: Investigative [1]
• Component Drugs:
  PHA848125 (DMS2Q9G): Small molecular drug
  THZ1 (DMU10FE): Small molecular drug
• High-throughput Screening Result:
  Testing Cell Line: DIPG25
  Zero Interaction Potency (ZIP) Score: 2.517
  Bliss Independence Score: 1.176
  Loewe Additivity Score: 2.978
  LHighest Single Agent (HSA) Score: 5.421

Molecular Interaction Atlas of This Drug Combination

Indication(s) of PHA848125

Disease Entry	ICD 11	Status	REF
Thymic cancer	2C27	Phase 2	[2]

PHA848125 Interacts with 1 DTT Molecule(s)

DTT Name	DTT ID	UniProt ID	Mode of Action	REF
Cyclin-dependent kinase 2 (CDK2)	TT7HF4W	CDK2_HUMAN	Inhibitor	[4]

Indication(s) of THZ1

Disease Entry	ICD 11	Status	REF
Nasopharyngeal carcinoma	2B6B	Investigative	[3]

THZ1 Interacts with 1 DTT Molecule(s)

DTT Name	DTT ID	UniProt ID	Mode of Action	REF
Cyclin-dependent kinase 7 (CDK7)	TTQYF7G	CDK7_HUMAN	Inhibitor	[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] 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: 7938).
• [3] Super-Enhancers Promote Transcriptional Dysregulation in Nasopharyngeal Carcinoma.Cancer Res. 2017 Dec 1;77(23):6614-6626.
• [4] Identification of N,1,4,4-tetramethyl-8-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide (PHA-848125), a potent, orally available cyclin dependent kinase inhibitor. J Med Chem. 2009 Aug 27;52(16):5152-63.
• [5] Targeting transcription regulation in cancer with a covalent CDK7 inhibitor. Nature. 2014 Jul 31;511(7511):616-20.