Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DMLRGX1)

• Drug Name: BAY 1082439 Drug Info

Indication

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

• Cross-matching ID:
  PubChem CID: 136336430
  TTD Drug ID: DMLRGX1

Molecule-Related Drug Atlas

Drug(s) Targeting PI3-kinase beta (PIK3CB)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Buparlisib	DM1WEHC	Breast cancer	2C60-2C65	Phase 3	[3]
PQR309	DMMCYZ8	Squamous head and neck cell carcinom	2D60.0	Phase 2	[4]
PA-799	DMLSYJQ	Colorectal cancer	2B91.Z	Phase 1/2	[5]
AZD8186	DMWYF1H	Solid tumour/cancer	2A00-2F9Z	Phase 1	[6]
GSK2636771	DMCBGLW	Prostate cancer	2C82.0	Phase 1	[7]
AZD6482	DMVP4E5	Thrombosis	DB61-GB90	Terminated	[8]
PP121	DMU8KTO	Discovery agent	N.A.	Investigative	[9]
PIK-75	DM9BQTX	Discovery agent	N.A.	Investigative	[10]
KU-0060648	DMQWS6U	Discovery agent	N.A.	Investigative	[11]
PI-3065	DMCQUWI	Discovery agent	N.A.	Investigative	[12]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
PI3-kinase beta (PIK3CB)	TTTHBCA	PK3CB_HUMAN	Modulator	[2]

References

• [1] ClinicalTrials.gov (NCT01728311) Open Label Study of BAY1082439 in Patients With Advanced Cancer. U.S. National Institutes of Health.
• [2] Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
• [3] Targeting the phosphoinositide 3-kinase pathway in cancer. Nat Rev Drug Discov. 2009 Aug;8(8):627-44.
• [4] 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. (Target id: 2154).
• [5] The selective class I PI3K inhibitor CH5132799 targets human cancers harboring oncogenic PIK3CA mutations. Clin Cancer Res. 2011 May 15;17(10):3272-81.
• [6] National Cancer Institute Drug Dictionary (drug id 751594).
• [7] 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: 7967).
• [8] Human target validation of phosphoinositide 3-kinase (PI3K)beta: effects on platelets and insulin sensitivity, using AZD6482 a novel PI3Kbeta inhibitor. J Thromb Haemost. 2012 Oct;10(10):2127-36.
• [9] Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nat Chem Biol. 2008 Nov;4(11):691-9.
• [10] Synthesis and biological evaluation of sulfonylhydrazone-substituted imidazo[1,2-a]pyridines as novel PI3 kinase p110alpha inhibitors. Bioorg Med Chem. 2007 Sep 1;15(17):5837-44.
• [11] 1-substituted (Dibenzo[b,d]thiophen-4-yl)-2-morpholino-4H-chromen-4-ones endowed with dual DNA-PK/PI3-K inhibitory activity. J Med Chem. 2013 Aug 22;56(16):6386-401.
• [12] Inactivation of PI(3)K p110delta breaks regulatory T-cell-mediated immune tolerance to cancer. Nature. 2014 Jun 19;510(7505):407-11.