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

General Information of Drug (ID: DMCBGLW)

Drug Name

GSK2636771 Drug Info

Synonyms

GSK2636771; 1372540-25-4; GSK-2636771; 2-methyl-1-(2-methyl-3-(trifluoromethyl)benzyl)-6-morpholino-1H-benzo[d]imidazole-4-carboxylic acid; UNII-DW94IAT0LS; DW94IAT0LS; GSK 2636771; 2-Methyl-1-((2-methyl-3-(trifluoromethyl)phenyl)methyl)-6-(4-morpholinyl)-1H-benzimidazole-4-carboxylic acid; 2-methyl-1-[[2-methyl-3-(trifluoromethyl)phenyl]methyl]-6-morpholin-4-ylbenzimidazole-4-carboxylic acid; lic acid; XTKLTGBKIDQGQL-UHFFFAOYSA-N

Indication

Disease Entry	ICD 11	Status	REF
Prostate cancer	2C82.0	Phase 1	[1]
Solid tumour/cancer	2A00-2F9Z	Phase 1	[2]

Cross-matching ID

PubChem CID: 56949517
CAS Number: CAS 1372540-25-4
TTD Drug ID: DMCBGLW

Molecule-Related Drug Atlas

Molecule Type:

DTT

Drug Status:

Clinical Trial Drug(s)

Discontinued Drug(s)

Investigative Drug(s)

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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]
BAY 1082439	DMLRGX1	Solid tumour/cancer	2A00-2F9Z	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]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

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Drug Therapeutic Target (DTT)

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

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References

1	Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
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: 7967).
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	Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
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.