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

General Information of Drug (ID: DMRL9IN)

• Drug Name: GW841819X Drug Info
• Synonyms: KB-75882

Indication

Disease Entry	ICD 11	Status	REF
Discovery agent	N.A.	Investigative	[1]

• Cross-matching ID:
  PubChem CID: 13953710
  TTD Drug ID: DMRL9IN

Molecule-Related Drug Atlas

Drug(s) Targeting Bromodomain-containing protein 4 (BRD4)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
CPI-0610	DMPXOYJ	Myelofibrosis	2A20.2	Phase 3	[3]
OTX-015	DMI8RG1	Acute myeloid leukaemia	2A60	Phase 1/2	[3]
PLX2853	DMX168L	Acute myeloid leukaemia	2A60	Phase 1/2	[4]
RVX-208	DM1LO8K	Alzheimer disease	8A20	Phase 1/2	[3]
INCB57643	DMBGU7V	Advanced malignancy	2A00-2F9Z	Phase 1/2	[4]
ABBV-744	DMTEA9C	Acute myeloid leukaemia	2A60	Phase 1	[4]
(+)-JQ1	DM1CZSJ	Testicular cancer	2C80	Phase 1	[5]
GSK525762	DMPAWBN	Haematological malignancy	2B33.Y	Phase 1	[3]
TEN010	DM4UOY5	Advanced solid tumour	2A00-2F9Z	Phase 1	[3]
AZD5153	DMW4GM2	Solid tumour/cancer	2A00-2F9Z	Phase 1	[4]

Drug(s) Targeting Bromodomain-containing protein 3 (BRD3)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
ABBV-744	DMTEA9C	Acute myeloid leukaemia	2A60	Phase 1	[4]
PMID26924192-Compound-104	DM346EU	N. A.	N. A.	Patented	[6]
PMID26924192-Compound-102	DMEJ107	N. A.	N. A.	Patented	[6]
PMID26924192-Compound-103	DMWOCP7	N. A.	N. A.	Patented	[6]
PMID26924192-Compound-105	DMAWLGI	N. A.	N. A.	Patented	[6]
Pyrrolo-pyrrolone derivative 1	DMN4SE5	N. A.	N. A.	Patented	[6]
XD14	DMUMACD	Discovery agent	N.A.	Investigative	[7]
PMID24000170C36	DMHUWZS	Discovery agent	N.A.	Investigative	[8]
PMID24000170C38	DMOLRIY	Discovery agent	N.A.	Investigative	[8]
I-BET151	DMYRUH2	Discovery agent	N.A.	Investigative	[9]

Drug(s) Targeting Bromodomain-containing protein 2 (BRD2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
OTX-015	DMI8RG1	Acute myeloid leukaemia	2A60	Phase 1/2	[3]
ABBV-744	DMTEA9C	Acute myeloid leukaemia	2A60	Phase 1	[4]
PMID26924192-Compound-104	DM346EU	N. A.	N. A.	Patented	[6]
PMID26924192-Compound-102	DMEJ107	N. A.	N. A.	Patented	[6]
PMID26924192-Compound-103	DMWOCP7	N. A.	N. A.	Patented	[6]
PMID26924192-Compound-105	DMAWLGI	N. A.	N. A.	Patented	[6]
Pyrrolo-pyrrolone derivative 1	DMN4SE5	N. A.	N. A.	Patented	[6]
PMID26924192-Compound-106	DM9HRZJ	N. A.	N. A.	Patented	[6]
XD14	DMUMACD	Discovery agent	N.A.	Investigative	[7]
PMID24000170C36	DMHUWZS	Discovery agent	N.A.	Investigative	[8]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Bromodomain-containing protein 2 (BRD2)	TTDP48B	BRD2_HUMAN	Inhibitor	[2]
Bromodomain-containing protein 3 (BRD3)	TTHE657	BRD3_HUMAN	Inhibitor	[2]
Bromodomain-containing protein 4 (BRD4)	TTRA6BO	BRD4_HUMAN	Inhibitor	[2]

References

• [1] 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: 7514).
• [2] Discovery and characterization of small molecule inhibitors of the BET family bromodomains. J Med Chem. 2011 Jun 9;54(11):3827-38.
• [3] Targeting bromodomains: epigenetic readers of lysine acetylation.Nat Rev Drug Discov.2014 May;13(5):337-56.
• [4] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [5] Selective inhibition of BET bromodomains. Nature. 2010 Dec 23;468(7327):1067-73.
• [6] BET inhibitors in cancer therapeutics: a patent review.Expert Opin Ther Pat. 2016;26(4):505-22.
• [7] 4-Acyl pyrroles: mimicking acetylated lysines in histone code reading. Angew Chem Int Ed Engl. 2013 Dec 23;52(52):14055-9.
• [8] Naphthyridines as novel BET family bromodomain inhibitors. ChemMedChem. 2014 Mar;9(3):580-9.
• [9] Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia. Nature. 2011 Oct 2;478(7370):529-33.