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

General Information of Drug (ID: DM8SBR2)

Drug Name

PMID25408830C3 Drug Info

Synonyms

GSK-5959; 901245-65-6; GSK5959; GSK 5959; 4uye; GTPL7811; MolPort-004-921-361; HMS1821D17; EX-A2263; BCP16039; ZINC8594565; BDBM50032912; AKOS000481208; MCULE-6727694163; CS-4867; NCGC00107508-01; HY-18665; C301-5895; 9F9; N-[

Indication

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

Cross-matching ID

PubChem CID: 15990224
TTD Drug ID: DM8SBR2

Molecule-Related Drug Atlas

Molecule Type:

DTT

Drug Status:

Clinical Trial Drug(s)

Investigative Drug(s)

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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	[2]
OTX-015	DMI8RG1	Acute myeloid leukaemia	2A60	Phase 1/2	[2]
PLX2853	DMX168L	Acute myeloid leukaemia	2A60	Phase 1/2	[3]
RVX-208	DM1LO8K	Alzheimer disease	8A20	Phase 1/2	[2]
INCB57643	DMBGU7V	Advanced malignancy	2A00-2F9Z	Phase 1/2	[3]
ABBV-744	DMTEA9C	Acute myeloid leukaemia	2A60	Phase 1	[3]
(+)-JQ1	DM1CZSJ	Testicular cancer	2C80	Phase 1	[4]
GSK525762	DMPAWBN	Haematological malignancy	2B33.Y	Phase 1	[2]
TEN010	DM4UOY5	Advanced solid tumour	2A00-2F9Z	Phase 1	[2]
AZD5153	DMW4GM2	Solid tumour/cancer	2A00-2F9Z	Phase 1	[3]
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Drug(s) Targeting Bromodomain and PHD finger containing 1 (BRPF1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
NI-57	DM52ITO	Discovery agent	N.A.	Investigative	[5]
OF-1	DMK8LEC	Discovery agent	N.A.	Investigative	[5]
PMID25408830C1	DM5GL23	Discovery agent	N.A.	Investigative	[1]
PMID25974391C34	DMGWZA3	Discovery agent	N.A.	Investigative	[6]
PMID25408830C2	DM20E13	Discovery agent	N.A.	Investigative	[1]
PFI-4	DMPKXNZ	Discovery agent	N.A.	Investigative	[5]
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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
Bromodomain and PHD finger containing 1 (BRPF1)	TTT46BN	BRPF1_HUMAN	Inhibitor	[1]
Bromodomain-containing protein 4 (BRD4)	TTRA6BO	BRD4_HUMAN	Inhibitor	[1]

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References

1	1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain. ACS Med Chem Lett. 2014 Sep 10;5(11):1190-5.
2	Targeting bromodomains: epigenetic readers of lysine acetylation.Nat Rev Drug Discov.2014 May;13(5):337-56.
3	Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
4	Selective inhibition of BET bromodomains. Nature. 2010 Dec 23;468(7327):1067-73.
5	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: 2730).
6	Discovery of a Chemical Tool Inhibitor Targeting the Bromodomains of TRIM24 and BRPF. J Med Chem. 2016 Feb 25;59(4):1642-7.