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

General Information of DTT (ID: TTRA6BO)

• DTT Name: Bromodomain-containing protein 4 (BRD4) DTT Info
• Gene Name: BRD4

Molecule-Related Drug & Molecule List

10 Clinical Trial Drug(s) Transported by This DTP

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

32 Patented Agent(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Aminocyclopentenone compound 1	DMYHRJD	N. A.	N. A.	Patented	[4]
Aminocyclopentenone compound 2	DMAYHNI	N. A.	N. A.	Patented	[4]
Aminocyclopentenone compound 3	DMFXK03	N. A.	N. A.	Patented	[4]
Aminocyclopentenone compound 4	DM745TN	N. A.	N. A.	Patented	[4]
Aminocyclopentenone compound 5	DMPW9ES	N. A.	N. A.	Patented	[4]
Aminocyclopentenone compound 6	DM0NJFZ	N. A.	N. A.	Patented	[4]
Benzothiazepine analog 10	DMR6XF4	N. A.	N. A.	Patented	[4]
Benzothiazepine analog 11	DMVC51O	N. A.	N. A.	Patented	[4]
Benzothiazepine analog 12	DM7XQ18	N. A.	N. A.	Patented	[4]
PMID26924192-Compound-102	DMEJ107	N. A.	N. A.	Patented	[4]
PMID26924192-Compound-103	DMWOCP7	N. A.	N. A.	Patented	[4]
PMID26924192-Compound-104	DM346EU	N. A.	N. A.	Patented	[4]
PMID26924192-Compound-105	DMAWLGI	N. A.	N. A.	Patented	[4]
PMID26924192-Compound-20	DMHAOF1	N. A.	N. A.	Patented	[4]
PMID26924192-Compound-21	DM4MZ29	N. A.	N. A.	Patented	[4]
PMID26924192-Compound-22	DMX964E	N. A.	N. A.	Patented	[4]
PMID26924192-Compound-23	DME60LY	N. A.	N. A.	Patented	[4]
PMID26924192-Compound-24	DMDN5Q4	N. A.	N. A.	Patented	[4]
PMID26924192-Compound-25	DMEL7XA	N. A.	N. A.	Patented	[4]
PMID26924192-Compound-30	DMWXNIJ	N. A.	N. A.	Patented	[4]
PMID26924192-Compound-31	DMIFV58	N. A.	N. A.	Patented	[4]
PMID26924192-Compound-32	DM0JSOZ	N. A.	N. A.	Patented	[4]
PMID26924192-Compound-33	DM9NWXM	N. A.	N. A.	Patented	[4]
Pyrazole and thiophene derivative 1	DMKTFJ2	N. A.	N. A.	Patented	[4]
Pyrazole and thiophene derivative 2	DMD51HM	N. A.	N. A.	Patented	[4]
Pyrazole and thiophene derivative 3	DMIKUN9	N. A.	N. A.	Patented	[4]
Pyrazole and thiophene derivative 4	DMDETKY	N. A.	N. A.	Patented	[4]
Pyrrolo-pyrrolone derivative 1	DMN4SE5	N. A.	N. A.	Patented	[4]
Pyrrolo-pyrrolone derivative 2	DM8VYMA	N. A.	N. A.	Patented	[4]
Pyrrolo-pyrrolone derivative 3	DMHGPU1	N. A.	N. A.	Patented	[4]
Pyrrolo-pyrrolone derivative 4	DMFJBZI	N. A.	N. A.	Patented	[4]
Pyrrolo-pyrrolone derivative 5	DMMX0N5	N. A.	N. A.	Patented	[4]

18 Investigative Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BzT-7	DMU13BY	Discovery agent	N.A.	Investigative	[5]
CPI-203	DMXSYTA	Discovery agent	N.A.	Investigative	[6]
GW841819X	DMRL9IN	Discovery agent	N.A.	Investigative	[7]
I-BET151	DMYRUH2	Discovery agent	N.A.	Investigative	[8]
isoxazole azepine compound 3	DMAFC3R	Discovery agent	N.A.	Investigative	[9]
MS417	DMXC30P	Discovery agent	N.A.	Investigative	[10]
MS436	DMNBFX0	Discovery agent	N.A.	Investigative	[11]
PFI-1	DMVFK3J	Discovery agent	N.A.	Investigative	[12]
PMID21851057C4d	DMI1FGV	Discovery agent	N.A.	Investigative	[13]
PMID23517011C9	DMFQVNL	Discovery agent	N.A.	Investigative	[14]
PMID24000170C36	DMHUWZS	Discovery agent	N.A.	Investigative	[15]
PMID24000170C38	DMOLRIY	Discovery agent	N.A.	Investigative	[15]
PMID25408830C1	DM5GL23	Discovery agent	N.A.	Investigative	[16]
PMID25408830C2	DM20E13	Discovery agent	N.A.	Investigative	[16]
PMID25408830C3	DM8SBR2	Discovery agent	N.A.	Investigative	[16]
PMID25703523C7d	DM4PZ37	Discovery agent	N.A.	Investigative	[17]
XD1	DMS3TZ5	Discovery agent	N.A.	Investigative	[18]
XD14	DMUMACD	Discovery agent	N.A.	Investigative	[18]

References

• [1] Targeting bromodomains: epigenetic readers of lysine acetylation.Nat Rev Drug Discov.2014 May;13(5):337-56.
• [2] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [3] Selective inhibition of BET bromodomains. Nature. 2010 Dec 23;468(7327):1067-73.
• [4] BET inhibitors in cancer therapeutics: a patent review.Expert Opin Ther Pat. 2016;26(4):505-22.
• [5] Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family. Bioorg Med Chem. 2012 Mar 15;20(6):1878-86.
• [6] BRD4 is an atypical kinase that phosphorylates serine2 of the RNA polymerase II carboxy-terminal domain. Proc Natl Acad Sci U S A. 2012 May 1;109(18):6927-32.
• [7] Discovery and characterization of small molecule inhibitors of the BET family bromodomains. J Med Chem. 2011 Jun 9;54(11):3827-38.
• [8] Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia. Nature. 2011 Oct 2;478(7370):529-33.
• [9] Discovery, Design, and Optimization of Isoxazole Azepine BET Inhibitors. ACS Med Chem Lett. 2013 Jul 16;4(9):835-40.
• [10] Down-regulation of NF- B transcriptional activity in HIV-associated kidney disease by BRD4 inhibition. J Biol Chem. 2012 Aug 17;287(34):28840-51.
• [11] Structure-guided design of potent diazobenzene inhibitors for the BET bromodomains. J Med Chem. 2013 Nov 27;56(22):9251-64.
• [12] Identification of a chemical probe for bromo and extra C-terminal bromodomain inhibition through optimization of a fragment-derived hit. J Med Chem. 2012 Nov 26;55(22):9831-7.
• [13] 3,5-dimethylisoxazoles act as acetyl-lysine-mimetic bromodomain ligands. J Med Chem. 2011 Oct 13;54(19):6761-70.
• [14] Optimization of 3,5-dimethylisoxazole derivatives as potent bromodomain ligands. J Med Chem. 2013 Apr 25;56(8):3217-27.
• [15] Naphthyridines as novel BET family bromodomain inhibitors. ChemMedChem. 2014 Mar;9(3):580-9.
• [16] 1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain. ACS Med Chem Lett. 2014 Sep 10;5(11):1190-5.
• [17] 9H-purine scaffold reveals induced-fit pocket plasticity of the BRD9 bromodomain. J Med Chem. 2015 Mar 26;58(6):2718-36.
• [18] 4-Acyl pyrroles: mimicking acetylated lysines in histone code reading. Angew Chem Int Ed Engl. 2013 Dec 23;52(52):14055-9.