Target Information

Target General Information

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Target ID

T58998 (Former ID: TTDNC00380)

Target Name

Bromodomain and extraterminal domain protein (BET)

Synonyms

Bromodomain and Extra Terminal protein

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Gene Name

NO-GeName

Target Type

Clinical trial target

[1]

Disease

[+] 1 Target-related Diseases

Myeloproliferative neoplasm [ICD-11: 2A20]

UniProt ID

NOUNIPROTAC

Drugs and Modes of Action

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Clinical Trial Drug(s)

[+] 10 Clinical Trial Drugs

CPI-0610

Drug Info

Phase 3

Myelofibrosis

[2]

BMS-986158

Drug Info

Phase 1/2

Solid tumour/cancer

[7]

OTX-015

Drug Info

Phase 1/2

Acute myeloid leukaemia

[8]

BI 894999

Drug Info

Phase 1

Solid tumour/cancer

[1]

FT-1101

Drug Info

Phase 1

Haematological malignancy

[1]

GS-5829

Drug Info

Phase 1

Solid tumour/cancer

[1]

GSK525762

Drug Info

Phase 1

Solid tumour/cancer

[16], [17], [18], [19]

Mivebresib

Drug Info

Phase 1

Acute myeloid leukaemia

[1]

PLX51107

Drug Info

Phase 1

Haematological malignancy

[1]

RG6146

Drug Info

Phase 1

Haematological malignancy

[1]

Mode of Action

[+] 1 Modes of Action

Inhibitor

[+] 43 Inhibitor drugs

CPI-0610

Drug Info

[1]

BMS-986158

Drug Info

[1]

OTX-015

Drug Info

[1]

BI 894999

Drug Info

[1]

FT-1101

Drug Info

[1]

GS-5829

Drug Info

[1]

GSK525762

Drug Info

[1]

Mivebresib

Drug Info

[1]

PLX51107

Drug Info

[1]

RG6146

Drug Info

[1]

Dihydropyrido pyrazinone compound 1

Drug Info

[20]

Isoxazole-based bicyclic compound 1

Drug Info

[20]

Isoxazole-based bicyclic compound 10

Drug Info

[20]

Isoxazole-based bicyclic compound 13

Drug Info

[20]

Isoxazole-based bicyclic compound 14

Drug Info

[20]

Isoxazole-based bicyclic compound 15

Drug Info

[20]

Isoxazole-based bicyclic compound 16

Drug Info

[20]

Isoxazole-based bicyclic compound 17

Drug Info

[20]

Isoxazole-based bicyclic compound 18

Drug Info

[20]

Isoxazole-based bicyclic compound 19

Drug Info

[20]

Isoxazole-based bicyclic compound 3

Drug Info

[20]

Isoxazole-based bicyclic compound 4

Drug Info

[20]

Isoxazole-based bicyclic compound 5

Drug Info

[20]

Isoxazole-based bicyclic compound 6

Drug Info

[20]

Isoxazole-based bicyclic compound 7

Drug Info

[20]

Isoxazole-based bicyclic compound 8

Drug Info

[20]

Isoxazole-based bicyclic compound 9

Drug Info

[20]

PMID26924192-Compound-50

Drug Info

[20]

PMID26924192-Compound-51

Drug Info

[20]

PMID26924192-Compound-52

Drug Info

[20]

PMID26924192-Compound-53

Drug Info

[20]

PMID26924192-Compound-54

Drug Info

[20]

PMID26924192-Compound-55

Drug Info

[20]

PMID26924192-Compound-56

Drug Info

[20]

PMID26924192-Compound-57

Drug Info

[20]

Pyrimido-indole derivative 1

Drug Info

[20]

Pyrimido-indole derivative 2

Drug Info

[20]

Pyrimido-indole derivative 3

Drug Info

[20]

Quinazolinone derivative 3

Drug Info

[20]

Quinazolinone derivative 4

Drug Info

[20]

Quinazolinone derivative 5

Drug Info

[20]

Tetra-hydro-quinoline derivative 3

Drug Info

[20]

Tetra-hydro-quinoline derivative 4

Drug Info

[20]

Drug Property Profile of Target

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(1) Molecular Weight (mw) based Drug Clustering

(2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering

(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering

(4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering

(5) Rotatable Bond Count (rotbonds) based Drug Clustering

(6) Topological Polar Surface Area (polararea) based Drug Clustering

"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five

Co-Targets

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Co-Targets

Co-Targets Info

Target Affiliated Biological Pathways

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KEGG Pathway

[+] 1 KEGG Pathways

SNARE interactions in vesicular transport

Reactome

[+] 1 Reactome Pathways

COPII (Coat Protein 2) Mediated Vesicle Transport

WikiPathways

[+] 3 WikiPathways

miR-targeted genes in squamous cell - TarBase

miR-targeted genes in muscle cell - TarBase

miR-targeted genes in lymphocytes - TarBase

References

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REF 1

Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)

REF 2

ClinicalTrials.gov (NCT04603495) Study of CPI-0610 in Myelofibrosis (MF) (MANIFEST-2). U.S. National Institutes of Health.

REF 3

ClinicalTrials.gov (NCT04471974) ZEN-3694, Enzalutamide, and Pembrolizumab for the Treatment of Metastatic Castration-Resistant Prostate Cancer. U.S. National Institutes of Health.

REF 4

ClinicalTrials.gov (NCT02711137) Open-Label Safety and Tolerability Study of INCB057643 in Subjects With Advanced Malignancies. U.S. National Institutes of Health.

REF 5

ClinicalTrials.gov (NCT03035591) ODM-207 in Patients With Advance Solid Tumours (BETIDES). U.S. National Institutes of Health.

REF 6

ClinicalTrials.gov (NCT02431260) An Open-Label, Dose-Escalation Study of INCB054329 in Patients With Advanced Malignancies. U.S. National Institutes of Health.

REF 7

ClinicalTrials.gov (NCT02419417) Study of BMS-986158 in Subjects With Select Advanced Cancers (BET). U.S. National Institutes of Health.

REF 8

ClinicalTrials.gov (NCT02303782) A Study Assessing tOTX015 in Combination With Azacitidine (AZA) or AZA Single Agent in Patients With Newly-diagnosed Acute Myeloid Leukemia (AML) Not Candidate for Standard Intensive Induction Therapy (SIIT). U.S. National Institutes of Health.

REF 9

Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)

REF 10

ClinicalTrials.gov (NCT04089527) Study to Evaluate the Safety, Tolerability, Pharmacokinetic and Pharmacodynamic of CC-95775 in Subjects With Advanced Solid Tumors and Relapsed/Refractory Non-Hodgkin Lymphoma. U.S. National Institutes of Health.

REF 11

ClinicalTrials.gov (NCT02705469) A Study of ZEN003694 in Patients With Metastatic Castration-Resistant Prostate Cancer. U.S. National Institutes of Health.

REF 12

ClinicalTrials.gov (NCT02369029) BAY1238097, First in Man. U.S. National Institutes of Health.

REF 13

ClinicalTrials.gov (NCT02630251) Dose Escalation Study of GSK2820151 in Subjects With Advanced or Recurrent Solid Tumors. U.S. National Institutes of Health.

REF 14

ClinicalTrials.gov (NCT03068351) Study of Bromodomain and Extra-Terminal Protein (BET) Inhibitor RO6870810 as Mono- and Combination Therapy in Advanced Multiple Myeloma. U.S. National Institutes of Health.

REF 15

ClinicalTrials.gov (NCT04047303) CNS Penetration, PK and PD of Preoperative CC-90010 in Progressive/Recurrent Diffuse Astrocytoma, Anaplastic Astrocytoma and Glioblastoma. U.S. National Institutes of Health.

REF 16

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: 7033).

REF 17

Selective inhibition of BET bromodomains. Nature. 2010 Dec 23;468(7327):1067-73.

REF 18

Suppression of inflammation by a synthetic histone mimic. Nature. 2010 Dec 23;468(7327):1119-23.

REF 19

Small molecules, big targets: drug discovery faces the protein-protein interaction challenge.Nat Rev Drug Discov. 2016 Aug;15(8):533-50.

REF 20

BET inhibitors in cancer therapeutics: a patent review.Expert Opin Ther Pat. 2016;26(4):505-22.

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