Target Information
| Target General Information | Top | |||||
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| Target ID |
T58998
(Former ID: TTDNC00380)
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| Target Name |
Bromodomain and extraterminal domain protein (BET)
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| Synonyms |
Bromodomain and Extra Terminal protein
Click to Show/Hide
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| Gene Name |
NO-GeName
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| Target Type |
Clinical trial target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Myeloproliferative neoplasm [ICD-11: 2A20] | |||||
| UniProt ID | ||||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Clinical Trial Drug(s) | [+] 22 Clinical Trial Drugs | + | ||||
| 1 | CPI-0610 | Drug Info | Phase 3 | Myelofibrosis | [2] | |
| 2 | ZEN-3694 | Drug Info | Phase 2 | Prostate cancer | [3] | |
| 3 | BMS-986158 | Drug Info | Phase 1/2 | Solid tumour/cancer | [4] | |
| 4 | INCB054329 | Drug Info | Phase 1/2 | Solid tumour/cancer | [5] | |
| 5 | INCB057643 | Drug Info | Phase 1/2 | Solid tumour/cancer | [6] | |
| 6 | ODM-207 | Drug Info | Phase 1/2 | Solid tumour/cancer | [7] | |
| 7 | OTX-015 | Drug Info | Phase 1/2 | Acute myeloid leukaemia | [8] | |
| 8 | (+)-JQ1 | Drug Info | Phase 1 | Testicular cancer | [9] | |
| 9 | BAY 1238097 | Drug Info | Phase 1 | Neoplasm | [10] | |
| 10 | BI 894999 | Drug Info | Phase 1 | Solid tumour/cancer | [1] | |
| 11 | CC-90010 | Drug Info | Phase 1 | Non-hodgkin lymphoma | [1] | |
| 12 | CC-90010 | Drug Info | Phase 1 | Glioblastoma of brain | [11] | |
| 13 | CC-95775 | Drug Info | Phase 1 | Non-hodgkin lymphoma | [12] | |
| 14 | FT-1101 | Drug Info | Phase 1 | Haematological malignancy | [1] | |
| 15 | GS-5829 | Drug Info | Phase 1 | Solid tumour/cancer | [1] | |
| 16 | GSK2820151 | Drug Info | Phase 1 | Solid tumour/cancer | [13] | |
| 17 | GSK525762 | Drug Info | Phase 1 | Solid tumour/cancer | [14], [15], [16], [17] | |
| 18 | Mivebresib | Drug Info | Phase 1 | Acute myeloid leukaemia | [1] | |
| 19 | PLX51107 | Drug Info | Phase 1 | Haematological malignancy | [1] | |
| 20 | RG6146 | Drug Info | Phase 1 | Haematological malignancy | [1] | |
| 21 | RO6870810 | Drug Info | Phase 1 | Multiple myeloma | [18] | |
| 22 | ZEN003694 | Drug Info | Phase 1 | Prostate cancer | [19] | |
| Mode of Action | [+] 1 Modes of Action | + | ||||
| Inhibitor | [+] 59 Inhibitor drugs | + | ||||
| 1 | CPI-0610 | Drug Info | [1] | |||
| 2 | ZEN-3694 | Drug Info | [20] | |||
| 3 | BMS-986158 | Drug Info | [1] | |||
| 4 | INCB054329 | Drug Info | [21] | |||
| 5 | INCB057643 | Drug Info | [22] | |||
| 6 | ODM-207 | Drug Info | [23] | |||
| 7 | OTX-015 | Drug Info | [1] | |||
| 8 | (+)-JQ1 | Drug Info | [9] | |||
| 9 | BAY 1238097 | Drug Info | [24] | |||
| 10 | BI 894999 | Drug Info | [1] | |||
| 11 | CC-90010 | Drug Info | [1] | |||
| 12 | CC-90010 | Drug Info | [25] | |||
| 13 | CC-95775 | Drug Info | [26] | |||
| 14 | FT-1101 | Drug Info | [1] | |||
| 15 | GS-5829 | Drug Info | [1] | |||
| 16 | GSK2820151 | Drug Info | [13] | |||
| 17 | GSK525762 | Drug Info | [1] | |||
| 18 | Mivebresib | Drug Info | [1] | |||
| 19 | PLX51107 | Drug Info | [1] | |||
| 20 | RG6146 | Drug Info | [1] | |||
| 21 | RO6870810 | Drug Info | [27] | |||
| 22 | ZEN003694 | Drug Info | [20] | |||
| 23 | Dihydropyrido pyrazinone compound 1 | Drug Info | [28] | |||
| 24 | Isoxazole-based bicyclic compound 1 | Drug Info | [28] | |||
| 25 | Isoxazole-based bicyclic compound 10 | Drug Info | [28] | |||
| 26 | Isoxazole-based bicyclic compound 11 | Drug Info | [28] | |||
| 27 | Isoxazole-based bicyclic compound 12 | Drug Info | [28] | |||
| 28 | Isoxazole-based bicyclic compound 13 | Drug Info | [28] | |||
| 29 | Isoxazole-based bicyclic compound 14 | Drug Info | [28] | |||
| 30 | Isoxazole-based bicyclic compound 15 | Drug Info | [28] | |||
| 31 | Isoxazole-based bicyclic compound 16 | Drug Info | [28] | |||
| 32 | Isoxazole-based bicyclic compound 17 | Drug Info | [28] | |||
| 33 | Isoxazole-based bicyclic compound 18 | Drug Info | [28] | |||
| 34 | Isoxazole-based bicyclic compound 19 | Drug Info | [28] | |||
| 35 | Isoxazole-based bicyclic compound 2 | Drug Info | [28] | |||
| 36 | Isoxazole-based bicyclic compound 3 | Drug Info | [28] | |||
| 37 | Isoxazole-based bicyclic compound 4 | Drug Info | [28] | |||
| 38 | Isoxazole-based bicyclic compound 5 | Drug Info | [28] | |||
| 39 | Isoxazole-based bicyclic compound 6 | Drug Info | [28] | |||
| 40 | Isoxazole-based bicyclic compound 7 | Drug Info | [28] | |||
| 41 | Isoxazole-based bicyclic compound 8 | Drug Info | [28] | |||
| 42 | Isoxazole-based bicyclic compound 9 | Drug Info | [28] | |||
| 43 | PMID26924192-Compound-50 | Drug Info | [28] | |||
| 44 | PMID26924192-Compound-51 | Drug Info | [28] | |||
| 45 | PMID26924192-Compound-52 | Drug Info | [28] | |||
| 46 | PMID26924192-Compound-53 | Drug Info | [28] | |||
| 47 | PMID26924192-Compound-54 | Drug Info | [28] | |||
| 48 | PMID26924192-Compound-55 | Drug Info | [28] | |||
| 49 | PMID26924192-Compound-56 | Drug Info | [28] | |||
| 50 | PMID26924192-Compound-57 | Drug Info | [28] | |||
| 51 | Pyrimido-indole derivative 1 | Drug Info | [28] | |||
| 52 | Pyrimido-indole derivative 2 | Drug Info | [28] | |||
| 53 | Pyrimido-indole derivative 3 | Drug Info | [28] | |||
| 54 | Quinazolinone derivative 3 | Drug Info | [28] | |||
| 55 | Quinazolinone derivative 4 | Drug Info | [28] | |||
| 56 | Quinazolinone derivative 5 | Drug Info | [28] | |||
| 57 | Tetra-hydro-quinoline derivative 2 | Drug Info | [28] | |||
| 58 | Tetra-hydro-quinoline derivative 3 | Drug Info | [28] | |||
| 59 | Tetra-hydro-quinoline derivative 4 | Drug Info | [28] | |||
| Drug Property Profile of Target | Top | |
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| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "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 | Top | |||||
|---|---|---|---|---|---|---|
| Co-Targets | ||||||
| Target Affiliated Biological Pathways | Top | |||||
|---|---|---|---|---|---|---|
| KEGG Pathway | [+] 1 KEGG Pathways | + | ||||
| 1 | SNARE interactions in vesicular transport | |||||
| Reactome | [+] 1 Reactome Pathways | + | ||||
| 1 | COPII (Coat Protein 2) Mediated Vesicle Transport | |||||
| WikiPathways | [+] 3 WikiPathways | + | ||||
| 1 | miR-targeted genes in squamous cell - TarBase | |||||
| 2 | miR-targeted genes in muscle cell - TarBase | |||||
| 3 | miR-targeted genes in lymphocytes - TarBase | |||||
| References | Top | |||||
|---|---|---|---|---|---|---|
| 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 (NCT02419417) Study of BMS-986158 in Subjects With Select Advanced Cancers (BET). U.S. National Institutes of Health. | |||||
| REF 5 | ClinicalTrials.gov (NCT02431260) An Open-Label, Dose-Escalation Study of INCB054329 in Patients With Advanced Malignancies. U.S. National Institutes of Health. | |||||
| REF 6 | ClinicalTrials.gov (NCT02711137) Open-Label Safety and Tolerability Study of INCB057643 in Subjects With Advanced Malignancies. U.S. National Institutes of Health. | |||||
| REF 7 | ClinicalTrials.gov (NCT03035591) ODM-207 in Patients With Advance Solid Tumours (BETIDES). 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 (NCT02369029) BAY1238097, First in Man. U.S. National Institutes of Health. | |||||
| REF 11 | 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 12 | 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 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 | 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 15 | Selective inhibition of BET bromodomains. Nature. 2010 Dec 23;468(7327):1067-73. | |||||
| REF 16 | Suppression of inflammation by a synthetic histone mimic. Nature. 2010 Dec 23;468(7327):1119-23. | |||||
| REF 17 | Small molecules, big targets: drug discovery faces the protein-protein interaction challenge.Nat Rev Drug Discov. 2016 Aug;15(8):533-50. | |||||
| REF 18 | 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 19 | ClinicalTrials.gov (NCT02705469) A Study of ZEN003694 in Patients With Metastatic Castration-Resistant Prostate Cancer. U.S. National Institutes of Health. | |||||
| REF 20 | Clinical pipeline report, company report or official report of Zenith Epigenetics. | |||||
| REF 21 | The Novel Bromodomain and Extraterminal Domain Inhibitor INCB054329 Induces Vulnerabilities in Myeloma Cells That Inform Rational Combination Strategies. Clin Cancer Res. 2019 Jan 1;25(1):300-311. | |||||
| REF 22 | Development of 2 Bromodomain and Extraterminal Inhibitors With Distinct Pharmacokinetic and Pharmacodynamic Profiles for the Treatment of Advanced Malignancies. Clin Cancer Res. 2020 Mar 15;26(6):1247-1257. | |||||
| REF 23 | First-in-human Phase 1 open label study of the BET inhibitor ODM-207 in patients with selected solid tumours. Br J Cancer. 2020 Dec;123(12):1730-1736. | |||||
| REF 24 | Preclinical evaluation of the BET bromodomain inhibitor BAY 1238097 for the treatment of lymphoma. Br J Haematol. 2017 Sep;178(6):936-948. | |||||
| REF 25 | Phase I study of CC-90010, a reversible, oral BET inhibitor in patients with advanced solid tumors and relapsed/refractory non-Hodgkin's lymphoma. Ann Oncol. 2020 Jun;31(6):780-788. | |||||
| REF 26 | Clinical pipeline report, company report or official report of Bristol-Myers Squibb. | |||||
| REF 27 | A Phase 1 study of RO6870810, a novel bromodomain and extra-terminal protein inhibitor, in patients with NUT carcinoma, other solid tumours, or diffuse large B-cell lymphoma. Br J Cancer. 2021 Feb;124(4):744-753. | |||||
| REF 28 | BET inhibitors in cancer therapeutics: a patent review.Expert Opin Ther Pat. 2016;26(4):505-22. | |||||
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