Proteins > Bromodomain-containing protein 3
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Bromodomain-containing protein 3
A bromodomain-containing protein 3 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q15059]
Synonyms
RING3-like protein
Research
Bioassay Publications (29)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 19 (65.52) | 24.3611 |
| 2020's | 10 (34.48) | 2.80 |
Compounds (9)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| ly 303511 | Homo sapiens (human) | IC50 | 11.5000 | 1 | 1 |
| 2-(4-morpholinyl)-8-phenyl-4h-1-benzopyran-4-one | Homo sapiens (human) | IC50 | 13.7000 | 1 | 1 |
| 6h-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide, 4-(4-chlorophenyl)-n-(4-hydroxyphenyl)-2,3,9-trimethyl-, (6s)- | Homo sapiens (human) | IC50 | 0.0609 | 4 | 4 |
| 6h-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide, 4-(4-chlorophenyl)-n-(4-hydroxyphenyl)-2,3,9-trimethyl-, (6s)- | Homo sapiens (human) | Ki | 0.0082 | 6 | 6 |
| jq1 compound | Homo sapiens (human) | IC50 | 0.0573 | 18 | 16 |
| jq1 compound | Homo sapiens (human) | Ki | 0.0078 | 4 | 4 |
| gsk525762a | Homo sapiens (human) | IC50 | 0.2070 | 5 | 5 |
| gsk525762a | Homo sapiens (human) | Ki | 0.0617 | 4 | 4 |
| LSM-6732 | Homo sapiens (human) | IC50 | 0.0390 | 3 | 3 |
| gsk1210151a | Homo sapiens (human) | IC50 | 0.1531 | 4 | 4 |
| gsk1210151a | Homo sapiens (human) | Ki | 0.0148 | 2 | 2 |
| i-bet726 | Homo sapiens (human) | IC50 | 0.1201 | 4 | 5 |
| rvx 208 | Homo sapiens (human) | IC50 | 13.7543 | 7 | 7 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| jq1 compound | Homo sapiens (human) | Kd | 0.0599 | 10 | 8 |
| gsk525762a | Homo sapiens (human) | Kd | 0.0476 | 6 | 6 |
| gsk1210151a | Homo sapiens (human) | Kd | 0.0352 | 2 | 2 |
| i-bet726 | Homo sapiens (human) | Kd | 0.0200 | 1 | 1 |
| rvx 208 | Homo sapiens (human) | Kd | 2.3736 | 7 | 7 |
Medulloblastoma drugs in development: Current leads, trials and drawbacks.European journal of medicinal chemistry, , Apr-05, Volume: 215, 2021
Discovery, structural insight, and bioactivities of BY27 as a selective inhibitor of the second bromodomains of BET proteins.European journal of medicinal chemistry, , Nov-15, Volume: 182, 2019
Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression.Journal of medicinal chemistry, , 01-25, Volume: 61, Issue:2, 2018
Drug Discovery Targeting Bromodomain-Containing Protein 4.Journal of medicinal chemistry, , 06-08, Volume: 60, Issue:11, 2017
Structure-Based Design of γ-Carboline Analogues as Potent and Specific BET Bromodomain Inhibitors.Journal of medicinal chemistry, , Jun-25, Volume: 58, Issue:12, 2015
Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site.Journal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
Structure-Based Discovery and Optimization of Furo[3,2-Journal of medicinal chemistry, , 04-14, Volume: 65, Issue:7, 2022
A Structure-based Design Approach for Generating High Affinity BRD4 D1-Selective Chemical Probes.Journal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
Discovery of Novel Dual-Target Inhibitor of Bromodomain-Containing Protein 4/Casein Kinase 2 Inducing Apoptosis and Autophagy-Associated Cell Death for Triple-Negative Breast Cancer Therapy.Journal of medicinal chemistry, , 12-23, Volume: 64, Issue:24, 2021
[no title available]Journal of medicinal chemistry, , 12-09, Volume: 64, Issue:23, 2021
Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffold Hopping, Optimization, and Pharmacological Evaluation.Journal of medicinal chemistry, , 05-28, Volume: 63, Issue:10, 2020
Discovery of Thieno[2,3-Journal of medicinal chemistry, , 04-09, Volume: 63, Issue:7, 2020
Controlling cellular distribution of drugs with permeability modifying moieties.MedChemComm, , Jun-01, Volume: 10, Issue:6, 2019
Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase-Bromodomain Inhibitor.Journal of medicinal chemistry, , 10-25, Volume: 61, Issue:20, 2018
Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression.Journal of medicinal chemistry, , 01-25, Volume: 61, Issue:2, 2018
Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation.European journal of medicinal chemistry, , May-10, Volume: 151, 2018
Structure-Based Design of γ-Carboline Analogues as Potent and Specific BET Bromodomain Inhibitors.Journal of medicinal chemistry, , Jun-25, Volume: 58, Issue:12, 2015
Development of live-cell imaging probes for monitoring histone modifications.Bioorganic & medicinal chemistry, , Mar-15, Volume: 20, Issue:6, 2012
[no title available],
Discovery of benzo[f]pyrido[4,3-b][1,4]oxazepin-10-one derivatives as orally available bromodomain and extra-terminal domain (BET) inhibitors with efficacy in an in vivo psoriatic animal model.Bioorganic & medicinal chemistry, , 03-15, Volume: 34, 2021
Discovery, structural insight, and bioactivities of BY27 as a selective inhibitor of the second bromodomains of BET proteins.European journal of medicinal chemistry, , Nov-15, Volume: 182, 2019
Fragment-based drug discovery of 2-thiazolidinones as BRD4 inhibitors: 2. Structure-based optimization.Journal of medicinal chemistry, , Feb-12, Volume: 58, Issue:3, 2015
Structure-Based Design of γ-Carboline Analogues as Potent and Specific BET Bromodomain Inhibitors.Journal of medicinal chemistry, , Jun-25, Volume: 58, Issue:12, 2015
Development of live-cell imaging probes for monitoring histone modifications.Bioorganic & medicinal chemistry, , Mar-15, Volume: 20, Issue:6, 2012
Fragment-based discovery of bromodomain inhibitors part 2: optimization of phenylisoxazole sulfonamides.Journal of medicinal chemistry, , Jan-26, Volume: 55, Issue:2, 2012
Discovery and characterization of small molecule inhibitors of the BET family bromodomains.Journal of medicinal chemistry, , Jun-09, Volume: 54, Issue:11, 2011
Design, Synthesis, and Biological Activity of 1,2,3-Triazolobenzodiazepine BET Bromodomain Inhibitors.ACS medicinal chemistry letters, , Dec-14, Volume: 8, Issue:12, 2017
Discovery of a Small-Molecule Bromodomain-Containing Protein 4 (BRD4) Inhibitor That Induces AMP-Activated Protein Kinase-Modulated Autophagy-Associated Cell Death in Breast Cancer.Journal of medicinal chemistry, , 12-28, Volume: 60, Issue:24, 2017
Structure-Based Design of a Bromodomain and Extraterminal Domain (BET) Inhibitor Selective for the N-Terminal Bromodomains That Retains an Anti-inflammatory and Antiproliferative Phenotype.Journal of medicinal chemistry, , 09-10, Volume: 63, Issue:17, 2020
Fragment-based drug discovery of 2-thiazolidinones as BRD4 inhibitors: 2. Structure-based optimization.Journal of medicinal chemistry, , Feb-12, Volume: 58, Issue:3, 2015
Structure-Based Design of γ-Carboline Analogues as Potent and Specific BET Bromodomain Inhibitors.Journal of medicinal chemistry, , Jun-25, Volume: 58, Issue:12, 2015
Identification of a novel series of BET family bromodomain inhibitors: binding mode and profile of I-BET151 (GSK1210151A).Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 22, Issue:8, 2012
Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site.Journal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffold Hopping, Optimization, and Pharmacological Evaluation.Journal of medicinal chemistry, , 05-28, Volume: 63, Issue:10, 2020
Discovery of Benzo[Journal of medicinal chemistry, , 12-26, Volume: 62, Issue:24, 2019
Discovery of Tetrahydroquinoxalines as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the Second Bromodomain.Journal of medicinal chemistry, , 05-24, Volume: 61, Issue:10, 2018
Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation.European journal of medicinal chemistry, , May-10, Volume: 151, 2018
Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase-Bromodomain Inhibitor.Journal of medicinal chemistry, , 10-25, Volume: 61, Issue:20, 2018
Drug Discovery Targeting Bromodomain-Containing Protein 4.Journal of medicinal chemistry, , 06-08, Volume: 60, Issue:11, 2017
Discovery of Benzo[cd]indol-2(1H)-ones as Potent and Specific BET Bromodomain Inhibitors: Structure-Based Virtual Screening, Optimization, and Biological Evaluation.Journal of medicinal chemistry, , Feb-25, Volume: 59, Issue:4, 2016
Enables
This protein enables 5 target(s):
| Target | Category | Definition |
|---|
| chromatin binding | molecular function | Binding to chromatin, the network of fibers of DNA, protein, and sometimes RNA, that make up the chromosomes of the eukaryotic nucleus during interphase. [GOC:jl, ISBN:0198506732, PMID:20404130] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| lysine-acetylated histone binding | molecular function | Binding to a histone in which a lysine residue has been modified by acetylation. [GOC:BHF, GOC:mah, GOC:rl, PMID:17582821] |
| lncRNA binding | molecular function | Binding to a long noncoding RNA (lncRNA). [PMID:25578728] |
| molecular condensate scaffold activity | molecular function | Binding and bringing together two or more macromolecules in contact, permitting those molecules to organize as a molecular condensate. [PMID:28225081] |
Located In
This protein is located in 1 target(s):
| Target | Category | Definition |
|---|
| nucleus | cellular component | A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators] |
Part Of
This protein is part of 1 target(s):
| Target | Category | Definition |
|---|
| chromatin | cellular component | The ordered and organized complex of DNA, protein, and sometimes RNA, that forms the chromosome. [GOC:elh, PMID:20404130] |
Involved In
This protein is involved in 5 target(s):
| Target | Category | Definition |
|---|
| chromatin organization | biological process | The assembly or remodeling of chromatin composed of DNA complexed with histones, other associated proteins, and sometimes RNA. [PMID:20404130] |
| regulation of transcription by RNA polymerase II | biological process | Any process that modulates the frequency, rate or extent of transcription mediated by RNA polymerase II. [GOC:go_curators, GOC:txnOH] |
| endodermal cell differentiation | biological process | The process in which a relatively unspecialized cell acquires the specialized features of an endoderm cell, a cell of the inner of the three germ layers of the embryo. [CL:0000223, GOC:yaf, PMID:17624332] |
| positive regulation of transcription by RNA polymerase II | biological process | Any process that activates or increases the frequency, rate or extent of transcription from an RNA polymerase II promoter. [GOC:go_curators, GOC:txnOH] |
| protein localization to chromatin | biological process | Any process in which a protein is transported to, or maintained at, a part of a chromosome that is organized into chromatin. [GOC:mah] |