Proteins > Bromodomain-containing protein 4
Page last updated: 2024-08-07 18:27:11
Bromodomain-containing protein 4
A bromodomain-containing protein 4 that is encoded in the genome of human. [PRO:DNx, UniProtKB:O60885]
Synonyms
Protein HUNK1
Research
Bioassay Publications (136)
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 | 83 (61.03) | 24.3611 |
2020's | 53 (38.97) | 2.80 |
Compounds (45)
Drugs with Inhibition Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
ly 303511 | Homo sapiens (human) | IC50 | 9.0500 | 1 | 1 |
2-(4-morpholinyl)-8-phenyl-4h-1-benzopyran-4-one | Homo sapiens (human) | IC50 | 12.4000 | 1 | 1 |
entinostat | Homo sapiens (human) | IC50 | 10.0000 | 2 | 2 |
sb 202190 | Homo sapiens (human) | IC50 | 2.9500 | 2 | 2 |
vorinostat | Homo sapiens (human) | IC50 | 4.1586 | 5 | 5 |
ferrocin c | Homo sapiens (human) | IC50 | 73.0000 | 1 | 1 |
n-methylpyrrolidone | Homo sapiens (human) | IC50 | 2,660.0000 | 1 | 1 |
4-Methyl-1,3,4,5-tetrahydro-2H-1,5-benzodiazepin-2-one | Homo sapiens (human) | IC50 | 220.0000 | 1 | 1 |
nitroxoline | Homo sapiens (human) | IC50 | 0.9800 | 2 | 2 |
lenalidomide | Homo sapiens (human) | IC50 | 5.1900 | 1 | 1 |
2-methyl-2,3,4,5-tetrahydro-1,5-benzoxazepin-4-one | Homo sapiens (human) | IC50 | 80.0000 | 1 | 1 |
methyl indole-3-carboxylate | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
2-(3,4-dihydroxyphenyl)-7,8-dihydroxy-1-benzopyran-4-one | Homo sapiens (human) | IC50 | 0.2040 | 1 | 1 |
romidepsin | Homo sapiens (human) | IC50 | 0.0360 | 1 | 1 |
belinostat | Homo sapiens (human) | IC50 | 0.0270 | 1 | 1 |
panobinostat | Homo sapiens (human) | IC50 | 0.0050 | 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 | 0.0454 | 21 | 21 |
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 | 0.0110 | 8 | 8 |
volasertib | Homo sapiens (human) | IC50 | 1.0700 | 1 | 1 |
nu 7441 | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
bi 2536 | Homo sapiens (human) | IC50 | 0.1211 | 13 | 12 |
bi 2536 | Homo sapiens (human) | Ki | 0.0560 | 1 | 1 |
tg101209 | Homo sapiens (human) | IC50 | 0.1300 | 4 | 4 |
fedratinib | Homo sapiens (human) | IC50 | 0.2900 | 1 | 1 |
jq1 compound | Homo sapiens (human) | IC50 | 0.8257 | 119 | 115 |
jq1 compound | Homo sapiens (human) | Ki | 0.0193 | 8 | 8 |
dinaciclib | Homo sapiens (human) | IC50 | 19.0000 | 1 | 1 |
gsk525762a | Homo sapiens (human) | IC50 | 0.2216 | 35 | 35 |
gsk525762a | Homo sapiens (human) | Ki | 0.0731 | 12 | 12 |
LSM-6732 | Homo sapiens (human) | IC50 | 0.0584 | 11 | 10 |
gsk1210151a | Homo sapiens (human) | IC50 | 0.3054 | 23 | 23 |
gsk1210151a | Homo sapiens (human) | Ki | 0.1023 | 6 | 6 |
i-bet726 | Homo sapiens (human) | IC50 | 0.1001 | 7 | 8 |
pelabresib | Homo sapiens (human) | IC50 | 0.0220 | 5 | 5 |
MS-417 | Homo sapiens (human) | Ki | 0.0168 | 2 | 2 |
sf 1126 | Homo sapiens (human) | IC50 | 5.3000 | 1 | 1 |
2-methoxy-n-(3-methyl-2-oxo-1,2,3,4-tetrahydroquinazolin-6-yl)benzenesulfonamide | Homo sapiens (human) | IC50 | 0.8376 | 13 | 13 |
cpi203 | Homo sapiens (human) | IC50 | 0.0920 | 1 | 1 |
pf-06687252 | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
dBET6 | Homo sapiens (human) | IC50 | 0.0654 | 2 | 2 |
MZ1 | Homo sapiens (human) | IC50 | 0.6725 | 2 | 2 |
MZ1 | Homo sapiens (human) | Ki | 0.1275 | 2 | 2 |
rvx 208 | Homo sapiens (human) | IC50 | 2.6223 | 28 | 28 |
Drugs with Activation Measurements
Drugs with Other Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
n-hydroxysuccinimide | Homo sapiens (human) | DC50 | 50.0000 | 1 | 1 |
jq1 compound | Homo sapiens (human) | DC50 | 5.0000 | 1 | 1 |
dBET6 | Homo sapiens (human) | DC50 | 0.0051 | 1 | 1 |
MZ1 | Homo sapiens (human) | DC50 | 0.0693 | 3 | 3 |
Current status in the discovery of dual BET/HDAC inhibitors.Bioorganic & medicinal chemistry letters, , 01-01, Volume: 31, 2021
Discovery of selective HDAC/BRD4 dual inhibitors as epigenetic probes.European journal of medicinal chemistry, , Jan-01, Volume: 209, 2021
Structure-based design, synthesis and in vitro antiproliferative effects studies of novel dual BRD4/HDAC inhibitors.Bioorganic & medicinal chemistry letters, , 09-01, Volume: 27, Issue:17, 2017
Synthesis and evaluation of novel dual BRD4/HDAC inhibitors.Bioorganic & medicinal chemistry, , 07-15, Volume: 25, Issue:14, 2017
[no title available]European journal of medicinal chemistry, , Jan-05, Volume: 227, 2022
Discovery of 2-((2-methylbenzyl)thio)-6-oxo-4-(3,4,5-trimethoxyphenyl)-1,6-dihydropyrimidine-5-carbonitrile as a novel and effective bromodomain and extra-terminal (BET) inhibitor for the treatment of sepsis.European journal of medicinal chemistry, , Aug-05, Volume: 238, 2022
Medulloblastoma drugs in development: Current leads, trials and drawbacks.European journal of medicinal chemistry, , Apr-05, Volume: 215, 2021
Discovery of selective HDAC/BRD4 dual inhibitors as epigenetic probes.European journal of medicinal chemistry, , Jan-01, Volume: 209, 2021
Discovery of 8-Methyl-pyrrolo[1,2-Journal of medicinal chemistry, , 04-23, Volume: 63, Issue:8, 2020
Structure-Based Discovery and Development of a Series of Potent and Selective Bromodomain and Extra-Terminal Protein Inhibitors.Journal of medicinal chemistry, , 09-26, Volume: 62, Issue:18, 2019
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
Rational design of 5-((1H-imidazol-1-yl)methyl)quinolin-8-ol derivatives as novel bromodomain-containing protein 4 inhibitors.European journal of medicinal chemistry, , Feb-01, Volume: 163, 2019
Benzoxazinone-containing 3,5-dimethylisoxazole derivatives as BET bromodomain inhibitors for treatment of castration-resistant prostate cancer.European journal of medicinal chemistry, , May-25, Volume: 152, 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 QCA570 as an Exceptionally Potent and Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of the Bromodomain and Extra-Terminal (BET) Proteins Capable of Inducing Complete and Durable Tumor Regression.Journal of medicinal chemistry, , Aug-09, Volume: 61, Issue:15, 2018
Drug Discovery Targeting Bromodomain-Containing Protein 4.Journal of medicinal chemistry, , 06-08, Volume: 60, Issue:11, 2017
Discovery of novel [1,2,4]triazolo[4,3-a]quinoxaline aminophenyl derivatives as BET inhibitors for cancer treatment.Bioorganic & medicinal chemistry letters, , 10-15, Volume: 27, Issue:20, 2017
Disrupting Acetyl-Lysine Recognition: Progress in the Development of Bromodomain Inhibitors.Journal of medicinal chemistry, , Feb-25, Volume: 59, Issue:4, 2016
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
Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors.Journal of medicinal chemistry, , 11-11, Volume: 64, Issue:21, 2021
Non-kinase targets of protein kinase inhibitors.Nature reviews. Drug discovery, , Volume: 16, Issue:6, 2017
Dihydropteridinone Inhibitors of BRD4.ACS medicinal chemistry letters, , Feb-11, Volume: 7, Issue:2, 2016
[no title available],
Polo-like Kinase 1 Inhibitors in Human Cancer Therapy: Development and Therapeutic Potential.Journal of medicinal chemistry, , 08-11, Volume: 65, Issue:15, 2022
Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors.Journal of medicinal chemistry, , 11-11, Volume: 64, Issue:21, 2021
Design, synthesis, and biological evaluation of 4,5-dihydro-[1,2,4]triazolo[4,3-f]pteridine derivatives as novel dual-PLK1/BRD4 inhibitors.European journal of medicinal chemistry, , Apr-01, Volume: 191, 2020
Designing Dual Inhibitors of Anaplastic Lymphoma Kinase (ALK) and Bromodomain-4 (BRD4) by Tuning Kinase Selectivity.Journal of medicinal chemistry, , 03-14, Volume: 62, Issue:5, 2019
Dual Inhibition of TAF1 and BET Bromodomains from the BI-2536 Kinase Inhibitor Scaffold.ACS medicinal chemistry letters, , Oct-10, Volume: 10, Issue:10, 2019
Structure-Guided Design and Development of Potent and Selective Dual Bromodomain 4 (BRD4)/Polo-like Kinase 1 (PLK1) Inhibitors.Journal of medicinal chemistry, , 09-13, Volume: 61, Issue:17, 2018
Structure-based optimization of a series of selective BET inhibitors containing aniline or indoline groups.European journal of medicinal chemistry, , Apr-25, Volume: 150, 2018
Privileged Structures and Polypharmacology within and between Protein Families.ACS medicinal chemistry letters, , Dec-13, Volume: 9, Issue:12, 2018
Drug Discovery Targeting Bromodomain-Containing Protein 4.Journal of medicinal chemistry, , 06-08, Volume: 60, Issue:11, 2017
Non-kinase targets of protein kinase inhibitors.Nature reviews. Drug discovery, , Volume: 16, Issue:6, 2017
Discovery of a series of dihydroquinoxalin-2(1H)-ones as selective BET inhibitors from a dual PLK1-BRD4 inhibitor.European journal of medicinal chemistry, , Sep-08, Volume: 137, 2017
Dihydropteridinone Inhibitors of BRD4.ACS medicinal chemistry letters, , Feb-11, Volume: 7, Issue:2, 2016
BRD4 Structure-Activity Relationships of Dual PLK1 Kinase/BRD4 Bromodomain Inhibitor BI-2536.ACS medicinal chemistry letters, , Jul-09, Volume: 6, Issue:7, 2015
[no title available],
Rational Design and Evaluation of 6-(Pyrimidin-2-ylamino)-3,4-dihydroquinoxalin-2(1Journal of medicinal chemistry, , 09-10, Volume: 63, Issue:17, 2020
Drug Discovery Targeting Bromodomain-Containing Protein 4.Journal of medicinal chemistry, , 06-08, Volume: 60, Issue:11, 2017
Non-kinase targets of protein kinase inhibitors.Nature reviews. Drug discovery, , Volume: 16, Issue:6, 2017
Discovery of a series of dihydroquinoxalin-2(1H)-ones as selective BET inhibitors from a dual PLK1-BRD4 inhibitor.European journal of medicinal chemistry, , Sep-08, Volume: 137, 2017
Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer.European journal of medicinal chemistry, , Feb-15, Volume: 230, 2022
Design and Synthesis of Dual EZH2/BRD4 Inhibitors to Target Solid Tumors.Journal of medicinal chemistry, , 05-12, Volume: 65, Issue:9, 2022
Structure-Based Discovery and Optimization of Furo[3,2-Journal of medicinal chemistry, , 04-14, Volume: 65, Issue:7, 2022
Development of BRD4 inhibitors as anti-inflammatory agents and antidotes for arsenicals.Bioorganic & medicinal chemistry letters, , 05-15, Volume: 64, 2022
[no title available]European journal of medicinal chemistry, , Jan-05, Volume: 227, 2022
Discovery of 2-((2-methylbenzyl)thio)-6-oxo-4-(3,4,5-trimethoxyphenyl)-1,6-dihydropyrimidine-5-carbonitrile as a novel and effective bromodomain and extra-terminal (BET) inhibitor for the treatment of sepsis.European journal of medicinal chemistry, , Aug-05, Volume: 238, 2022
Development of an N-Terminal BRD4 Bromodomain-Targeted Degrader.ACS medicinal chemistry letters, , Oct-13, Volume: 13, Issue:10, 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, 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-Guided Design of a "Bump-and-Hole" Bromodomain-Based Degradation Tag.Journal of medicinal chemistry, , 08-12, Volume: 64, Issue:15, 2021
Discovery of 3,5-dimethylisoxazole derivatives as novel, potent inhibitors for bromodomain and extraterminal domain (BET) family.Bioorganic & medicinal chemistry, , 06-01, Volume: 39, 2021
Current status in the discovery of dual BET/HDAC inhibitors.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 38, 2021
Current status in the discovery of dual BET/HDAC inhibitors.Bioorganic & medicinal chemistry letters, , 01-01, Volume: 31, 2021
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
4-Methyl-1,2,3-Triazoles as Journal of medicinal chemistry, , 07-22, Volume: 64, Issue:14, 2021
Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors.Journal of medicinal chemistry, , 11-11, Volume: 64, Issue:21, 2021
Discovery of 8-Methyl-pyrrolo[1,2-Journal of medicinal chemistry, , 04-23, Volume: 63, Issue:8, 2020
BET proteins: Investigating BRDT as a potential target for male contraception.Bioorganic & medicinal chemistry letters, , 03-15, Volume: 30, Issue:6, 2020
Design, synthesis and biological evaluation of novel 6-phenyl-1,3a,4,10b-tetrahydro-2H-benzo[c]thiazolo[4,5-e]azepin-2-one derivatives as potential BRD4 inhibitors.Bioorganic & medicinal chemistry, , 08-01, Volume: 28, Issue:15, 2020
Novel Pyrrolopyridone Bromodomain and Extra-Terminal Motif (BET) Inhibitors Effective in Endocrine-Resistant ER+ Breast Cancer with Acquired Resistance to Fulvestrant and Palbociclib.Journal of medicinal chemistry, , 07-09, Volume: 63, Issue:13, 2020
4-Acyl Pyrroles as Dual BET-BRD7/9 Bromodomain Inhibitors Address BETi Insensitive Human Cancer Cell Lines.Journal of medicinal chemistry, , 12-24, Volume: 63, Issue:24, 2020
Discovery of novel small molecule induced selective degradation of the bromodomain and extra-terminal (BET) bromodomain protein BRD4 and BRD2 with cellular potencies.Bioorganic & medicinal chemistry, , 01-01, Volume: 28, Issue:1, 2020
Identification of 3,5-Dimethylisoxazole Derivatives as BRD4 Inhibitors for the Treatment of Colorectal Cancer.ACS medicinal chemistry letters, , Nov-12, Volume: 11, Issue:11, 2020
Design, synthesis and biological evaluation of indole-2-one derivatives as potent BRD4 inhibitors.European journal of medicinal chemistry, , Dec-15, Volume: 208, 2020
Discovery of a new class of PROTAC BRD4 degraders based on a dihydroquinazolinone derivative and lenalidomide/pomalidomide.Bioorganic & medicinal chemistry, , 01-01, Volume: 28, Issue:1, 2020
Discovery of Thieno[2,3-Journal of medicinal chemistry, , 04-09, Volume: 63, Issue:7, 2020
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
Design, synthesis and biological evaluation of 3,5-dimethylisoxazole and pyridone derivatives as BRD4 inhibitors.Bioorganic & medicinal chemistry letters, , 10-01, Volume: 29, Issue:19, 2019
Structure-Based Discovery and Development of a Series of Potent and Selective Bromodomain and Extra-Terminal Protein Inhibitors.Journal of medicinal chemistry, , 09-26, Volume: 62, Issue:18, 2019
Binding pocket-based design, synthesis and biological evaluation of novel selective BRD4-BD1 inhibitors.Bioorganic & medicinal chemistry, , 05-01, Volume: 27, Issue:9, 2019
Novel phenanthridin-6(5H)-one derivatives as potent and selective BET bromodomain inhibitors: Rational design, synthesis and biological evaluation.European journal of medicinal chemistry, , Oct-01, Volume: 179, 2019
Discovery of Benzo[Journal of medicinal chemistry, , 12-26, Volume: 62, Issue:24, 2019
Pharmacokinetics-Driven Optimization of 7-Methylimidazo[1,5-ACS medicinal chemistry letters, , Dec-12, Volume: 10, Issue:12, 2019
Controlling cellular distribution of drugs with permeability modifying moieties.MedChemComm, , Jun-01, Volume: 10, Issue:6, 2019
Structure-Guided Design and Development of Potent and Selective Dual Bromodomain 4 (BRD4)/Polo-like Kinase 1 (PLK1) Inhibitors.Journal of medicinal chemistry, , 09-13, Volume: 61, Issue:17, 2018
Benzoxazinone-containing 3,5-dimethylisoxazole derivatives as BET bromodomain inhibitors for treatment of castration-resistant prostate cancer.European journal of medicinal chemistry, , May-25, Volume: 152, 2018
Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds.Journal of medicinal chemistry, , 01-25, Volume: 61, Issue:2, 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
BET bromodomain ligands: Probing the WPF shelf to improve BRD4 bromodomain affinity and metabolic stability.Bioorganic & medicinal chemistry, , 07-15, Volume: 26, Issue:11, 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
Y08060: A Selective BET Inhibitor for Treatment of Prostate Cancer.ACS medicinal chemistry letters, , Mar-08, Volume: 9, Issue:3, 2018
Structure-based optimization of a series of selective BET inhibitors containing aniline or indoline groups.European journal of medicinal chemistry, , Apr-25, Volume: 150, 2018
Discovery of QCA570 as an Exceptionally Potent and Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of the Bromodomain and Extra-Terminal (BET) Proteins Capable of Inducing Complete and Durable Tumor Regression.Journal of medicinal chemistry, , Aug-09, Volume: 61, Issue:15, 2018
Targeting Brd4 for cancer therapy: inhibitors and degraders.MedChemComm, , Nov-01, Volume: 9, Issue:11, 2018
GNE-371, a Potent and Selective Chemical Probe for the Second Bromodomains of Human Transcription-Initiation-Factor TFIID Subunit 1 and Transcription-Initiation-Factor TFIID Subunit 1-like.Journal of medicinal chemistry, , 10-25, Volume: 61, Issue:20, 2018
Structure-Based Discovery and Optimization of Benzo[ d]isoxazole Derivatives as Potent and Selective BET Inhibitors for Potential Treatment of Castration-Resistant Prostate Cancer (CRPC).Journal of medicinal chemistry, , 04-12, Volume: 61, Issue:7, 2018
Design, synthesis and biological evaluation of novel 4-phenylisoquinolinone BET bromodomain inhibitors.Bioorganic & medicinal chemistry letters, , 06-01, Volume: 28, Issue:10, 2018
A "Click Chemistry Platform" for the Rapid Synthesis of Bispecific Molecules for Inducing Protein Degradation.Journal of medicinal chemistry, , 01-25, Volume: 61, Issue:2, 2018
Design and Characterization of Novel Covalent Bromodomain and Extra-Terminal Domain (BET) Inhibitors Targeting a Methionine.Journal of medicinal chemistry, , 09-27, Volume: 61, Issue:18, 2018
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
Structure-based design, synthesis and in vitro antiproliferative effects studies of novel dual BRD4/HDAC inhibitors.Bioorganic & medicinal chemistry letters, , 09-01, Volume: 27, Issue:17, 2017
Discovery of a series of dihydroquinoxalin-2(1H)-ones as selective BET inhibitors from a dual PLK1-BRD4 inhibitor.European journal of medicinal chemistry, , Sep-08, Volume: 137, 2017
Discovery of N-(4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl)ethanesulfonamide (ABBV-075/Mivebresib), a Potent and Orally Available Bromodomain and Extraterminal Domain (BET) Family Bromodomain Inhibitor.Journal of medicinal chemistry, , 10-26, Volume: 60, Issue:20, 2017
Design, synthesis and biological evaluation of 7-methylimidazo[1,5-a]pyrazin-8(7H)-one derivatives as BRD4 inhibitors.Bioorganic & medicinal chemistry, , 04-15, Volume: 25, Issue:8, 2017
Drug Discovery Targeting Bromodomain-Containing Protein 4.Journal of medicinal chemistry, , 06-08, Volume: 60, Issue:11, 2017
Synthesis and evaluation of novel dual BRD4/HDAC inhibitors.Bioorganic & medicinal chemistry, , 07-15, Volume: 25, Issue:14, 2017
Structure-Based Discovery of 4-(6-Methoxy-2-methyl-4-(quinolin-4-yl)-9H-pyrimido[4,5-b]indol-7-yl)-3,5-dimethylisoxazole (CD161) as a Potent and Orally Bioavailable BET Bromodomain Inhibitor.Journal of medicinal chemistry, , 05-11, Volume: 60, Issue:9, 2017
Design and characterization of bivalent BET inhibitors.Nature chemical biology, , Volume: 12, Issue:12, 2016
Disrupting Acetyl-Lysine Recognition: Progress in the Development of Bromodomain Inhibitors.Journal of medicinal chemistry, , Feb-25, Volume: 59, Issue:4, 2016
Development of 4,5-dihydro-benzodiazepinone derivatives as a new chemical series of BRD4 inhibitors.European journal of medicinal chemistry, , Oct-04, Volume: 121, 2016
Targeting epigenetic reader and eraser: Rational design, synthesis and in vitro evaluation of dimethylisoxazoles derivatives as BRD4/HDAC dual inhibitors.Bioorganic & medicinal chemistry letters, , 06-15, Volume: 26, Issue:12, 2016
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
Discovery of Benzotriazolo[4,3-d][1,4]diazepines as Orally Active Inhibitors of BET Bromodomains.ACS medicinal chemistry letters, , Feb-11, Volume: 7, Issue:2, 2016
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
Discovery and structure-activity relationship studies of N6-benzoyladenine derivatives as novel BRD4 inhibitors.Bioorganic & medicinal chemistry, , Mar-01, Volume: 23, Issue:5, 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
Biased multicomponent reactions to develop novel bromodomain inhibitors.Journal of medicinal chemistry, , Nov-13, Volume: 57, Issue:21, 2014
Affinity map of bromodomain protein 4 (BRD4) interactions with the histone H4 tail and the small molecule inhibitor JQ1.The Journal of biological chemistry, , Mar-28, Volume: 289, Issue:13, 2014
Discovery, Design, and Optimization of Isoxazole Azepine BET Inhibitors.ACS medicinal chemistry letters, , Sep-12, Volume: 4, Issue:9, 2013
Optimization of 3,5-dimethylisoxazole derivatives as potent bromodomain ligands.Journal of medicinal chemistry, , Apr-25, Volume: 56, Issue:8, 2013
Bromodomains: are readers right for epigenetic therapy?ACS medicinal chemistry letters, , Sep-13, Volume: 3, Issue:9, 2012
Progress in the development and application of small molecule inhibitors of bromodomain-acetyl-lysine interactions.Journal of medicinal chemistry, , Nov-26, Volume: 55, Issue:22, 2012
Fragment-based discovery of bromodomain inhibitors part 2: optimization of phenylisoxazole sulfonamides.Journal of medicinal chemistry, , Jan-26, Volume: 55, Issue:2, 2012
Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.Bioorganic & medicinal chemistry, , Mar-15, Volume: 20, Issue:6, 2012
Development of live-cell imaging probes for monitoring histone modifications.Bioorganic & medicinal chemistry, , Mar-15, Volume: 20, Issue:6, 2012
[no title available],
Identification and Optimization of a Ligand-Efficient Benzoazepinone Bromodomain and Extra Terminal (BET) Family Acetyl-Lysine Mimetic into the Oral Candidate Quality Molecule I-BET432.Journal of medicinal chemistry, , 11-24, Volume: 65, Issue:22, 2022
Discovery of a Novel Bromodomain and Extra Terminal Domain (BET) Protein Inhibitor, I-BET282E, Suitable for Clinical Progression.Journal of medicinal chemistry, , 08-26, Volume: 64, Issue:16, 2021
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
Design, synthesis and biological evaluation of novel 6-phenyl-1,3a,4,10b-tetrahydro-2H-benzo[c]thiazolo[4,5-e]azepin-2-one derivatives as potential BRD4 inhibitors.Bioorganic & medicinal chemistry, , 08-01, Volume: 28, Issue:15, 2020
Sulfoximines as Rising Stars in Modern Drug Discovery? Current Status and Perspective on an Emerging Functional Group in Medicinal Chemistry.Journal of medicinal chemistry, , 12-10, Volume: 63, Issue:23, 2020
Lead optimization and efficacy evaluation of quinazoline-based BET family inhibitors for potential treatment of cancer and inflammatory diseases.Bioorganic & medicinal chemistry letters, , 05-15, Volume: 29, Issue:10, 2019
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
Rational design of 5-((1H-imidazol-1-yl)methyl)quinolin-8-ol derivatives as novel bromodomain-containing protein 4 inhibitors.European journal of medicinal chemistry, , Feb-01, Volume: 163, 2019
Structure-guided discovery of a novel, potent, and orally bioavailable 3,5-dimethylisoxazole aryl-benzimidazole BET bromodomain inhibitor.Bioorganic & medicinal chemistry, , 02-01, Volume: 27, Issue:3, 2019
Discovery and lead identification of quinazoline-based BRD4 inhibitors.Bioorganic & medicinal chemistry letters, , 11-15, Volume: 28, Issue:21, 2018
Structure-based optimization of a series of selective BET inhibitors containing aniline or indoline groups.European journal of medicinal chemistry, , Apr-25, Volume: 150, 2018
Benzoxazinone-containing 3,5-dimethylisoxazole derivatives as BET bromodomain inhibitors for treatment of castration-resistant prostate cancer.European journal of medicinal chemistry, , May-25, Volume: 152, 2018
Targeting Brd4 for cancer therapy: inhibitors and degraders.MedChemComm, , Nov-01, Volume: 9, Issue:11, 2018
Design, synthesis and biological evaluation of novel 4-phenylisoquinolinone BET bromodomain inhibitors.Bioorganic & medicinal chemistry letters, , 06-01, Volume: 28, Issue:10, 2018
Straightforward hit identification approach in fragment-based discovery of bromodomain-containing protein 4 (BRD4) inhibitors.Bioorganic & medicinal chemistry, , 07-23, Volume: 26, Issue:12, 2018
Design and Characterization of Novel Covalent Bromodomain and Extra-Terminal Domain (BET) Inhibitors Targeting a Methionine.Journal of medicinal chemistry, , 09-27, Volume: 61, Issue:18, 2018
Discovery of a series of dihydroquinoxalin-2(1H)-ones as selective BET inhibitors from a dual PLK1-BRD4 inhibitor.European journal of medicinal chemistry, , Sep-08, Volume: 137, 2017
Discovery of novel [1,2,4]triazolo[4,3-a]quinoxaline aminophenyl derivatives as BET inhibitors for cancer treatment.Bioorganic & medicinal chemistry letters, , 10-15, Volume: 27, Issue:20, 2017
Structure-Based Discovery of 4-(6-Methoxy-2-methyl-4-(quinolin-4-yl)-9H-pyrimido[4,5-b]indol-7-yl)-3,5-dimethylisoxazole (CD161) as a Potent and Orally Bioavailable BET Bromodomain Inhibitor.Journal of medicinal chemistry, , 05-11, Volume: 60, Issue:9, 2017
New Synthetic Routes to Triazolo-benzodiazepine Analogues: Expanding the Scope of the Bump-and-Hole Approach for Selective Bromo and Extra-Terminal (BET) Bromodomain Inhibition.Journal of medicinal chemistry, , Feb-25, Volume: 59, Issue:4, 2016
Optimization of a Series of Bivalent Triazolopyridazine Based Bromodomain and Extraterminal Inhibitors: The Discovery of (3R)-4-[2-[4-[1-(3-Methoxy-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)-4-piperidyl]phenoxy]ethyl]-1,3-dimethyl-piperazin-2-one (AZD5153).Journal of medicinal chemistry, , 09-08, Volume: 59, Issue:17, 2016
Disrupting Acetyl-Lysine Recognition: Progress in the Development of Bromodomain Inhibitors.Journal of medicinal chemistry, , Feb-25, Volume: 59, Issue:4, 2016
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
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
Discovery of epigenetic regulator I-BET762: lead optimization to afford a clinical candidate inhibitor of the BET bromodomains.Journal of medicinal chemistry, , Oct-10, Volume: 56, Issue:19, 2013
Optimization of 3,5-dimethylisoxazole derivatives as potent bromodomain ligands.Journal of medicinal chemistry, , Apr-25, Volume: 56, Issue:8, 2013
Discovery, Design, and Optimization of Isoxazole Azepine BET Inhibitors.ACS medicinal chemistry letters, , Sep-12, Volume: 4, Issue:9, 2013
Fragment-based discovery of bromodomain inhibitors part 2: optimization of phenylisoxazole sulfonamides.Journal of medicinal chemistry, , Jan-26, Volume: 55, Issue:2, 2012
Development of live-cell imaging probes for monitoring histone modifications.Bioorganic & medicinal chemistry, , Mar-15, Volume: 20, Issue:6, 2012
Discovery and characterization of small molecule inhibitors of the BET family bromodomains.Journal of medicinal chemistry, , Jun-09, Volume: 54, Issue:11, 2011
Discovery of 4-Hydroxyquinazoline Derivatives as Small Molecular BET/PARP1 Inhibitors That Induce Defective Homologous Recombination and Lead to Synthetic Lethality for Triple-Negative Breast Cancer Therapy.Journal of medicinal chemistry, , 05-12, Volume: 65, Issue:9, 2022
Non-kinase targets of protein kinase inhibitors.Nature reviews. Drug discovery, , Volume: 16, Issue:6, 2017
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
[no title available],
Discovery of a Novel Bromodomain and Extra Terminal Domain (BET) Protein Inhibitor, I-BET282E, Suitable for Clinical Progression.Journal of medicinal chemistry, , 08-26, Volume: 64, Issue:16, 2021
GSK789: A Selective Inhibitor of the First Bromodomains (BD1) of the Bromo and Extra Terminal Domain (BET) Proteins.Journal of medicinal chemistry, , 09-10, Volume: 63, Issue:17, 2020
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
Structure-guided discovery of a novel, potent, and orally bioavailable 3,5-dimethylisoxazole aryl-benzimidazole BET bromodomain inhibitor.Bioorganic & medicinal chemistry, , 02-01, Volume: 27, Issue:3, 2019
BET bromodomain ligands: Probing the WPF shelf to improve BRD4 bromodomain affinity and metabolic stability.Bioorganic & medicinal chemistry, , 07-15, Volume: 26, Issue:11, 2018
Structure-based design, synthesis and in vitro antiproliferative effects studies of novel dual BRD4/HDAC inhibitors.Bioorganic & medicinal chemistry letters, , 09-01, Volume: 27, Issue:17, 2017
Structure-Based Discovery of 4-(6-Methoxy-2-methyl-4-(quinolin-4-yl)-9H-pyrimido[4,5-b]indol-7-yl)-3,5-dimethylisoxazole (CD161) as a Potent and Orally Bioavailable BET Bromodomain Inhibitor.Journal of medicinal chemistry, , 05-11, Volume: 60, Issue:9, 2017
Disrupting Acetyl-Lysine Recognition: Progress in the Development of Bromodomain Inhibitors.Journal of medicinal chemistry, , Feb-25, Volume: 59, Issue:4, 2016
Discovery of Benzotriazolo[4,3-d][1,4]diazepines as Orally Active Inhibitors of BET Bromodomains.ACS medicinal chemistry letters, , Feb-11, Volume: 7, Issue:2, 2016
Design and characterization of bivalent BET inhibitors.Nature chemical biology, , Volume: 12, Issue:12, 2016
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
Discovery and structure-activity relationship studies of N6-benzoyladenine derivatives as novel BRD4 inhibitors.Bioorganic & medicinal chemistry, , Mar-01, Volume: 23, Issue:5, 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
Discovery, Design, and Optimization of Isoxazole Azepine BET Inhibitors.ACS medicinal chemistry letters, , Sep-12, Volume: 4, Issue:9, 2013
Optimization of 3,5-dimethylisoxazole derivatives as potent bromodomain ligands.Journal of medicinal chemistry, , Apr-25, Volume: 56, Issue:8, 2013
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
Targeting Brd4 for cancer therapy: inhibitors and degraders.MedChemComm, , Nov-01, Volume: 9, Issue:11, 2018
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
Structure-based design, synthesis and in vitro antiproliferative effects studies of novel dual BRD4/HDAC inhibitors.Bioorganic & medicinal chemistry letters, , 09-01, Volume: 27, Issue:17, 2017
The discovery of I-BET726 (GSK1324726A), a potent tetrahydroquinoline ApoA1 up-regulator and selective BET bromodomain inhibitor.Journal of medicinal chemistry, , Oct-09, Volume: 57, Issue:19, 2014
Discovery of 2-((2-methylbenzyl)thio)-6-oxo-4-(3,4,5-trimethoxyphenyl)-1,6-dihydropyrimidine-5-carbonitrile as a novel and effective bromodomain and extra-terminal (BET) inhibitor for the treatment of sepsis.European journal of medicinal chemistry, , Aug-05, Volume: 238, 2022
Clinical candidates modulating protein-protein interactions: The fragment-based experience.European journal of medicinal chemistry, , Apr-01, Volume: 167, 2019
Rational design of 5-((1H-imidazol-1-yl)methyl)quinolin-8-ol derivatives as novel bromodomain-containing protein 4 inhibitors.European journal of medicinal chemistry, , Feb-01, Volume: 163, 2019
Straightforward hit identification approach in fragment-based discovery of bromodomain-containing protein 4 (BRD4) inhibitors.Bioorganic & medicinal chemistry, , 07-23, Volume: 26, Issue:12, 2018
Methylpyrrole inhibitors of BET bromodomains.Bioorganic & medicinal chemistry letters, , 05-15, Volume: 27, Issue:10, 2017
Fragment-Based, Structure-Enabled Discovery of Novel Pyridones and Pyridone Macrocycles as Potent Bromodomain and Extra-Terminal Domain (BET) Family Bromodomain Inhibitors.Journal of medicinal chemistry, , 05-11, Volume: 60, Issue:9, 2017
Development of BRD4 inhibitors as anti-inflammatory agents and antidotes for arsenicals.Bioorganic & medicinal chemistry letters, , 05-15, Volume: 64, 2022
Design, synthesis and biological evaluation of indole-2-one derivatives as potent BRD4 inhibitors.European journal of medicinal chemistry, , Dec-15, Volume: 208, 2020
Chiral Analogues of PFI-1 as BET Inhibitors and Their Functional Role in Myeloid Malignancies.ACS medicinal chemistry letters, , Oct-08, Volume: 11, Issue:10, 2020
Design, synthesis and biological evaluation of 3,5-dimethylisoxazole and pyridone derivatives as BRD4 inhibitors.Bioorganic & medicinal chemistry letters, , 10-01, Volume: 29, Issue:19, 2019
Design, synthesis and biological evaluation of benzo[cd]indol-2(1H)-ones derivatives as BRD4 inhibitors.European journal of medicinal chemistry, , May-25, Volume: 152, 2018
BET bromodomain ligands: Probing the WPF shelf to improve BRD4 bromodomain affinity and metabolic stability.Bioorganic & medicinal chemistry, , 07-15, Volume: 26, Issue:11, 2018
Straightforward hit identification approach in fragment-based discovery of bromodomain-containing protein 4 (BRD4) inhibitors.Bioorganic & medicinal chemistry, , 07-23, Volume: 26, Issue:12, 2018
Development of 4,5-dihydro-benzodiazepinone derivatives as a new chemical series of BRD4 inhibitors.European journal of medicinal chemistry, , Oct-04, Volume: 121, 2016
Discovery of novel small-molecule inhibitors of BRD4 using structure-based virtual screening.Journal of medicinal chemistry, , Oct-24, Volume: 56, Issue:20, 2013
Optimization of 3,5-dimethylisoxazole derivatives as potent bromodomain ligands.Journal of medicinal chemistry, , Apr-25, Volume: 56, Issue:8, 2013
Identification of a chemical probe for bromo and extra C-terminal bromodomain inhibition through optimization of a fragment-derived hit.Journal of medicinal chemistry, , Nov-26, Volume: 55, Issue:22, 2012
Amide-to-Ester Substitution as a Strategy for Optimizing PROTAC Permeability and Cellular Activity.Journal of medicinal chemistry, , 12-23, Volume: 64, Issue:24, 2021
Estimating the cooperativity of PROTAC-induced ternary complexes using RSC medicinal chemistry, , Oct-20, Volume: 12, Issue:10, 2021
Proteolysis targeting chimeras (PROTACs) in 'beyond rule-of-five' chemical space: Recent progress and future challenges.Bioorganic & medicinal chemistry letters, , 07-01, Volume: 29, Issue:13, 2019
Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds.Journal of medicinal chemistry, , 01-25, Volume: 61, Issue:2, 2018
A "Click Chemistry Platform" for the Rapid Synthesis of Bispecific Molecules for Inducing Protein Degradation.Journal of medicinal chemistry, , 01-25, Volume: 61, Issue:2, 2018
Dual-target inhibitors of poly (ADP-ribose) polymerase-1 for cancer therapy: Advances, challenges, and opportunities.European journal of medicinal chemistry, , Feb-15, Volume: 230, 2022
Discovery of 2-((2-methylbenzyl)thio)-6-oxo-4-(3,4,5-trimethoxyphenyl)-1,6-dihydropyrimidine-5-carbonitrile as a novel and effective bromodomain and extra-terminal (BET) inhibitor for the treatment of sepsis.European journal of medicinal chemistry, , Aug-05, Volume: 238, 2022
[no title available]European journal of medicinal chemistry, , Jan-05, Volume: 227, 2022
CRCM5484: A BET-BDII Selective Compound with Differential Anti-leukemic Drug Modulation.Journal of medicinal chemistry, , 04-14, Volume: 65, Issue:7, 2022
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 Thieno[2,3-Journal of medicinal chemistry, , 04-09, Volume: 63, Issue:7, 2020
Design and Synthesis of a Highly Selective and Journal of medicinal chemistry, , 09-10, Volume: 63, Issue:17, 2020
Discovery of Journal of medicinal chemistry, , 05-28, Volume: 63, Issue:10, 2020
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
Design, synthesis and biological evaluation of 3,5-dimethylisoxazole and pyridone derivatives as BRD4 inhibitors.Bioorganic & medicinal chemistry letters, , 10-01, Volume: 29, Issue:19, 2019
Binding pocket-based design, synthesis and biological evaluation of novel selective BRD4-BD1 inhibitors.Bioorganic & medicinal chemistry, , 05-01, Volume: 27, Issue:9, 2019
Discovery of Benzo[Journal of medicinal chemistry, , 12-26, Volume: 62, Issue:24, 2019
Design, synthesis and biological evaluation of hypolipidemic compounds based on BRD4 inhibitor RVX-208.Bioorganic & medicinal chemistry letters, , 08-15, Volume: 29, Issue:16, 2019
Rational design of 5-((1H-imidazol-1-yl)methyl)quinolin-8-ol derivatives as novel bromodomain-containing protein 4 inhibitors.European journal of medicinal chemistry, , Feb-01, Volume: 163, 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 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
Structure-based design, synthesis and in vitro antiproliferative effects studies of novel dual BRD4/HDAC inhibitors.Bioorganic & medicinal chemistry letters, , 09-01, Volume: 27, Issue:17, 2017
Drug Discovery Targeting Bromodomain-Containing Protein 4.Journal of medicinal chemistry, , 06-08, Volume: 60, Issue:11, 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
Development of 4,5-dihydro-benzodiazepinone derivatives as a new chemical series of BRD4 inhibitors.European journal of medicinal chemistry, , Oct-04, Volume: 121, 2016
Disrupting Acetyl-Lysine Recognition: Progress in the Development of Bromodomain Inhibitors.Journal of medicinal chemistry, , Feb-25, Volume: 59, Issue:4, 2016
New Synthetic Routes to Triazolo-benzodiazepine Analogues: Expanding the Scope of the Bump-and-Hole Approach for Selective Bromo and Extra-Terminal (BET) Bromodomain Inhibition.Journal of medicinal chemistry, , Feb-25, Volume: 59, Issue:4, 2016
Discovery and structure-activity relationship studies of N6-benzoyladenine derivatives as novel BRD4 inhibitors.Bioorganic & medicinal chemistry, , Mar-01, Volume: 23, Issue:5, 2015
Enables
This protein enables 12 target(s):
Target | Category | Definition |
transcription cis-regulatory region binding | molecular function | Binding to a specific sequence of DNA that is part of a regulatory region that controls transcription of that section of the DNA. The transcribed region might be described as a gene, cistron, or operon. [GOC:txnOH] |
p53 binding | molecular function | Binding to one of the p53 family of proteins. [GOC:hjd] |
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] |
transcription coregulator activity | molecular function | A transcription regulator activity that modulates the transcription of specific gene sets via binding to a DNA-bound DNA-binding transcription factor, either on its own or as part of a complex. Coregulators often act by altering chromatin structure and modifications. For example, one class of transcription coregulators modifies chromatin structure through covalent modification of histones. A second class remodels the conformation of chromatin in an ATP-dependent fashion. A third class modulates interactions of DNA-bound DNA-binding transcription factors with other transcription coregulators. [GOC:txnOH-2018, PMID:10213677, PMID:16858867, PMID:24203923, PMID:25957681, Wikipedia:Transcription_coregulator] |
transcription coactivator activity | molecular function | A transcription coregulator activity that activates or increases the transcription of specific gene sets via binding to a DNA-bound DNA-binding transcription factor, either on its own or as part of a complex. Coactivators often act by altering chromatin structure and modifications. For example, one class of transcription coactivators modifies chromatin structure through covalent modification of histones. A second class remodels the conformation of chromatin in an ATP-dependent fashion. A third class modulates interactions of DNA-bound DNA-binding transcription factors with other transcription coregulators. A fourth class of coactivator activity is the bridging of a DNA-binding transcription factor to the general (basal) transcription machinery. The Mediator complex, which bridges sequence-specific DNA binding transcription factors and RNA polymerase, is also a transcription coactivator. [GOC:txnOH-2018, PMID:10213677, PMID:16858867] |
protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
RNA polymerase II CTD heptapeptide repeat kinase activity | molecular function | Catalysis of the reaction: ATP + RNA polymerase II large subunit CTD heptapeptide repeat (consensus YSPTSPS) = ADP + H+ + phosphorylated RNA polymerase II. [EC:2.7.11.23, GOC:mah, PMID:28248323] |
enzyme binding | molecular function | Binding to an enzyme, a protein with catalytic activity. [GOC:jl] |
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] |
RNA polymerase II C-terminal domain binding | molecular function | Binding to the C-terminal domain (CTD) of the largest subunit of RNA polymerase II. The CTD is comprised of repeats of a heptapeptide with the consensus sequence YSPTSPS. The number of repeats varies with the species and a minimum number of repeats is required for RNAP II function. [PMID:20889714] |
P-TEFb complex binding | molecular function | Binding to a P-TEFb complex. [GOC:pga, PMID:18391197] |
histone reader activity | molecular function | A chromatin adaptor that recognizes specific forms of histones, either modified by a post-translational modification, or the unmodified form. Histone readers have roles in many processes, including in centromere function or in modulating the accessibility of cis-regulatory regions to the transcription machinery. [PMID:11498575, PMID:25688442, PMID:31082667, PMID:32260176, PMID:34726351] |
Located In
This protein is located in 3 target(s):
Target | Category | Definition |
condensed nuclear chromosome | cellular component | A highly compacted molecule of DNA and associated proteins resulting in a cytologically distinct nuclear chromosome. [GOC:elh] |
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] |
nucleoplasm | cellular component | That part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653] |
Involved In
This protein is involved in 8 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] |
DNA damage response | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a stimulus indicating damage to its DNA from environmental insults or errors during metabolism. [GOC:go_curators] |
positive regulation of transcription elongation by RNA polymerase II | biological process | Any process that activates or increases the frequency, rate or extent of transcription elongation, the extension of an RNA molecule after transcription initiation and promoter clearance by the addition of ribonucleotides, catalyzed by RNA polymerase II. [GOC:mah, GOC:txnOH] |
positive regulation of canonical NF-kappaB signal transduction | biological process | Any process that activates or increases the frequency, rate or extent of a canonical NF-kappaB signaling cascade. [GOC:jl] |
positive regulation of DNA-templated transcription | biological process | Any process that activates or increases the frequency, rate or extent of cellular DNA-templated transcription. [GOC:go_curators, GOC:txnOH] |
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] |
regulation of inflammatory response | biological process | Any process that modulates the frequency, rate or extent of the inflammatory response, the immediate defensive reaction (by vertebrate tissue) to infection or injury caused by chemical or physical agents. [GOC:ai] |
positive regulation of T-helper 17 cell lineage commitment | biological process | Any process that activates or increases the frequency, rate or extent of T-helper 17 cell lineage commitment. [GOC:BHF, GOC:mah] |