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)

TimeframeStudies on this Protein(%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's83 (61.03)24.3611
2020's53 (38.97)2.80

Compounds (45)

Drugs with Inhibition Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
ly 303511Homo sapiens (human)IC509.050011
2-(4-morpholinyl)-8-phenyl-4h-1-benzopyran-4-oneHomo sapiens (human)IC5012.400011
entinostatHomo sapiens (human)IC5010.000022
sb 202190Homo sapiens (human)IC502.950022
vorinostatHomo sapiens (human)IC504.158655
ferrocin cHomo sapiens (human)IC5073.000011
n-methylpyrrolidoneHomo sapiens (human)IC502,660.000011
4-Methyl-1,3,4,5-tetrahydro-2H-1,5-benzodiazepin-2-oneHomo sapiens (human)IC50220.000011
nitroxolineHomo sapiens (human)IC500.980022
lenalidomideHomo sapiens (human)IC505.190011
2-methyl-2,3,4,5-tetrahydro-1,5-benzoxazepin-4-oneHomo sapiens (human)IC5080.000011
methyl indole-3-carboxylateHomo sapiens (human)IC50100.000011
2-(3,4-dihydroxyphenyl)-7,8-dihydroxy-1-benzopyran-4-oneHomo sapiens (human)IC500.204011
romidepsinHomo sapiens (human)IC500.036011
belinostatHomo sapiens (human)IC500.027011
panobinostatHomo sapiens (human)IC500.005011
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)IC500.04542121
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)Ki0.011088
volasertibHomo sapiens (human)IC501.070011
nu 7441Homo sapiens (human)IC501.000011
bi 2536Homo sapiens (human)IC500.12111312
bi 2536Homo sapiens (human)Ki0.056011
tg101209Homo sapiens (human)IC500.130044
fedratinibHomo sapiens (human)IC500.290011
jq1 compoundHomo sapiens (human)IC500.8257119115
jq1 compoundHomo sapiens (human)Ki0.019388
dinaciclibHomo sapiens (human)IC5019.000011
gsk525762aHomo sapiens (human)IC500.22163535
gsk525762aHomo sapiens (human)Ki0.07311212
LSM-6732Homo sapiens (human)IC500.05841110
gsk1210151aHomo sapiens (human)IC500.30542323
gsk1210151aHomo sapiens (human)Ki0.102366
i-bet726Homo sapiens (human)IC500.100178
pelabresibHomo sapiens (human)IC500.022055
MS-417Homo sapiens (human)Ki0.016822
sf 1126Homo sapiens (human)IC505.300011
2-methoxy-n-(3-methyl-2-oxo-1,2,3,4-tetrahydroquinazolin-6-yl)benzenesulfonamideHomo sapiens (human)IC500.83761313
cpi203Homo sapiens (human)IC500.092011
pf-06687252Homo sapiens (human)IC50100.000011
dBET6Homo sapiens (human)IC500.065422
MZ1Homo sapiens (human)IC500.672522
MZ1Homo sapiens (human)Ki0.127522
rvx 208Homo sapiens (human)IC502.62232828

Drugs with Activation Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
alprazolamHomo sapiens (human)Kd2.460011
sb 202190Homo sapiens (human)Kd3.400011
volasertibHomo sapiens (human)Kd0.162765
bi 2536Homo sapiens (human)EC500.002010
bi 2536Homo sapiens (human)Kd0.0489109
N-methyl-N-[2-[[[2-[(2-oxo-1,3-dihydroindol-5-yl)amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]methyl]phenyl]methanesulfonamideHomo sapiens (human)Kd0.445011
tg101209Homo sapiens (human)Kd0.123011
fedratinibHomo sapiens (human)Kd0.164011
ro3280Homo sapiens (human)Kd0.215733
bi d1870Homo sapiens (human)Kd3.500011
xmd 8-92Homo sapiens (human)Kd0.835044
lrrk2-in1Homo sapiens (human)Kd0.109733
jq1 compoundHomo sapiens (human)EC500.120333
jq1 compoundHomo sapiens (human)Kd0.09123155
gsk525762aHomo sapiens (human)EC500.440011
gsk525762aHomo sapiens (human)Kd0.05451010
gsk1210151aHomo sapiens (human)Kd0.133922
i-bet726Homo sapiens (human)Kd0.013744
2-methoxy-n-(3-methyl-2-oxo-1,2,3,4-tetrahydroquinazolin-6-yl)benzenesulfonamideHomo sapiens (human)Kd0.136011
MZ1Homo sapiens (human)Kd0.024733
rvx 208Homo sapiens (human)Kd1.13012222
pp242Homo sapiens (human)Kd1.700011

Drugs with Other Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
n-hydroxysuccinimideHomo sapiens (human)DC5050.000011
jq1 compoundHomo sapiens (human)DC505.000011
dBET6Homo sapiens (human)DC500.005111
MZ1Homo sapiens (human)DC500.069333

Enables

This protein enables 12 target(s):

TargetCategoryDefinition
transcription cis-regulatory region bindingmolecular functionBinding 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 bindingmolecular functionBinding to one of the p53 family of proteins. [GOC:hjd]
chromatin bindingmolecular functionBinding 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 activitymolecular functionA 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 activitymolecular functionA 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 bindingmolecular functionBinding to a protein. [GOC:go_curators]
RNA polymerase II CTD heptapeptide repeat kinase activitymolecular functionCatalysis 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 bindingmolecular functionBinding to an enzyme, a protein with catalytic activity. [GOC:jl]
lysine-acetylated histone bindingmolecular functionBinding 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 bindingmolecular functionBinding 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 bindingmolecular functionBinding to a P-TEFb complex. [GOC:pga, PMID:18391197]
histone reader activitymolecular functionA 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):

TargetCategoryDefinition
condensed nuclear chromosomecellular componentA highly compacted molecule of DNA and associated proteins resulting in a cytologically distinct nuclear chromosome. [GOC:elh]
nucleuscellular componentA 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]
nucleoplasmcellular componentThat 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):

TargetCategoryDefinition
chromatin organizationbiological processThe assembly or remodeling of chromatin composed of DNA complexed with histones, other associated proteins, and sometimes RNA. [PMID:20404130]
DNA damage responsebiological processAny 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 IIbiological processAny 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 transductionbiological processAny process that activates or increases the frequency, rate or extent of a canonical NF-kappaB signaling cascade. [GOC:jl]
positive regulation of DNA-templated transcriptionbiological processAny 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 IIbiological processAny 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 responsebiological processAny 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 commitmentbiological processAny process that activates or increases the frequency, rate or extent of T-helper 17 cell lineage commitment. [GOC:BHF, GOC:mah]