Page last updated: 2024-08-05 15:50:08

bromodomain-containing protein 4 inhibitor

Any inhibitor of bromodomain-containing protein 4 (BRD4).

ChEBI ID: 137114

Members (2)

MemberDefinitionClass
jq1 compoundA member of the class of thienotriazolodiazepines that is the tert-butyl ester of [(6S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl]acetic acid. An inhibitor of bromodomain-containing protein 4 that exhibits anti-cancer and cardioprotective properties.JQ1
pelabresibAn organic heterotricyclic compound that is 4H-[1,2]oxazolo[5,4-d][2]benzazepine substituted by methyl, 2-amino-2-oxoethyl, and 4-chlorophenyl groups at positions 1, 4S and 6, respectively. It is a small molecule inhibitor of bromodomain and extra-terminal (BET) proteins and exhibits antineoplastic activity.pelabresib

Research

Studies (118)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's70 (59.32)24.3611
2020's48 (40.68)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials1 (0.80%)5.53%
Reviews10 (8.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other114 (91.20%)84.16%

Protein Targets (34)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
cytochrome P450 2C9, partialHomo sapiens (human)Potency10.684011
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency11.987711
EWS/FLI fusion proteinHomo sapiens (human)Potency5.227644
Fumarate hydrataseHomo sapiens (human)Potency37.221211
GVesicular stomatitis virusPotency10.684011
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency10.684011
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency10.684012
Interferon betaHomo sapiens (human)Potency4.199927
polyproteinZika virusPotency37.221211
PPM1D proteinHomo sapiens (human)Potency3.119214

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Bromodomain testis-specific proteinHomo sapiens (human)IC500.19021313
Bromodomain-containing protein 1Homo sapiens (human)IC5044.500011
Bromodomain-containing protein 2Homo sapiens (human)IC500.09592222
Bromodomain-containing protein 2Homo sapiens (human)Ki0.012844
Bromodomain-containing protein 3Homo sapiens (human)IC500.05731818
Bromodomain-containing protein 3Homo sapiens (human)Ki0.007844
Bromodomain-containing protein 4Homo sapiens (human)IC500.7933124124
Bromodomain-containing protein 4Homo sapiens (human)Ki0.019388
CREB-binding proteinHomo sapiens (human)IC509.715333
Cytochrome P450 1A2Homo sapiens (human)IC500.820011
Cytochrome P450 3A4Homo sapiens (human)IC500.052822
Histone acetyltransferase p300Homo sapiens (human)IC5019.400011
Histone deacetylase 1Homo sapiens (human)IC500.291011
Histone deacetylase 11 Homo sapiens (human)IC500.291011
Histone deacetylase 2Homo sapiens (human)IC500.291011
Histone deacetylase 3Homo sapiens (human)IC500.291011
Histone deacetylase 4Homo sapiens (human)IC500.291011
Histone deacetylase 5Homo sapiens (human)IC500.291011
Histone deacetylase 6Homo sapiens (human)IC500.291011
Histone deacetylase 7Homo sapiens (human)IC500.291011
Histone deacetylase 8Homo sapiens (human)IC500.291011
Histone deacetylase 9Homo sapiens (human)IC500.291011
Polyamine deacetylase HDAC10Homo sapiens (human)IC500.291011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Bromodomain testis-specific proteinHomo sapiens (human)Kd0.178677
Bromodomain-containing protein 2Homo sapiens (human)Kd0.08271212
Bromodomain-containing protein 3Homo sapiens (human)Kd0.05991010
Bromodomain-containing protein 4Homo sapiens (human)EC500.120333
Bromodomain-containing protein 4Homo sapiens (human)Kd0.09123157
Chain A, Bromodomain testis-specific proteinHomo sapiens (human)Kd0.190111
Chain A, Bromodomain-containing protein 4Homo sapiens (human)Kd0.049011
CREB-binding proteinHomo sapiens (human)Kd9.600011

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Bromodomain-containing protein 4Homo sapiens (human)DC505.000011
DNA damage-binding protein 1Homo sapiens (human)DC505.000011
Protein cereblonHomo sapiens (human)DC505.000011