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)
| Member | Definition | Class |
|---|---|---|
| jq1 compound | A 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 |
| pelabresib | An 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)
| Timeframe | Studies, Drugs with This Role(%) | 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 | 70 (59.32) | 24.3611 |
| 2020's | 48 (40.68) | 2.80 |
Study Types
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 1 (0.80%) | 5.53% |
| Reviews | 10 (8.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 114 (91.20%) | 84.16% |
Protein Targets (34)
Potency Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 10.6840 | 1 | 1 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 11.9877 | 1 | 1 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 5.2276 | 4 | 4 |
| Fumarate hydratase | Homo sapiens (human) | Potency | 37.2212 | 1 | 1 |
| G | Vesicular stomatitis virus | Potency | 10.6840 | 1 | 1 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 10.6840 | 1 | 1 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 10.6840 | 1 | 2 |
| Interferon beta | Homo sapiens (human) | Potency | 4.1999 | 2 | 7 |
| polyprotein | Zika virus | Potency | 37.2212 | 1 | 1 |
| PPM1D protein | Homo sapiens (human) | Potency | 3.1192 | 1 | 4 |
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Bromodomain testis-specific protein | Homo sapiens (human) | IC50 | 0.1902 | 13 | 13 |
| Bromodomain-containing protein 1 | Homo sapiens (human) | IC50 | 44.5000 | 1 | 1 |
| Bromodomain-containing protein 2 | Homo sapiens (human) | IC50 | 0.0959 | 22 | 22 |
| Bromodomain-containing protein 2 | Homo sapiens (human) | Ki | 0.0128 | 4 | 4 |
| Bromodomain-containing protein 3 | Homo sapiens (human) | IC50 | 0.0573 | 18 | 18 |
| Bromodomain-containing protein 3 | Homo sapiens (human) | Ki | 0.0078 | 4 | 4 |
| Bromodomain-containing protein 4 | Homo sapiens (human) | IC50 | 0.7933 | 124 | 124 |
| Bromodomain-containing protein 4 | Homo sapiens (human) | Ki | 0.0193 | 8 | 8 |
| CREB-binding protein | Homo sapiens (human) | IC50 | 9.7153 | 3 | 3 |
| Cytochrome P450 1A2 | Homo sapiens (human) | IC50 | 0.8200 | 1 | 1 |
| Cytochrome P450 3A4 | Homo sapiens (human) | IC50 | 0.0528 | 2 | 2 |
| Histone acetyltransferase p300 | Homo sapiens (human) | IC50 | 19.4000 | 1 | 1 |
| Histone deacetylase 1 | Homo sapiens (human) | IC50 | 0.2910 | 1 | 1 |
| Histone deacetylase 11 | Homo sapiens (human) | IC50 | 0.2910 | 1 | 1 |
| Histone deacetylase 2 | Homo sapiens (human) | IC50 | 0.2910 | 1 | 1 |
| Histone deacetylase 3 | Homo sapiens (human) | IC50 | 0.2910 | 1 | 1 |
| Histone deacetylase 4 | Homo sapiens (human) | IC50 | 0.2910 | 1 | 1 |
| Histone deacetylase 5 | Homo sapiens (human) | IC50 | 0.2910 | 1 | 1 |
| Histone deacetylase 6 | Homo sapiens (human) | IC50 | 0.2910 | 1 | 1 |
| Histone deacetylase 7 | Homo sapiens (human) | IC50 | 0.2910 | 1 | 1 |
| Histone deacetylase 8 | Homo sapiens (human) | IC50 | 0.2910 | 1 | 1 |
| Histone deacetylase 9 | Homo sapiens (human) | IC50 | 0.2910 | 1 | 1 |
| Polyamine deacetylase HDAC10 | Homo sapiens (human) | IC50 | 0.2910 | 1 | 1 |
Activation Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Bromodomain testis-specific protein | Homo sapiens (human) | Kd | 0.1786 | 7 | 7 |
| Bromodomain-containing protein 2 | Homo sapiens (human) | Kd | 0.0827 | 12 | 12 |
| Bromodomain-containing protein 3 | Homo sapiens (human) | Kd | 0.0599 | 10 | 10 |
| Bromodomain-containing protein 4 | Homo sapiens (human) | EC50 | 0.1203 | 3 | 3 |
| Bromodomain-containing protein 4 | Homo sapiens (human) | Kd | 0.0912 | 31 | 57 |
| Chain A, Bromodomain testis-specific protein | Homo sapiens (human) | Kd | 0.1901 | 1 | 1 |
| Chain A, Bromodomain-containing protein 4 | Homo sapiens (human) | Kd | 0.0490 | 1 | 1 |
| CREB-binding protein | Homo sapiens (human) | Kd | 9.6000 | 1 | 1 |
Other Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Bromodomain-containing protein 4 | Homo sapiens (human) | DC50 | 5.0000 | 1 | 1 |
| DNA damage-binding protein 1 | Homo sapiens (human) | DC50 | 5.0000 | 1 | 1 |
| Protein cereblon | Homo sapiens (human) | DC50 | 5.0000 | 1 | 1 |