| + |
JQ1 | down-regulates activity 
chemical inhibition
|
BRD2 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-261987 |
|
|
in vitro |
|
| pmid |
sentence |
| 20871596 |
Enantiomerically pure (+)-JQ1 bound with a Kd of about 50 nM and 90 nM to the first and second bromodomains of BRD4, respectively (Fig. 1c, Supplementary Table 3). Comparable binding to both domains of BRD3 was observed, whereas the first bromodomains of BRDT and BRD2 revealed about 3-fold weaker binding.|Here, we present a first, thoroughly characterized inhibitor of the BET-family of bromodomains. |
|
| Publications: |
1 |
Organism: |
In Vitro |
| + |
BRD2 | up-regulates activity 
relocalization
|
TP53BP1 |
0.272 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-262035 |
|
|
Homo sapiens |
U2-OS Cell |
| pmid |
sentence |
| 29018219 |
BRD2 is required to recruit 53BP1 to DSBs.|When BRD2 recruitment was blocked with shRNA or JQ1 (Fig. 3a and Supplementary Figure 3c) or a panel of BRD2 siRNAs (Supplementary Figure 3a), the recruitment of 53BP1 to DSBs was significantly delayed. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
HDAC11 | down-regulates activity
binding
|
BRD2 |
0.346 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-262058 |
|
|
Homo sapiens |
HEK-293 Cell |
| pmid |
sentence |
| 30089714 |
Ex vivo and cell-based assays revealed that HDAC11 catalytic activity suppresses the BAT transcriptional program, in both the basal state and in response to β-adrenergic receptor signaling, through a mechanism that is dependent on physical association with BRD2, a bromodomain and extraterminal (BET) acetyl-histone-binding protein. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
2-[(4S)-6-(4-chlorophenyl)-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-N-ethylacetamide | down-regulates activity
chemical inhibition
|
BRD2 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-262202 |
|
|
in vitro |
|
| pmid |
sentence |
| 24015967 |
This paper describes the discovery and structure-activity relationships (SAR) of potent benzodiazepine inhibitors that disrupt the function of the BET family of bromodomains (BRD2, BRD3, and BRD4). This work has yielded a potent, selective compound I-BET762 that is now under evaluation |
|
| Publications: |
1 |
Organism: |
In Vitro |
| + |
Tert-butyl 2-[(9S)-7-(4-chlorophenyl)-4,5,13-trimethyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaen-9-yl]acetate | down-regulates activity
chemical inhibition
|
BRD2 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-261124 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 30080437 |
Through the integrative analyses of ChIP-seq and CAGE data, we elucidate the involvement of BRD2 in gene regulation upon BET inhibition by JQ1 in H23 cells. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
BRD7 | up-regulates quantity by expression 
transcriptional regulation
|
BRD2 |
0.421 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-253763 |
|
|
Homo sapiens |
Nasopharyngeal Carcinoma Cell |
| pmid |
sentence |
| 12600283 |
BRD7 protein could respectively interact with proteins, BRD2 and BRD3, and BRD7 could up-regulate the expression levels of BRD2 and BRD3 genes in mRNA level to some extent. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
H4C1 | up-regulates activity
relocalization
|
BRD2 |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-262062 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 12776177 |
Thus, the TIP60 HAT complex is recruited to MYC-target genes and, probably with other other HATs, contributes to histone acetylation in response to mitogenic signals. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
CID 132010322 | down-regulates activity
chemical inhibition
|
BRD2 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-261103 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 31969702 |
ABBV-744 potently inhibited the BD2 domain of BET family proteins with more than 290× selectivity relative to the BD1 domains of BRD2, BRD3 and BRD4 |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
BRD2 | up-regulates activity
relocalization
|
ZMYND8 |
0.292 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-262036 |
|
|
Homo sapiens |
HEK-293 Cell |
| pmid |
sentence |
| 29018219 |
ZMYND8 and BRD2 therefore work together to protect H4Ac domains from HDAC activity.|Further, when BRD2 was depleted, ZMYND8 accumulation was lost (Fig. 2e), indicating that either BRD2, or the underlying H4Ac, is required for ZMYND8 loading. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
2-[(9S)-7-(4-Chlorophenyl)-4,5,13-trimethyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaen-9-yl]-N-[8-[[2-[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]oxyacetyl]amino]octyl]acetamide | down-regulates quantity
chemical inhibition
|
BRD2 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-261095 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 29764999 |
DBET6 induces efficient degradation of BET proteins and inhibits the proliferation of GBM cells |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
3.0
BRD2
- 
- 