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Epigenetic Reader Domain

Inhibitory Selectivity

Catalog No.Inhibitor Name Epigenetic Reader Domain
A12729(*)-JQ1
***
A11783I-BET151
*
A12545PFI-1
**
A11440I-BET-762
***
A13956RVX-208
*
A13227SGC-CBP30
****
A13163Bromosporine
****
A13890OTX015
****
A12948UNC1215
**
A13717UNC669
*
A14133GSK1324726A
***
A13749MS436
**
A13068CPI-203
***
A13957PFI-3

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

产品 1 到 50 共 81个

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  1. I-BRD9
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    I-BRD9

    Catalog No. A15872
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    Selective BRD9 抑制剂
    I-BRD9是一种有效的选择性BRD9抑制剂，pIC50为7.3，而对BRD4的pIC50为5.3。 了解更多
  2. BI-7273
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    BI-7273

    Catalog No. A16068
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    BRD9 BD 抑制剂
    BI-7273是一种选择性的，细胞可渗透的BRD9 BD抑制剂。 了解更多
  3. BI-9564
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    BI-9564

    Catalog No. A16196
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    BRD7/9 抑制剂
    BI-9564是BRD9和BRD7溴结构域的有效和选择性抑制剂（Kds分别为14.1和239 nM；IC50分别为75 nM和3.4 uM）。 了解更多
  4. VZ185
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    VZ185

    Catalog No. A18685
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    dual BRD7/9 PROTAC degrader
    VZ185 is a potent, fast, and selective dual BRD7/9 PROTAC degrader with DC50s of 4.5 and 1.8 nM, respectively. 了解更多
  5. ZXH-3-26
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    ZXH-3-26

    Catalog No. A18399
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    PROTAC BRD4 degrader
    ZXH-3-26 is a selective PROTAC BRD4 degrader with a DC50/5h (DC50/5h referring to half-maximal degradation after 5 hours of treatment) of ~ 5 nM. 了解更多
  6. (E)-ZL0420
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    (E)-ZL0420

    Catalog No. A20136
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    BRD4 inhibitor
    ZL0420 is a potent and selective bromodomain-containing protein 4 (BRD4) inhibitor with IC50 values of 27 nM against BRD4 BD1 and 32 nM against BRD4 BD2. 了解更多
  7. ZL0454
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    ZL0454

    Catalog No. A20123
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    BRD4 inhibitor
    ZL0454 is a potent and selective Bromodomain-containing protein 4 (BRD4) inhibitor with an IC50 of 49 and 32 nM for BD1 and BD2. 了解更多
  8. BMS-986158
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    BMS-986158

    Catalog No. A19442
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    Bromodomain inhibitor
    BMS-986158 is an inhibitor of the bromodomain and extra-terminal (BET) proteins. 了解更多
  9. MS417
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    MS417

    Catalog No. A19433
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    BRD4 inhibitor
    MS417 is a BET-specific BRD4 inhibitor, binds to BRD4-BD1 and BRD4-BD2 with IC50s of 30, 46 nM and Kds of 36.1, 25.4 nM, respectively, with weak selectivity at CBP BRD (IC50, 32.7 μM). 了解更多
  10. MZP-54
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    MZP-54

    Catalog No. A19426
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    BRD3/4 degrader
    MZP-54 is a selective degrader of BRD3/4 based on PROTAC technology, with a Kd of 4 nM for Brd4BD2. 了解更多
  11. MZP-55
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    MZP-55

    Catalog No. A19415
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    BRD3/4 degrader
    MZP-55 is a selective degrader of BRD3/4 based on PROTAC technology, with a Kd of 8 nM for Brd4BD2. 了解更多
  12. dBET57
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    dBET57

    Catalog No. A19133
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    BRD4BD1degrader
    dBET57 is a potent and selective degrader of BRD4BD1 based on the PROTAC technology. 了解更多
  13. CD235
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    CD235

    Catalog No. A19115
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    BET bromodomain inhibitor
    CD235 is a structurally similar analogue of CD161. CD161 is a potent and orally bioavailable BET bromodomain inhibitor. 了解更多
  14. BETd-246
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    BETd-246

    Catalog No. A18913
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    BRD inhibitor
    BETd-246 is a second-generation BET bromodomain (BRD) inhibitor, exhibiting superior selectivity, potency and antitumor activity. 了解更多
  15. Bromodomain IN-1
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    Bromodomain IN-1

    Catalog No. A18845
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    Bromodomain inhibitor
    Bromodomain IN-1 is a Bromodomain inhibitor extracted from patent WO2016069578A1, compound 4 . 了解更多
  16. BRD4 Inhibitor-10
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    BRD4 Inhibitor-10

    Catalog No. A18679
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    BRD4-BD1 inhibitor
    BRD4 Inhibitor-10 is a potent BRD4-BD1 inhibitor extracted from patent WO2015022332A1, Compound II-25, has an IC50 of 8 nM. 了解更多
  17. GSK9311
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    GSK9311

    Catalog No. A12453
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    inhibitor of the BRPF bromodomain
    GSK9311 is a potent inhibitor of the BRPF bromodomain with pIC50 values of 6.0 and 4.3 for BRPF1 and BRPF2, respectively. 了解更多
  18. BET-IN-1
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    BET-IN-1

    Catalog No. A12141
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    bromodomain inhibitor
    BET-IN-1 is a bromodomain inhibitor extracted from patent WO/2013024104A1, compound example 2, has a plC50 in the range 6.0 - 7.0. IC50 value: 6.0 - 7.0 (plC50) Target: bromodomain 了解更多
  19. GS-626510
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    GS-626510

    Catalog No. A13305
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    BET family bromodomains inhibitor
    GS-626510 is a potent, and orally bioavailable BET family bromodomains inhibitor, with Kd values of 0.59-3.2 nM for BRD2/3/4, with IC50 values of 83 nM and 78 nM foe BD1 and BD2, respectively. 了解更多
  20. (Rac)-BAY1238097
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    (Rac)-BAY1238097

    Catalog No. A21598
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    BET inhibitor
    (Rac)-BAY1238097 is a BET inhibitor, with an IC50 of 1.02 μM for BRD4. Used in cancer research. 了解更多
  21. INCB054329 Racemate
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    INCB054329 Racemate

    Catalog No. A21609
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    BET protein inhibitor
    INCB054329 Racemate is a BET protein inhibitor. 了解更多
  22. CPI-0610 carboxylic acid
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    CPI-0610 carboxylic acid

    Catalog No. A21714
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    BET inhibitor
    CPI-0610 carboxylic acid is a potent bromodomain and extra-terminal (BET) protein inhibitor. CPI-0610 carboxylic acid has the potential in the therapy of multiple myeloma. 了解更多
  23. AZD5153 6-Hydroxy-2-naphthoic acid
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    AZD5153 6-Hydroxy-2-naphthoic acid

    Catalog No. A21852
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    BET/BRD4 bromodomain inhibitor
    AZD5153 6-Hydroxy-2-naphthoic acid is the 6-Hydroxy-2-naphthoic acid of AZD5153. AZD5153 is a potent, selective, and orally available BET/BRD4 bromodomain inhibitor; disrupts BRD4 with an IC50 of 1.7 nM. 了解更多
  24. Molibresib besylate
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    Molibresib besylate

    Catalog No. A21855
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    BET bromodomain inhibitor
    Molibresib besylate (GSK 525762C; I-BET 762 besylate) is a BET bromodomain inhibitor with IC50 of 32.5-42.5 nM. 了解更多
  25. MS436
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    MS436

    Catalog No. A13749
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    BRD4 抑制剂
    MS436是用于BRD4溴结构域的重氮基小分子抑制剂，Ki值为30-50 nM。 了解更多
  26. I-CBP112
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    I-CBP112

    Catalog No. A13165
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    CBP/p300 bromodomain 抑制剂
    I-CBP112是一种高效且选择性的p300/CBP溴结构域抑制剂（对于CBP，IC50为?0.14-0.17 uM，对于p300为?0.625 uM）。 了解更多
  27. UNC1215
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    UNC1215

    Catalog No. A12948
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    L3MBTL3 抑制剂
    UNC1215是具有细胞活性的L3MBTL3的强效选择性拮抗剂。 了解更多
  28. OTX015
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    OTX015

    Catalog No. A13890
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    BET 抑制剂
    OTX015是口服可生物利用的BRD2，BRD3和BRD4的小分子抑制剂（EC50s = 10-19 nM）。 了解更多
  29. SGC-CBP30
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    SGC-CBP30

    Catalog No. A13227
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    CBP/p300 bromodomain 抑制剂
    SGC-CBP30是一种有效且选择性的CREBBP（CBP）和EP300抑制剂，无细胞试验中IC50分别为21 nM和38 nM。它们是一般的转录共激活因子。 了解更多
  30. (+)-JQ1
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    (+)-JQ1

    Catalog No. A12729
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    BET 抑制剂
    (+)-JQ1是有效的，高亲和力的选择性BET溴结构域抑制剂。 了解更多
  31. UNC 669
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    UNC 669

    Catalog No. A13717
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    L3MBTL 抑制剂
    UNC669是L3MBTL1和L3MBTL3的抑制剂,对L3MBTL1和L3MBTL3具有选择性（IC50分别为4.2μM和3.1μM）。 了解更多
  32. Bromosporine
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    Bromosporine

    Catalog No. A13163
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    bromodomain 抑制剂
    Bromosporine是一种针对溴结构域的广谱抑制剂，对于BRD2，BRD4，BRD9和CECR2的IC50分别为0.41μM，0.29μM，0.122μM和0.017μM。 了解更多
  33. CPI-203
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    CPI-203

    Catalog No. A13068
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    BET bromodomain 抑制剂
    CPI203是溴结构域和额外末端（BET）家族蛋白BRD4的新型有效，选择性和细胞渗透性抑制剂，IC50为?37 nM（BRD4α筛选试验）。 了解更多
  34. GSK 525762A (I-BET-762)
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    GSK 525762A (I-BET-762)

    Catalog No. A11440
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    BET 抑制剂
    GSK 525762A (I-BET-762)是BET(溴域和末端外)家族的小分子抑制剂。 了解更多
  35. PFI-1
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    PFI-1

    Catalog No. A12545
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    BET 抑制剂
    PFI-1是BET溴结构域抑制剂，对BRD2和BRD4表现出抑制活性。 了解更多
  36. GSK 1210151A (I-BET151)
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    GSK 1210151A (I-BET151)

    Catalog No. A11783
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    BET Bromodomain 抑制剂
    GSK 1210151A (I-BET151)是溴结构域和额外末端（BET）家族蛋白BRD2，BRD3和BRD4的新型选择性抑制剂。 了解更多
  37. A1874
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    A1874

    Catalog No. A18735
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    BRD4-degrading PROTAC
    A1874 is a nutlin-based and BRD4-degrading PROTAC with a DC50 of 32 nM (induce BRD4 degradation in cells). Effective in inhibiting many cancer cell lines proliferation. 了解更多
  38. Apabetalone (RVX-208)
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    Apabetalone (RVX-208)

    Catalog No. A13956
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    BET bromodomain 抑制剂
    RVX-208是一种有效的BET溴结构域抑制剂，对BD2的IC50为0.510 uM，是BD1选择性的170倍。 了解更多
  39. P300/CBP-IN-3
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    P300/CBP-IN-3

    Catalog No. A18544
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    p300/CBP histone acetyltransferase inhibitor
    P300/CBP-IN-3, a p300/CBP histone acetyltransferase inhibitor. 了解更多
  40. BRD-IN-3
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    BRD-IN-3

    Catalog No. A18454
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    BRD inhibitor
    BRD-IN-3 ((R,R)-36n) is a highly potent PCAF bromodomain (BRD) inhibitor, with an IC50 of 7 nM. BRD-IN-3 also exhibits activity against GCN5 and FALZ. 了解更多
  41. PFI-3
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    PFI-3

    Catalog No. A13957
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    SMARCA bromodomains probe
    PFI-3是SMARCA溴结构域的选择性化学探针。 了解更多
  42. GNE-049
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    GNE-049

    Catalog No. A20206
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    CBP inhibitor
    GNE-049 is a highly potent and selective CBP inhibitor with an IC50 of 1.1 nM in TR-FRET assay. GNE-049 also inhibits BRET and BRD4(1) with IC50s of 12 nM and 4200 nM, respectively. 了解更多
  43. Anacardic Acid
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    Anacardic Acid

    Catalog No. A14226
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    KAT5 (Tip60), p300/PCAF 抑制剂
    Anacardic Acid是p300和p300/CBP相关因子组蛋白乙酰转移酶的有效抑制剂。 了解更多
  44. GSK 525768A
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    GSK 525768A

    Catalog No. A14134
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    GSK 525768A是GSK 525762A的对映体化合物，GSK 525762A是一种有效的小分子抑制剂，可破坏溴多糖BET家族（Brd2、Brd3和Brd4）的功能；GSK 525768A对BET没有活性。 了解更多
  45. GSK1324726A (I-BET726)
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    GSK1324726A (I-BET726)

    Catalog No. A14133
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    BET 抑制剂
    GSK1324726A (I-BET726)是一种新型、高效、选择性的BET蛋白小分子抑制剂，对BRD2（IC50 = 41 nM）、BRD3（IC50 = 31 nM）和BRD4（IC50 = 22 nM）具有高度的亲和力。 了解更多
  46. (-)-JQ1
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    (-)-JQ1

    Catalog No. A14160
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    BET bromodomain 抑制剂
    (-)-JQ1蛋白家族蛋白质的溴结构域和额外末端结构域（BET）家族，包括BRD2，BRD3和BRD4，在许多细胞过程中起着关键作用，包括炎症基因表达，有丝分裂和病毒/宿主相互作用，这是通过控制组蛋白乙酰化的过程来实现的。依赖的染色质复合物。 了解更多
  47. GSK2801
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    GSK2801

    Catalog No. A14015
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    BAZ2A and BAZ2B 抑制剂
    GSK2801是BAZ2家族含溴结构域蛋白的强效抑制剂。 了解更多
  48. ZEN-3219
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    ZEN-3219

    Catalog No. A19367
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    BET inhibitor
    ZEN-3219 is a BET inhibitor with IC50s of 0.48, 0.16 and 0.47 μM for BRD4(BD1), BRD4(BD2) and BRD4(BD1BD2), respectively. ZEN-3219 can be used to form PROTACs to induce degradation of BRD4. 了解更多
  49. SF1126
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    SF1126

    Catalog No. A12704
    Pan PI3K 抑制剂
    SF1126是一种水溶性小分子前药，包含泛PI3K/mTOR抑制剂LY294002/SF1101与含RGD的四肽SF1174共轭，具有潜在的抗肿瘤和抗血管生成活性。 了解更多
  50. C646
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    C646

    Catalog No. A12815
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    p300/CBP 抑制剂
    C646是选择性的p300/CREB结合蛋白（CBP）抑制剂（Ki = 400 nM）。 了解更多

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作用机制
  1. Inhibitor (抑制剂) (70)
  2. Modulator (调节剂) (1)
  3. Degrader (降解剂) (7)
靶点
  1. BAZ2A (2)
  2. BAZ2B (2)
  3. BET (5)
  4. BRD2 (7)
  5. BRD3 (4)
  6. BRD4 (9)
  7. BRD7 (1)
  8. BRD9 (4)
  9. BRPF1 (4)
  10. BRPF2 (1)
  11. CECR2 (1)
  12. KAT5 (Tip60) (1)
  13. L3MBTL (2)
  14. L3MBTL1 (1)
  15. p300/CBP (7)
  16. PCAF (1)
  17. SMARCA4 (1)
  18. TAF1 (1)
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