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Epigenetic Reader Domain

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Items 1-50 of 338

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Citations
  1. A16859
    ARV-825

    BRD4 Inhibitor

    ARV-825 is a hetero-bifunctional molecule that is composed of a BRD4 binding moiety joined to an E3 ligase cereblon binding moiety using proteolysis targeting chimera (PROTAC) technology.
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  2. A13068
    CPI-203

    BET bromodomain Inhibitor

    CPI203 is a novel potent, selective and cell permeable inhibitor of the bromodomain and extra terminal (BET) family protein BRD4 with an IC50 of ~37 nM (BRD4 α-screen assay).
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  3. A12729
    (+)-JQ1

    BET Inhibitor

    (+)-JQ1 is a potent, high affinity, selective BET bromodomain inhibitor.
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  4. A13227
    SGC-CBP30

    CBP/p300 bromodomain inhibitor

    SGC-CBP30 is a potent and selective inhibitor of CREBBP (CBP) and EP300; which are general transcriptional co-activators.
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  5. A12545
    PFI-1

    BET inhibitor

    PFI-1 is a BET bromodomain inhibitor that exhibits inhibitory activity at BRD2 and BRD4.
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  6. A11783
    GSK 1210151A (I-BET151)

    BET Bromodomain Inhibitor

    GSK1210151A is a novel selective inhibitor of the bromodomain and extra terminal (BET) family proteins BRD2, BRD3, and BRD4.
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  7. A20579
    JQ1 (carboxylic acid)

    BRD4 inhibitor

    JQ-1 carboxylic acid is a highly potent, selective and cell-permeable BRD4 inhibitor with IC50s of 77 nM and 33 nM for BRD4(1) and BRD4(2), respectively.
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  8. A12815
    C646

    p300/CBP inhibitor

    C646 is a selective p300/CREB-binding protein (CBP) inhibitor (Ki = 400 nM).
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  9. A14133
    GSK1324726A (I-BET726)

    BET inhibitor

    GSK1324726A (I-BET726) is a novel, potent, and selective small molecule inhibitor of BET proteins with high affinity to BRD2 (IC50= 41 nM), BRD3 (IC50= 31 nM), and BRD4 (IC50= 22 nM).
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  10. A11440
    Molibresib (GSK 525762A, I-BET-762)

    BET inhibitor

    GSK-525762A is a small molecule inhibitor of the BET (Bromodomain and Extra-Terminal) family
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  11. A12141
    I-BET282

    Bromodomain inhibitor

    I-BET282 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

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  12. A17175
    CF53

    BET inhibitor

    CF53 is a bromodomain and extra-terminal (BET) bromodomain Inhibitor with IC50 value of 11.7 nM.
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  13. A17180
    TP-472

    BRD9/7 inhibitor

    TP-472 is a potent BRD9/7 inhibitor with Kd of 33 and 340 nM, respectively.
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  14. A17226
    Mivebresib (ABBV-075)

    BET inhibitor

    Mivebresib, also known as ABBV-075, is a potent BET inhibitor (bromodomain (BRD)-containing proteind) with potential antineoplastic activity.
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  15. A18344
    666-15

    selective CREB inhibitor

    666-15 is a potent and selective CREB inhibitor with an IC50 of 81 nM.
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  16. A18345
    PLX51107

    selective BET inhibitor

    PLX51107 is a potent and selective BET inhibitor, with Kds of 1.6, 2.1, 1.7, and 5 nM for BD1 and 5.9, 6.2, 6.1, and 120 nM for BD2 of BRD2, BRD3, BRD4, and BRDT, respectively; PLX51107 also interacts with the bromodomains of CBP and EP300 (Kd, in the 100 nM range).
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  17. A18454
    BRD-IN-3

    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.
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  18. A15872
    I-BRD9

    Selective BRD9 inhibitor

    I-BRD9 is a potent and selective BRD9 inhibitor with pIC50 of 7.3, while it displayed a pIC50 of 5.3 against BRD4.
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  19. A15876
    PF-CBP1

    CREBBP inhibitor

    PF-CBP1 is a highly selective inhibitor of the bromodomain of CREB-binding protein(CREBBP).It inhibits CREBBP and p300 bromodomains with IC50 of 125 and 363 nM respectively.
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  20. A15947
    BAZ2-ICR

    BAZ2 bromodomain inhibitor

    BAZ2-ICR is an excellent chemical probe for functional studies of the BAZ2 bromodomains in vitro and in vivo.
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  21. A16000
    OF-1

    BRPF1B/BRPF2 bromodomain inhibitor

    OF-1 is a chemical probe for BRPF bromodomains. OF-1 has been shown to bind to BRPF1B with a KD of 100 nM (ITC), to BRPF2 with a KD of 500 nM (ITC) and to BRPF3 with a KD of 2.4 uM (ITC).
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  22. A16068
    BI-7273

    BRD9 BD Inhibitor

    BI-7273 is a selective, and cell-permeable BRD9 BD inhibitor.
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  23. A16076
    Pelabresib (CPI 0610)

    BET bromodomain inhibitor

    CPI 0610 is a small molecule inhibitor of the Bromodomain and Extra-Terminal (BET) family of proteins, with potential antineoplastic activity.
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  24. A16092
    GSK 5959

    BRPF1 bromodomain inhibitor

    GSK 5959 is a potent, selective and cell permeable BRPF1 bromodomain inhibitor with IC50 ~ 80 nM. Exhibits >100-fold selectivity for BRPF1 over a panel of 35 other bromodomains, including BRPF2/3 and BET family bromodomains.
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  25. A16180
    EML 425

    CBP/p300 inhibitor

    EML 425 is a reversible and non-competitive CBP/p300 inhibitor that is cell permeable (IC50 values are 1.1 and 2.9 uM, respectively).
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  26. A16196
    BI-9564

    BRD7/9 inhibitor

    BI-9564 is a potent and selective inhibitor of BRD9 and BRD7 bromodomains (Kds = 14.1 and 239 nM; IC50s = 75 nM and 3.4 uM, respectively).
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  27. A16330
    GSK6853

    BRPF1 bromodomain inhibitor

    GSK6853 is a potent and selective inhibitor of the BRPF1 bromodomain. shows excellent BRPF1 potency (pKd 9.5) and greater than 1600-fold selectivity over all other bromodomains tested.
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  28. A16355
    CeMMEC13

    TAF1 inhibitor

    CeMMEC13 is an isoquinolinone that selectively inhibits the second bromodomain of TAF1 (IC50 = 2.1 μM).
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  29. A16366
    OXF BD 02

    BRD4 inhibitor

    OXF BD 02, selective inhibitor of the first bromodomain of BRD4 (BRD4(1)) (IC50 = 382 nM). Exhibits 2-3-fold selectivity for BRD4(1) over the CBP bromodomain and has little affinity for a range of other bromodomains.
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  30. A16367
    GW841819X

    BET Inhibitor

    GW841819X is an analogue of (+)-JQ1 and a novel inhibitor of BET bromodomains. GW841819X was a single enantiomer but of undefined chirality at the 4-position of the benzodiazepine ring 3.
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  31. A16368
    BET-BAY 002

    BET inhibitor

    BET-BAY 002 is a potent BET inhibitor; shows efficacy in a multiple myeloma model.
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  32. A16470
    CPI-637

    CBP/EP300 bromodomain inhibitor

    CPI-637 is a selective and cell-active benzodiazepinone CBP/EP300 bromodomain inhibitor.
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  33. A16829
    ZL0420

    BRD4 inhibitor

    ZL0420 is a potent and selective BRD4 inhibitor with IC50 values of 27 nM against BRD4 BD1 and 32 nM against BRD4 BD2 respectively and good selectivity over that of the related BRD2 homolog.
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  34. A16830
    A-485

    p300/CBP inhibitor

    A-485 is a potent and selective HAT inhibitor of p300/CBP in vitro with an IC50 of 10 nM in a p300 TR-FRET assay and 3 nM in a CBP TR-FRET assay with selectivity > 1000-fold over closely related HATs.
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  35. A16831
    ABBV-744

    BET bromodomain inhibitor

    ABBV-744 is a BDII-selective BET bromodomain inhibitor that is being investigated to treat AML and metastic castration-resistant prostate cancer.
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  36. A16872
    HJB-97

    BET bromodomian inhibitor

    HJB-97 is a potent BET bromodomian inhibitor. It acts by targeting BRD2/3/4 BD1 and BD2.
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  37. A16881
    BAY1238097

    BET inhibitor

    BAY1238097 is a potent and selective BET inhibitor. BAY1238097 binds to the acetylated lysine recognition motifs on the BRD of BET proteins, thereby preventing the interaction between BET proteins and histones.
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  38. A19506
    FL-411

    BRD4 inhibitor

    FL-411 is a potent and selective BRD4 inhibitor with an IC50 of 0.43±0.09 μM for BRD4.
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  39. A19516
    BET-IN-4

    BRD4 inhibitor

    BET-IN-4 is a potent BET bromodomain protein (BRD4) inhibitor, with an IC50 of ?? 1 μM.
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  40. A19656
    Y06137

    BET inhibitor

    Y06137 is a potent and selective BET inhibitor for treatment of castration-resistant prostate cancer (CRPC). Y06137 binds to the BRD4(1) bromodomain with a Kd of 81 nM.
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  41. A19665
    Y06036

    BET inhibitor

    Y06036 is a potent and selective BET inhibitor, which binds to the BRD4(1) bromodomain with Kd value of 82 nM. Antitumor activity.
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  42. A19737
    INCB-057643

    BET inhibitor

    INCB-057643 is a novel, orally bioavailable BET inhibitor.
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  43. A19798
    GNE-781

    CBP inhibitor

    GNE-781 is a highly potent and selective CBP inhibitor with an IC50 of 0.94 nM in TR-FRET assay. GNE-781 also inhibits BRET and BRD4(1) with IC50s of 6.2 nM and 5100 nM, respectively.
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  44. A19831
    BET bromodomain inhibitor

    BET inhibitor

    BET bromodomain inhibitor is a potent BET inhibitor extracted from patent WO/2015/153871A2, compound example 11.
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  45. A19900
    CeMMEC1

    BRD4 inhibitor

    CeMMEC1 is an inhibitor of BRD4, and also has high affinity for TAF1, with an IC50 of 0.9 μM for TAF1, and a Kd of 1.8 μM for TAF1 .
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  46. A20036
    Inobrodib (CCS-1477)

    p300/CBP bromodomain inhibitor

    Inobrodib (CCS-1477) is a potent p300/CBP bromodomain inhibitor.

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  47. A20123
    ZL0454

    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.
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  48. A20136
    (E)-ZL0420

    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.
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  49. A20149
    I-BET762 carboxylic acid

    BRD4 inhibitor

    I-BET762 carboxylic acid (Molibresib carboxylic acid) is an I-BET762-based warhead ligand for conjugation reactions of PROTAC targeting on BET. I-BET762 carboxylic acid (Molibresib carboxylic acid) is a BRD4 inhibitor with a pIC50 of 5.1.
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  50. A20162
    BET-IN-2

    BET inhibitor

    BET-IN-2 is a BET inhibitor with an IC50 of 52 nM for BRD4-BD1.
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