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CPI-637 | CPI-637 : Antagonist of EP300, CREBBP
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
EP300
  • IC 50:51 nM
    CREBBP
    • Kd:30 nM
    • IC 50:30 nM
    • EC 50:300 nM
    • EC 50:600 nM
    Antagonist
    up to 10 uM

    Selectivity

    In Vitro Selectivity Assessment

    Potency: IC50 - BRD9: 0.73 uM, BRD4: 11 uM

    Potency Assay Off-Target:
    In TR-FRET assays, CPI-637 was at least 700-fold selective for the targets over other Bromodomain pr ...
    Selectivity Assessment Description:
    In TR-FRET assays, CPI-637 was at least 700-fold selective for the targets over other Bromodomain pr ...

    Potency
    Cellular
    In Vitro

    EP300

    Mode of Action: Antagonist

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.1021/acsmedchemlett.6b00075

    CREBBP

    Mode of Action: Antagonist

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.1021/acsmedchemlett.6b00075

    Negative Control Compounds

    enant-CPI-637: S)-4-methyl-6-(1-methyl-3-(1-methyl-1H-pyrazol-4-yl)-1H-indazol-5-yl)-1,3,4,5-tetrahydro-2H-benzo[b][1,4]diazepin-2-one

    Chemical Information

    Molecular Formula C22H22N6O
    SMILEs C[C@@H]1CC(=O)Nc2cccc(-c3ccc4c(c3)c(-c3cnn(C)c3)nn4C)c2N1
    InChI InChI=1S/C22H22N6O/c1-13-9-20(29)25-18-6-4-5-16(22(18)24-13)14-7-8-19-17(10-14)21(26-28(19)3)15-11-23-27(2)12-15/h4-8,10-13,24H,9H2,1-3H3,(H,25,29)/t13-/m1/s1
    Molecular weight 386.19 Da
    AlogP 3.783400000000002
    HBond acceptors 7
    HBond donors 2
    Atoms 51

    References

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    Expert Reviews

    by SERP
    (on 27 Apr 2017 )
    Cellular Use Rating
    CPI-637 is a potent dual inhibitor of CBP (30 nM) and EP300 (51 nM) as measured by TR-FRET platform assays. CPI-637 is active in cells and inhibits MYC expression in AMO-1 cells with an EC50=600 nM....
    by SERP
    (on 15 May 2017 )
    Cellular Use Rating
    This is a high quality probe that is appropriate for interrogating CBP/EP300 cell biology in certain circumstances. CPI-637 is structurally differentiated from other CBP/EP300 chemical probes, and thus...
    by SERP
    (on 17 Nov 2020 )
    Cellular Use Rating
    This is a high quality compound originating from a dedicated medicinal chemistry effort to arrive at a molecule with 30/51 nM IC50 against CBP/EP300 in TR-FRET assays that causes cellular phenotypes...
    Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria