|T000050, KDM5 Tracer
Compound Image

T000050

KDM5 Tracer


  • Description

    Formula:

    C37H40BF2N11O3

    avg. MolWt:

    735.61 u

    PAINS elements:

    none detected

    SMILES:

    display
  • Properties

    Store at:

    -80 °C

    Absorption:

    450 nm

    Emission:

    590 nm

    clogP:

    4.09
  • References

    Contributing Lab:

    Promega Corp., Madison

  • Experimental

    Assay window 4.99
    \(Z'\) 0.73
    CP agreement yes
    Tracer titration

    \(K_\mathrm{D}^{\,\mathrm{app}}\):

    > 10 µM
    titration curve
    raw data
    Tracer displacement
    i

    Compound used for displacement:

    unlabelled parent ligand

    \(\mathrm{EC}_{50}\):

    713 nM
    displacement curve
    raw data

    Comment: NLuc-KDM5A

    Assay window 4.73
    \(Z'\) 0.76
    CP agreement yes
    Tracer titration

    \(K_\mathrm{D}^{\,\mathrm{app}}\):

    6510 nM
    titration curve
    raw data
    Tracer displacement
    i

    Compound used for displacement:

    unlabelled parent ligand

    \(\mathrm{EC}_{50}\):

    539 nM
    displacement curve
    raw data

    Comment: NLuc-KDM5B

    Assay window 5.89
    \(Z'\) 0.62
    CP agreement yes
    Tracer titration

    \(K_\mathrm{D}\):

    1917 nM
    titration curve
    raw data
    Tracer displacement
    i

    Compound used for displacement:

    GSK467

    \(\mathrm{IC}_{50}\):

    72 µM
    displacement curve
    raw data

    Comment: NLuc-KDM5B

    Assay window 4.47
    \(Z'\) 0.69
    CP agreement yes
    Tracer titration

    \(K_\mathrm{D}^{\,\mathrm{app}}\):

    > 10 µM
    titration curve
    raw data
    Tracer displacement
    i

    Compound used for displacement:

    unlabelled parent ligand

    \(\mathrm{EC}_{50}\):

    1 µM
    displacement curve
    raw data

    Comment: NLuc-KDM5C

    Assay window 9.03
    \(Z'\) 0.71
    CP agreement yes
    Tracer titration

    \(K_\mathrm{D}\):

    1391 nM
    titration curve
    raw data
    Tracer displacement
    i

    Compound used for displacement:

    GSK467

    \(\mathrm{IC}_{50}\):

    20 nM
    displacement curve
    raw data

    Comment: NLuc-KDM5C