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BMX-IN-1 | BMX-IN-1 : covalent inhibitor of BMX
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
BMX
  • IC50:8 nM
  • IC50:25 nM
covalent inhibitor
Up to 25 nM

Selectivity

In Vitro Selectivity Assessment

Potency: IC50 - BTK 10.4 nM

Potency Assay Off-Target:
Assessed activity against 442 kinases using the KinomeScan approach
In Cell Selectivity Assessment

Potency: GI50 - TEL-JAK1 4.92 uM, TEL-JAK2 5.83 uM, TEL-JAK3 7.98 uM, TEL-TYK2 E957D 6.09 uM, TEL-BLK 3.64 uM

Potency Assay Off-Target:
Inhibits the proliferation of a panel of murine Ba/F3 cells that were transformed with TEL fusion of ...

Potency
Cellular
In Vitro

BMX

Mode of Action: covalent inhibitor

Structure-Activity-Relationship data available? No

Chemical Information

Molecular Formula C29H24N4O4S
SMILEs C=CC(=O)Nc1cc(-n2c(=O)ccc3cnc4ccc(-c5ccc(NS(C)(=O)=O)cc5)cc4c32)ccc1C
InChI InChI=1S/C29H24N4O4S/c1-4-27(34)31-26-16-23(12-5-18(26)2)33-28(35)14-9-21-17-30-25-13-8-20(15-24(25)29(21)33)19-6-10-22(11-7-19)32-38(3,36)37/h4-17,32H,1H2,2-3H3,(H,31,34)
Molecular weight 524.15 Da
AlogP 5.01032
HBond acceptors 8
HBond donors 2
Atoms 62

References

Publications

    Cross References

    canSARChEMBLBindingDB

    Vendors

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    Expert Reviews

    by SERP
    (on 27 Jun 2016 )
    Cellular Use Rating
    Based on the data in Supplementary Table 1, this probe also binds to 63 other kinases (score less than or equal to 75%) at 1 micromolar concentration. So choosing a concentration well below 1 micromolar...
    by SERP
    (on 6 Jul 2016 )
    Cellular Use Rating
    ( The reviewer did not leave any comments )
    by SERP
    (on 12 Sept 2016 )
    Cellular Use Rating
    BMX-IN-1 is an irreversible inhibitor of the kinase BMX and is the best available probe for it. It is also a potent inhibitor of BTK. In a broad kinome scan experiment (DiscoverX technology), BMX-IN-1...
    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