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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
Vendors
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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 public 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