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CM11 | Degrader (PROTAC) of VHL
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
VHL
  • Kd:10 nM
  • DC50:10-100 nM
Degrader (PROTAC)
10-500 nM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
Kinase off-target screening results. CM11 was screened at 1 μM concentration against a panel of 5 ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
To evaluate the specificity of homo-PROTAC-induced degradation, and identify potential off-targets, ...

Potency
Cellular
In Vitro

VHL

Mode of Action: Degrader (PROTAC)

Structure-Activity-Relationship data available? No

DOI Reference: 10.1038/s41467-017-00954-1

Negative Control Compounds

CMP98 (cis-cis) - inactive epimer on each side
CMP99 (cis-trans) - inactive epimer on one side, act as VHL inhibitor but not degrader

Orthogonal Probes def

VH298

Chemical Information

Molecular Formula C58H82N8O14S2
SMILEs Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCOCCOCCOCCOCCOCC(=O)N[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)NCc2ccc(-c3scnc3C)cc2)C(C)(C)C)C(C)(C)C)cc1
InChI InChI=1S/C58H82N8O14S2/c1-37-49(81-35-61-37)41-13-9-39(10-14-41)29-59-53(71)45-27-43(67)31-65(45)55(73)51(57(3,4)5)63-47(69)33-79-25-23-77-21-19-75-17-18-76-20-22-78-24-26-80-34-48(70)64-52(58(6,7)8)56(74)66-32-44(68)28-46(66)54(72)60-30-40-11-15-42(16-12-40)50-38(2)62-36-82-50/h9-16,35-36,43-46,51-52,67-68H,17-34H2,1-8H3,(H,59,71)(H,60,72)(H,63,69)(H,64,70)/t43-,44-,45+,46+,51-,52-/m1/s1
Molecular weight 1178.54 Da
AlogP 3.5680400000000096
HBond acceptors 22
HBond donors 6
Atoms 164

References

Publications

Cross References

canSARChEMBLBindingDB

Vendors

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Expert Reviews

by SERP
(on 15 Apr 2020 )
Cellular Use Rating
A negative control known as CMP-98 is available and should be used when testing the activity of CM-11.
by SERP
(on 15 Apr 2020 )
Cellular Use Rating
( The reviewer did not leave any comments )
by SERP
(on 1 May 2020 )
Cellular Use Rating
CM11 is a potent and selective degrader of VHL that will induce auto-degradation of VHL in compatible cell lines. To distinguish inhibition versus degradation effects complenetary use of a VHL inhibitor...
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