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VUBI1 | VUBI1 : Activator of SOS1
RATINGS:
Cellular Use: (2 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
SOS1
  • Ki:44 nM
  • EC50:94 nM
Activator
up to 10 uM

Selectivity

Potency
Cellular
In Vitro

SOS1

Mode of Action: Activator

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.8b01108

Negative Control Compounds

BI-9930
SMILES: CN1CCN(CC1)C1=C2N(CC3=CC(C)=C(F)C(C)=C3)C(=NC2=CC(Cl)=C1)N1CC2(CNC2)C1

Chemical Information

Molecular Formula C26H32ClFN6
SMILEs Cc1cc(Cn2c(N3CC4(CNC4)C3)nc3c(N4CCN(C)CC4)cc(Cl)cc32)cc(C)c1F
InChI InChI=1S/C26H32ClFN6/c1-17-8-19(9-18(2)23(17)28)12-34-22-11-20(27)10-21(32-6-4-31(3)5-7-32)24(22)30-25(34)33-15-26(16-33)13-29-14-26/h8-11,29H,4-7,12-16H2,1-3H3
Molecular weight 482.24 Da
AlogP 0.0
HBond acceptors 6
HBond donors 1
Atoms 66

Vendors

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Expert Reviews

by SERP
(on 23 Sept 2024 )
Cellular Use Rating
Activity is in the single digit µM range. However, cellular concentration ranges higher than 10 µM are not recommended due to the absence of selectivity data of any kind.
by SERP
(on 15 Oct 2024 )
Cellular Use Rating
VUBI1 is the most potent SOS1 activator with a confirmed biophysical interactions to SOS1 in a RAS:SOS1:RAS co-crystal structure. VUBI1 demonstrated the typical biphasic modulation of downstream pERK1/2...
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