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BIO-2007817 | BIO-2007817 : Molecular glue activator for PRKN and phospho-ubiquitin
RATINGS:
Cellular Use: (2 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
PRKN
  • Kd:10 nM
  • EC50:150 nM
  • % ac:50%
Molecular Glues
up to 10 uM

Selectivity

Potency
Cellular
In Vitro

PRKN

Mode of Action: Molecular Glues

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1038/s41467-024-51889-3

Negative Control Compounds

canSAR7437550
Notes: The inactive diastereomer BIO-200781848 bound the Complex with 150-fold less affinity in ITC assay.

Chemical Information

Molecular Formula C32H36N6O3
SMILEs CO[C@H](C(=O)N1Cc2c(-c3ccc(C(=O)N4CCCc5ccccc54)cc3)cnn2C[C@H]1C(C)C)c1cnn(C)c1
InChI InChI=1S/C32H36N6O3/c1-21(2)28-20-38-29(19-37(28)32(40)30(41-4)25-16-33-35(3)18-25)26(17-34-38)22-11-13-24(14-12-22)31(39)36-15-7-9-23-8-5-6-10-27(23)36/h5-6,8,10-14,16-18,21,28,30H,7,9,15,19-20H2,1-4H3/t28-,30-/m0/s1
Molecular weight 552.28 Da
AlogP 4.631100000000004
HBond acceptors 9
HBond donors --
Atoms 77

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Expert Reviews

by SERP
(on 31 Oct 2024 )
Cellular Use Rating
( The reviewer did not leave any comments )
by SERP
(on 5 Nov 2024 )
Cellular Use Rating
BIO-2007817 is one of the best compounds for assessing parkin activity in cells, as it has a unique activation mechanism by gluing parkin and pUb. However, its activity might not be sufficient. Even at...
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