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MEZIGDOMIDE | MEZIGDOMIDE : Degrader of CRBN
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 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
CRBN
  • IC50:37.2 nM
  • IC50:2.3 nM
  • EC50:3 nM
Degrader, CELMoD
up to 100 nM

Selectivity

Potency
Cellular
In Vitro

CRBN

Mode of Action: Degrader, CELMoD

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.9b01928

In Vivo Validations

Rat
Dose: 2 mg/Kg
Route of delivery: Intravenous
Systemic clearance: 6.8 ± 1.0 mL/min/Kg

DOI Reference: 10.1021/acs.jmedchem.9b01928

Dose: 10 mg/Kg
Route of delivery: Oral
Cmax: 3.2 ± 0.5 uM
Tmax: 0.8 ± 0.3 h
Area Under the Curve:: 16.4 ± 6.8 uM*h
Bioavailability: 38% ± 17%

DOI Reference: 10.1021/acs.jmedchem.9b01928

Monkey (Cynomolgus)
Dose: 3 mg/Kg
Route of delivery: Oral
Cmax: 0.22 ± 0.08 uM
Area Under the Curve:: 1.1 ± 0.3 uM*h

DOI Reference: 10.1021/acs.jmedchem.9b01928

Negative Control Compounds

CANSAR3333581
Notes: R- Enantiomer IC50 4510 nM

Chemical Information

Molecular Formula C32H30FN5O4
SMILEs N#Cc1ccc(N2CCN(Cc3ccc(COc4cccc5c4CN([C@H]4CCC(=O)NC4=O)C5=O)cc3)CC2)c(F)c1
InChI InChI=1S/C32H30FN5O4/c33-26-16-23(17-34)8-9-27(26)37-14-12-36(13-15-37)18-21-4-6-22(7-5-21)20-42-29-3-1-2-24-25(29)19-38(32(24)41)28-10-11-30(39)35-31(28)40/h1-9,16,28H,10-15,18-20H2,(H,35,39,40)/t28-/m0/s1
Molecular weight 567.23 Da
AlogP 0.0
HBond acceptors 9
HBond donors 1
Atoms 72

References

Publications

Cross References

canSARChEMBLPDB

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Expert Reviews

by SERP
(on 24 Oct 2022 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )
by SERP
(on 15 Nov 2022 )
Cellular Use Rating
In Model Organisms
The (R) and (S) enantiomers racemize on the timescale of course in cell culture, therefore, for in vitro experiments, the N-methylated compound, or another related inactive analogue may be a better negative...
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