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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

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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

(R)-CC-92480
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 public 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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