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NURR1-Ant-29 | NURR1-Ant-29 : Agonist of NR4A2
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (1 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
NR4A2
  • IC50:300 nM
  • EC50:110 nM
  • EC50:220 nM
Agonist
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Selective 15x over DHODH inhibitory potency (IC50 = 1.7 ± 0.4 μM), and >10-fold selectivity over Nur ...

Potency
Cellular
In Vitro

NR4A2

Mode of Action: Agonist

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.3c00415

In Vivo Validations

Rat
Dose: 5 mg/Kg
Route of delivery: Oral
Plasma half life: 4.4 h
Cmax: 56 uM
Area Under the Curve:: 290 uM*h
Bioavailability: 89%

DOI Reference: 10.1021/acs.jmedchem.3c00415

Chemical Information

Molecular Formula C22H18FNO4
SMILEs C#CCOc1cccc(-c2ccc(NC(=O)C3=C(C(=O)O)CCC3)c(F)c2)c1
InChI InChI=1S/C22H18FNO4/c1-2-11-28-16-6-3-5-14(12-16)15-9-10-20(19(23)13-15)24-21(25)17-7-4-8-18(17)22(26)27/h1,3,5-6,9-10,12-13H,4,7-8,11H2,(H,24,25)(H,26,27)
Molecular weight 379.12 Da
AlogP 4.008300000000002
HBond acceptors 5
HBond donors 2
Atoms 46

Expert Reviews

by SERP
(on 17 May 2026)
Cellular Use Rating
In Model Organisms
The Nurr1 agonist compound 29 demonstrates selectivity for human Nurr1 over its closely related sister receptors (Nur77 and NOR1), a panel of other nuclear receptors, and DHODH, though no additional panel...
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