JV322 |
JV322 : Agonist of NR4A1, NR4A2, NR4A3
Probe Summary
| Targets | Biochemical/Biophysical Potency | Cellular Potency |
|---|---|---|
| NR4A1 |
|
|
| NR4A2 |
| |
| NR4A3 |
|
300 - 600 nM
Selectivity
In Vitro Selectivity Assessment
Potency Assay Off-Target:
JV332 is selective over nuclear receptors outside the NR4A family with moderate DHODH activation at ...
Potency Cellular
In Vitro
NR4A1
Mode of Action: Agonist
Structure-Activity-Relationship data available? No
DOI Reference: 10.1021/acs.jmedchem.5c03217
NR4A2
Mode of Action: Agonist
Structure-Activity-Relationship data available? No
DOI Reference: 10.1021/acs.jmedchem.5c03217
NR4A3
Mode of Action: Agonist
Structure-Activity-Relationship data available? No
DOI Reference: 10.1021/acs.jmedchem.5c03217
Negative Control Compounds
JV339
Notes: Methylation of the amide linker of JV332 (53) in JV339 (54) abolished activity on all NR4A receptors up to 100 μM corresponding to at least 1000-fold reduced potency.
SMILES:
O=C(O)C1=C(C(N(C)C2=CC=C(C3=C4C(OC(F)(O4)F)=CC=C3)C=C2Cl)=O)CCC1
Chemical Information
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