ME43

ME43 : Agonist of NR4A2, NR4A1 and NR4A3

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(0 ratings)

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Probe ME43 is in the process of SERP review.

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Information

NR4A2
NR4A1
NR4A3

Agonist

up to 1 uM

Additional Data

SGC Chemical Probe Collection

In Vitro Validations

Uniprot ID: P43354

Target Class: NHR

Target SubClass: --

Potency: Kd

Potency Value: 120 nM

Potency Assay: ITC using recombinant Nurr1

PDB ID for probe-target interaction (3D structure): --

Target aliases:

Nuclear receptor subfamily 4 group A member 2, TIN ...

DOI Reference: 10.1021/acs.jmedchem.4c03104

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay (off target): Profiled on nuclear receptors outside the NR4A family, ME43 revealed moderate PXR activation as only off-target at 3 μM (EC50 = 1.5 ± 0.6 μM) corresponding to at least 25-fold selectivity.

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SERP ratings and comments

SERP Ratings

In Cell Rating

SERP Comments:

Cellular activity was observed across several Nurr1 complexes with EC50s < 100 nM. Established off-target effects (eg PXR) were observed at 3 uM, suggesting that use of the probe at concentrations < or << 1 uM is most likely to capture selective on-target effects. The overall data set supporting the probe is strong and includes X-Ray co-crystallography and ITC as biochemical assays in addition to various cellular reporters. While not a liability, no CETSA or other cellular target engagement data has been reported. Overall, a strong well characterized probe.

(last updated: 22 Feb 2026 )