JNJ-54119936

JNJ-54119936 : Inverse Agonist of RORC

Structure

SERP Rating

Probe JNJ-54119936 is in the process of SERP review.

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Information

RORC

Inverse Agonist

Up to 1µM

Additional Data

SGC image SGC Chemical Probe Collection

In Vitro Validations

Uniprot ID: P51449

Target Class: NHR

Target SubClass: Orphan Receptor

Potency: Kd

Potency Value: 5.3 nM

Potency Assay: Binding to RORC ligand-binding domain (ThermoFluor Binding Assay)

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

Target aliases:

Nuclear receptor ROR-gamma, RZRG, RORG, NR1F3, ROR ...

DOI Reference: 10.1038/s41598-021-90497-9

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

Selectivity within target family - RORA TF qKD > 75 µM; RORB TF qKD > 75 µM Nuclear receptor selectivity: PPARA, PPARD, PPARG, NR1H3, NR1H2, NR1I3, NR1H4, NR3C1, NR1D1, NR1D2, THRA, THRB, VDR, NR1I2, RXRA: No significant ago/antagonism at 3 µM Selectivity outside target family - Cerep Panel (50 targets) at 1 and 10 µM: all < 50 % inhibition DiscoverX panel (50 kinases) at 10 µM: all < 50 % inhibition

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