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GSK2033

GSK2033 : Antagonist, Inverse Agonist, mix Agonist/Antagonist in vivo of NR1H2 and NR1H3

Structure

Information

  • NR1H2
  • NR1H3
  • Antagonist, Inverse Agonist, mix Agonist/Antagonist in vivo
  • >100 nM

In Vitro Validations

Uniprot ID: P55055
Target Class: NHR
Target SubClass: NR1 Subfamily
Potency: IC 50
Potency Value: 31.6 nM
Potency Assay: LXR LEADseeker binding assay
PDB ID for probe-target interaction (3D structure): --
Structure-activity relationship: yes
Target aliases:
Oxysterols receptor LXR-beta, UNR, NER, LXRB, NR1H ...

DOI Reference: 10.1021/jm901797p

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Cell:
GSK2033 was inactive (XC50 > 10 μM) in cellular and biochemical NR assays, including PXR, LRH-1, and FXR.
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SERP ratings and comments

No SERP comments found for GSK2033