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Assay Detail

CHEMBL5527764

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inverse agonist activity at Gal4-fused human full length Nurr1 heterodimer transfected in HEK293T cells cotransfected with pSG5-RXR/pFR-Luc-DR5/pRL-SV40 (DR5) incubated for 12 to 14 hrs by firefly/renilla based Dual-Glo luciferase assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Nuclear receptor subfamily 4 group A member 2 (CHEMBL5002)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structural Optimization of Oxaprozin for Selective Inverse Nurr1 Agonism.
Willems S, Busch R, Nawa F, Ballarotto M, Lillich FF, Kasch T, López-García Ú, Marschner JA, Rüger LA, Renelt B, Ohrndorf J, Arifi S, Zaienne D, Proschak E, Pabel J, Merk D.
J Med Chem (2024) 67 : 13324 -13348
PubMed 39081058 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 4.92 4.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1071 OXAPROZIN 4.0 1 4.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1071 OXAPROZIN IC50 = 12000.0 nM 4.92