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Assay Detail

CHEMBL5369675

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

Binding
Agonist activity at Gal4-fused human full length Nurr1 transfected in human HEK293T cells co-transfected with pFR-Luc-NBRE/pRL-SV40 assessed as activation of NBRE luciferase activity incubated for 16 hrs by Dual-Glo luciferase assay
2
Total Activities
2
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

Structure-Guided Design of Nurr1 Agonists Derived from the Natural Ligand Dihydroxyindole.
Sai M, Vietor J, Kornmayer M, Egner M, López-García Ú, Höfner G, Pabel J, Marschner JA, Wein T, Merk D.
J Med Chem (2023) 66 : 13556 -13567
PubMed 37751901 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 5.55 5.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5415710 1 5.70
CHEMBL5405956 1 5.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5415710 EC50 = 2000.0 nM 5.70
CHEMBL5405956 EC50 = 4000.0 nM 5.40