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Assay Detail

CHEMBL5527779

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

Binding
Inverse agonist activity at Gal4-fused human Nurr1 L444F mutant transfected in HEK293T cells incubated for 16 hrs by firefly/renilla based Dual-Glo luciferase assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293T
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 3 5.09 5.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5549932 1 5.16
CHEMBL331916 1 5.10
CHEMBL1071 OXAPROZIN 4.0 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5549932 IC50 = 7000.0 nM 5.16
CHEMBL331916 IC50 = 8000.0 nM 5.10
CHEMBL1071 OXAPROZIN IC50 = 10000.0 nM 5.00