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Assay Detail

CHEMBL5033037

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

Binding
Agonist activity at TAE expressed in human HEK293T cells coexpressing human full-length TLX/Gal4-VP 16 assessed as renilla luciferase reporter activity incubated for 14 hrs by Dual-glo luciferase
7
Total Activities
7
Compounds Tested
2
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 2 group E member 1 (CHEMBL1961788)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Propranolol Activates the Orphan Nuclear Receptor TLX to Counteract Proliferation and Migration of Glioblastoma Cells.
Faudone G, Bischoff-Kont I, Rachor L, Willems S, Zhubi R, Kaiser A, Chaikuad A, Knapp S, Fürst R, Heering J, Merk D.
J Med Chem (2021) 64 : 8727 -8738
PubMed 34115934 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 4.40 4.43
Activity 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL27 PROPRANOLOL 4.0 1 4.43
CHEMBL31888 1 4.37
CHEMBL269236 TRYPTOLINE 1 -
CHEMBL3304960 1 -
CHEMBL631 PROPAFENONE 4.0 1 -
CHEMBL24 ATENOLOL 4.0 1 -
CHEMBL471 SOTALOL 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL27 PROPRANOLOL EC50 = 37000.0 nM 4.43
CHEMBL31888 EC50 = 43000.0 nM 4.37
CHEMBL269236 TRYPTOLINE EC50 > 100000.0 nM -
CHEMBL3304960 EC50 > 100000.0 nM -
CHEMBL631 PROPAFENONE EC50 - -
CHEMBL24 ATENOLOL EC50 - -
CHEMBL471 SOTALOL Activity - -