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Assay Detail

CHEMBL4370880

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

Binding
Agonist activity at Nurr1 in mouse N2A cells harboring NBRE by luciferase reporter gene assay
34
Total Activities
17
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type N2a
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Nuclear receptor subfamily 4 group A member 2 (CHEMBL3879839)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Development of a novel NURR1/NOT agonist from hit to lead and candidate for the potential treatment of Parkinson's disease.
Lesuisse D, Malanda A, Peyronel JF, Evanno Y, Lardenois P, De-Peretti D, Abécassis PY, Barnéoud P, Brunel P, Burgevin MC, Cegarra C, Auger F, Dommergue A, Lafon C, Even L, Tsi J, Luc TPH, Almario A, Olivier A, Castel MN, Taupin V, Rooney T, Vigé X.
Bioorg Med Chem Lett (2019) 29 : 929 -932
PubMed 30773432 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Emax 17 - -
EC50 17 8.38 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4579076 2 9.22
CHEMBL4435806 2 9.10
CHEMBL4472621 2 9.00
CHEMBL4576867 2 9.00
CHEMBL4542579 2 9.00
CHEMBL4453191 2 9.00
CHEMBL4516628 2 9.00
CHEMBL4440924 2 9.00
CHEMBL4475835 2 8.92
CHEMBL4455780 2 8.70
CHEMBL4464547 2 8.60
CHEMBL4450849 2 7.70
CHEMBL4465777 2 7.68
CHEMBL4528015 2 7.58
CHEMBL4521080 2 7.26
CHEMBL4454933 2 7.17
CHEMBL4473547 2 6.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4579076 EC50 = 0.6 nM 9.22
CHEMBL4435806 EC50 = 0.8 nM 9.10
CHEMBL4472621 EC50 = 1.0 nM 9.00
CHEMBL4576867 EC50 = 1.0 nM 9.00
CHEMBL4440924 EC50 = 1.0 nM 9.00
CHEMBL4516628 EC50 = 1.0 nM 9.00
CHEMBL4453191 EC50 = 1.0 nM 9.00
CHEMBL4542579 EC50 = 1.0 nM 9.00
CHEMBL4475835 EC50 = 1.2 nM 8.92
CHEMBL4455780 EC50 = 2.0 nM 8.70
CHEMBL4464547 EC50 = 2.5 nM 8.60
CHEMBL4450849 EC50 = 20.0 nM 7.70
CHEMBL4465777 EC50 = 21.0 nM 7.68
CHEMBL4528015 EC50 = 26.5 nM 7.58
CHEMBL4521080 EC50 = 55.0 nM 7.26
CHEMBL4454933 EC50 = 67.6 nM 7.17
CHEMBL4473547 EC50 = 292.0 nM 6.54
CHEMBL4473547 Emax = 52.0 % -
CHEMBL4475835 Emax = 64.0 % -
CHEMBL4579076 Emax = 86.0 % -
CHEMBL4453191 Emax = 68.0 % -
CHEMBL4542579 Emax = 85.0 % -
CHEMBL4516628 Emax = 104.0 % -
CHEMBL4435806 Emax = 72.0 % -
CHEMBL4440924 Emax = 103.0 % -
CHEMBL4450849 Emax = 62.0 % -
CHEMBL4528015 Emax = 68.0 % -
CHEMBL4464547 Emax = 85.0 % -
CHEMBL4454933 Emax = 70.0 % -
CHEMBL4576867 Emax = 240.0 % -
CHEMBL4465777 Emax = 61.0 % -
CHEMBL4472621 Emax = 204.0 % -
CHEMBL4455780 Emax = 87.0 % -
CHEMBL4521080 Emax = 85.0 % -