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Assay Detail

CHEMBL5343631

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

Binding
Binding affinity to recombinant N-terminal His6-tagged human Nurr1 LBD (362 to 598 residues) expressed in Escherichia coli BL21(DE3)-R3-pRARE2 by ITC method
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
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

<i>De Novo</i> Design of Nurr1 Agonists <i>via</i> Fragment-Augmented Generative Deep Learning in Low-Data Regime.
Ballarotto M, Willems S, Stiller T, Nawa F, Marschner JA, Grisoni F, Merk D.
J Med Chem (2023) 66 : 8170 -8177
PubMed 37256819 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 7 6.21 6.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5419377 1 6.85
CHEMBL197194 VIDOFLUDIMUS 3.0 1 6.16
CHEMBL5398399 1 5.62
CHEMBL5428075 1 -
CHEMBL5435108 1 -
CHEMBL5395387 1 -
CHEMBL5428771 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5419377 Kd = 140.0 nM 6.85
CHEMBL197194 VIDOFLUDIMUS Kd = 700.0 nM 6.16
CHEMBL5398399 Kd = 2400.0 nM 5.62
CHEMBL5428075 Kd - -
CHEMBL5435108 Kd - -
CHEMBL5395387 Kd - -
CHEMBL5428771 Kd - -