Assay Detail
Binding
CHEMBL5369666
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Agonist activity at Gal4-fused human full length Nurr1 transfected in human HEK293T cells co-transfected with pFR-Luc/pRL-SV40 assessed as activation of luciferase activity incubated for 16 hrs by Dual-Glo luciferase assay
11
Total Activities
11
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.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 11 | 5.21 | 6.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1201753 | PITAVASTATIN | 4.0 | 1 | 6.92 |
| CHEMBL2220442 | FLUVASTATIN | 4.0 | 1 | 5.72 |
| CHEMBL5415710 | — | — | 1 | 5.52 |
| CHEMBL5405956 | — | — | 1 | 5.52 |
| CHEMBL5399464 | — | — | 1 | 5.30 |
| CHEMBL5431873 | — | — | 1 | 5.22 |
| CHEMBL5438087 | — | — | 1 | 4.92 |
| CHEMBL5416432 | — | — | 1 | 4.80 |
| CHEMBL5406325 | — | — | 1 | 4.55 |
| CHEMBL682 | AMODIAQUINE | 4.0 | 1 | 4.44 |
| CHEMBL555013 | — | — | 1 | 4.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1201753 | PITAVASTATIN | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL2220442 | FLUVASTATIN | EC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL5415710 | — | EC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL5405956 | — | EC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL5399464 | — | EC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL5431873 | — | EC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL5438087 | — | EC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL5416432 | — | EC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL5406325 | — | EC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL682 | AMODIAQUINE | EC50 | = | 36000.0 | nM | 4.44 |
| CHEMBL555013 | — | EC50 | = | 40000.0 | nM | 4.40 |