Assay Detail
Binding
CHEMBL5527742
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inverse agonist activity at Gal4-fused human full length Nurr1 LBD transfected in HEK293T cells assessed as suppression of Nurr1 activation incubated for 16 hrs by firefly/renilla based Dual-Glo luciferase assay
47
Total Activities
43
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
Structural Optimization of Oxaprozin for Selective Inverse Nurr1 Agonism.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 47 | 4.53 | 5.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5417665 | — | — | 1 | 5.36 |
| CHEMBL4851009 | — | — | 1 | 5.16 |
| CHEMBL5567300 | — | — | 1 | 4.92 |
| CHEMBL5560531 | — | — | 1 | 4.89 |
| CHEMBL4439422 | — | — | 1 | 4.85 |
| CHEMBL4863720 | — | — | 1 | 4.85 |
| CHEMBL4858779 | — | — | 1 | 4.82 |
| CHEMBL5394779 | — | — | 1 | 4.80 |
| CHEMBL5562146 | — | — | 1 | 4.77 |
| CHEMBL333698 | — | — | 1 | 4.77 |
| CHEMBL5561118 | — | — | 1 | 4.72 |
| CHEMBL4875485 | — | — | 1 | 4.66 |
| CHEMBL5532573 | — | — | 3 | 4.64 |
| CHEMBL5558226 | — | — | 1 | 4.64 |
| CHEMBL5399947 | — | — | 1 | 4.62 |
| CHEMBL5555816 | — | — | 1 | 4.62 |
| CHEMBL4851869 | — | — | 1 | 4.60 |
| CHEMBL5549932 | — | — | 1 | 4.58 |
| CHEMBL5559650 | — | — | 1 | 4.55 |
| CHEMBL4858476 | — | — | 1 | 4.51 |
| CHEMBL5560120 | — | — | 1 | 4.48 |
| CHEMBL4847339 | — | — | 1 | 4.47 |
| CHEMBL5562187 | — | — | 3 | 4.46 |
| CHEMBL331916 | — | — | 1 | 4.44 |
| CHEMBL1609102 | — | — | 1 | 4.42 |
| CHEMBL5563133 | — | — | 1 | 4.40 |
| CHEMBL5562156 | — | — | 1 | 4.39 |
| CHEMBL5568366 | — | — | 1 | 4.37 |
| CHEMBL5560912 | — | — | 1 | 4.37 |
| CHEMBL5561231 | — | — | 1 | 4.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5417665 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL4851009 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL5567300 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL5560531 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL4439422 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL4863720 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL4858779 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL5394779 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL5562146 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL333698 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL5561118 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL4875485 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL5558226 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL5532573 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL5555816 | — | IC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL5399947 | — | IC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL4851869 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL5549932 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL5559650 | — | IC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL4858476 | — | IC50 | = | 31000.0 | nM | 4.51 |
| CHEMBL5560120 | — | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL5532573 | — | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL4847339 | — | IC50 | = | 34000.0 | nM | 4.47 |
| CHEMBL5562187 | — | IC50 | = | 35000.0 | nM | 4.46 |
| CHEMBL331916 | — | IC50 | = | 36000.0 | nM | 4.44 |
| CHEMBL1609102 | — | IC50 | = | 38000.0 | nM | 4.42 |
| CHEMBL5532573 | — | IC50 | = | 39000.0 | nM | 4.41 |
| CHEMBL5563133 | — | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL5562156 | — | IC50 | = | 41000.0 | nM | 4.39 |
| CHEMBL5560912 | — | IC50 | = | 43000.0 | nM | 4.37 |
| CHEMBL5568366 | — | IC50 | = | 43000.0 | nM | 4.37 |
| CHEMBL5561231 | — | IC50 | = | 46000.0 | nM | 4.34 |
| CHEMBL5562187 | — | IC50 | = | 50000.0 | nM | 4.30 |
| CHEMBL5398853 | — | IC50 | = | 50000.0 | nM | 4.30 |
| CHEMBL5542726 | — | IC50 | = | 52000.0 | nM | 4.28 |
| CHEMBL1707568 | — | IC50 | = | 56000.0 | nM | 4.25 |
| CHEMBL5557077 | — | IC50 | = | 58000.0 | nM | 4.24 |
| CHEMBL5562187 | — | IC50 | = | 60000.0 | nM | 4.22 |
| CHEMBL5566789 | — | IC50 | = | 64000.0 | nM | 4.19 |
| CHEMBL5559721 | — | IC50 | = | 69000.0 | nM | 4.16 |
| CHEMBL5395851 | — | IC50 | = | 70000.0 | nM | 4.16 |
| CHEMBL5559129 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL4873831 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4876667 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4864263 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL5567959 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4859732 | — | IC50 | > | 50000.0 | nM | - |