Assay Detail
Functional
CHEMBL5135478
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inverse agonist activity at 5-HT2A receptor (unknown origin) expressed in mouse NIH3T3 cells using o-nitrophenyl-D-galacto pyranoside incubated for 120 hrs
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | NIH3T3 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Improving the treatment of Parkinson's disease: Structure-based development of novel 5-HT<sub>2A</sub> receptor antagonists/inverse agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 38 | 7.73 | 8.71 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5189473 | — | — | 1 | 8.71 |
| CHEMBL5205903 | — | — | 1 | 8.68 |
| CHEMBL5184906 | — | — | 1 | 8.65 |
| CHEMBL5197899 | — | — | 1 | 8.60 |
| CHEMBL5173703 | — | — | 1 | 8.52 |
| CHEMBL5191581 | — | — | 1 | 8.37 |
| CHEMBL5172822 | — | — | 1 | 8.22 |
| CHEMBL5198919 | — | — | 1 | 8.18 |
| CHEMBL5175451 | — | — | 1 | 8.12 |
| CHEMBL5208211 | — | — | 1 | 8.08 |
| CHEMBL5200788 | — | — | 1 | 8.05 |
| CHEMBL5184297 | — | — | 1 | 8.04 |
| CHEMBL5185362 | — | — | 1 | 8.01 |
| CHEMBL5173149 | — | — | 1 | 8.00 |
| CHEMBL5178732 | — | — | 1 | 7.79 |
| CHEMBL5184703 | — | — | 1 | 7.64 |
| CHEMBL5192882 | — | — | 1 | 7.52 |
| CHEMBL5200155 | — | — | 1 | 7.48 |
| CHEMBL5198741 | — | — | 1 | 7.48 |
| CHEMBL5181200 | — | — | 1 | 7.37 |
| CHEMBL5200074 | — | — | 1 | 7.37 |
| CHEMBL2111101 | PIMAVANSERIN | 4.0 | 1 | 7.30 |
| CHEMBL5205849 | — | — | 1 | 7.19 |
| CHEMBL5198862 | — | — | 1 | 7.06 |
| CHEMBL5194786 | — | — | 1 | 7.00 |
| CHEMBL5194545 | — | — | 1 | 6.90 |
| CHEMBL5188950 | — | — | 1 | 6.87 |
| CHEMBL5188595 | — | — | 1 | 6.80 |
| CHEMBL5181432 | — | — | 1 | 6.06 |
| CHEMBL5181824 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5189473 | — | IC50 | = | 1.95 | nM | 8.71 |
| CHEMBL5205903 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL5184906 | — | IC50 | = | 2.23 | nM | 8.65 |
| CHEMBL5197899 | — | IC50 | = | 2.54 | nM | 8.60 |
| CHEMBL5173703 | — | IC50 | = | 3.05 | nM | 8.52 |
| CHEMBL5191581 | — | IC50 | = | 4.29 | nM | 8.37 |
| CHEMBL5172822 | — | IC50 | = | 6.01 | nM | 8.22 |
| CHEMBL5198919 | — | IC50 | = | 6.54 | nM | 8.18 |
| CHEMBL5175451 | — | IC50 | = | 7.59 | nM | 8.12 |
| CHEMBL5208211 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL5200788 | — | IC50 | = | 8.85 | nM | 8.05 |
| CHEMBL5184297 | — | IC50 | = | 9.22 | nM | 8.04 |
| CHEMBL5185362 | — | IC50 | = | 9.79 | nM | 8.01 |
| CHEMBL5173149 | — | IC50 | = | 10.04 | nM | 8.00 |
| CHEMBL5178732 | — | IC50 | = | 16.4 | nM | 7.79 |
| CHEMBL5184703 | — | IC50 | = | 22.8 | nM | 7.64 |
| CHEMBL5192882 | — | IC50 | = | 30.49 | nM | 7.52 |
| CHEMBL5200155 | — | IC50 | = | 33.34 | nM | 7.48 |
| CHEMBL5198741 | — | IC50 | = | 32.8 | nM | 7.48 |
| CHEMBL5181200 | — | IC50 | = | 42.74 | nM | 7.37 |
| CHEMBL5200074 | — | IC50 | = | 42.78 | nM | 7.37 |
| CHEMBL2111101 | PIMAVANSERIN | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL5205849 | — | IC50 | = | 64.94 | nM | 7.19 |
| CHEMBL5198862 | — | IC50 | = | 86.4 | nM | 7.06 |
| CHEMBL5194786 | — | IC50 | = | 101.0 | nM | 7.00 |
| CHEMBL5194545 | — | IC50 | = | 127.0 | nM | 6.90 |
| CHEMBL5188950 | — | IC50 | = | 134.1 | nM | 6.87 |
| CHEMBL5188595 | — | IC50 | = | 159.2 | nM | 6.80 |
| CHEMBL5181432 | — | IC50 | = | 872.4 | nM | 6.06 |
| CHEMBL5200635 | — | IC50 | - | — | - | |
| CHEMBL5199061 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL5179185 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL5176379 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL5169670 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL5201875 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL5174421 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL5193532 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL5181824 | — | IC50 | > | 500.0 | nM | - |