Assay Detail
Functional
CHEMBL4615083
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Antagonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of serotonin hydrochloride-induced calcium flux preincubated for 1 hr followed by serotonin hydrochloride addition by calcium 6 dye based FLIPR assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, Synthesis, and Biological Evaluation of New Peripheral 5HT2A Antagonists for Nonalcoholic Fatty Liver Disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 7.78 | 9.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4635010 | — | — | 1 | 9.41 |
| CHEMBL4644559 | — | — | 1 | 9.22 |
| CHEMBL4647697 | — | — | 1 | 9.06 |
| CHEMBL4638548 | — | — | 1 | 8.71 |
| CHEMBL4638345 | — | — | 1 | 8.08 |
| CHEMBL2111101 | PIMAVANSERIN | 4.0 | 1 | 7.66 |
| CHEMBL4633971 | — | — | 1 | 7.46 |
| CHEMBL4649679 | — | — | 1 | 6.50 |
| CHEMBL4640741 | — | — | 1 | 5.95 |
| CHEMBL4639499 | — | — | 1 | 5.70 |
| CHEMBL4645022 | — | — | 1 | - |
| CHEMBL4633476 | — | — | 1 | - |
| CHEMBL4642682 | — | — | 1 | - |
| CHEMBL4636657 | — | — | 1 | - |
| CHEMBL4646280 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4635010 | — | IC50 | = | 0.39 | nM | 9.41 |
| CHEMBL4644559 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4647697 | — | IC50 | = | 0.87 | nM | 9.06 |
| CHEMBL4638548 | — | IC50 | = | 1.93 | nM | 8.71 |
| CHEMBL4638345 | — | IC50 | = | 8.35 | nM | 8.08 |
| CHEMBL2111101 | PIMAVANSERIN | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4633971 | — | IC50 | = | 34.65 | nM | 7.46 |
| CHEMBL4649679 | — | IC50 | = | 317.3 | nM | 6.50 |
| CHEMBL4640741 | — | IC50 | = | 1126.0 | nM | 5.95 |
| CHEMBL4639499 | — | IC50 | = | 2018.0 | nM | 5.70 |
| CHEMBL4645022 | — | IC50 | - | — | - | |
| CHEMBL4633476 | — | IC50 | - | — | - | |
| CHEMBL4642682 | — | IC50 | - | — | - | |
| CHEMBL4636657 | — | IC50 | - | — | - | |
| CHEMBL4646280 | — | IC50 | - | — | - |