Assay Detail
Functional
CHEMBL4195142
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin calcium mobilization preincubated for 25 mins followed by serotonin challenge measured for 30 secs by aequorin-derived luminescence assay
16
Total Activities
8
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and activity of di- or trisubstituted N-(phenoxyalkyl)- or N-{2-[2-(phenoxy)ethoxy]ethyl}piperazine derivatives on the central nervous system.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 7.07 | 8.32 |
| Kb | 8 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL8618 | NAN-190 | — | 2 | 8.32 |
| CHEMBL4209888 | — | — | 2 | 8.14 |
| CHEMBL38288 | — | — | 2 | 7.77 |
| CHEMBL4207653 | — | — | 2 | 7.25 |
| CHEMBL4212812 | — | — | 2 | 6.54 |
| CHEMBL4213352 | — | — | 2 | 6.42 |
| CHEMBL4205526 | — | — | 2 | 6.22 |
| CHEMBL4203310 | — | — | 2 | 5.93 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL8618 | NAN-190 | IC50 | = | 4.73 | nM | 8.32 |
| CHEMBL4209888 | — | IC50 | = | 7.19 | nM | 8.14 |
| CHEMBL38288 | — | IC50 | = | 16.9 | nM | 7.77 |
| CHEMBL4207653 | — | IC50 | = | 56.8 | nM | 7.25 |
| CHEMBL4212812 | — | IC50 | = | 291.0 | nM | 6.54 |
| CHEMBL4213352 | — | IC50 | = | 376.0 | nM | 6.42 |
| CHEMBL4205526 | — | IC50 | = | 595.0 | nM | 6.22 |
| CHEMBL4203310 | — | IC50 | = | 1180.0 | nM | 5.93 |
| CHEMBL4209888 | — | Kb | = | 1.8 | nM | - |
| CHEMBL4205526 | — | Kb | = | 146.0 | nM | - |
| CHEMBL4212812 | — | Kb | = | 71.5 | nM | - |
| CHEMBL4213352 | — | Kb | = | 92.3 | nM | - |
| CHEMBL4207653 | — | Kb | = | 13.9 | nM | - |
| CHEMBL4203310 | — | Kb | = | 291.0 | nM | - |
| CHEMBL8618 | NAN-190 | Kb | = | 1.2 | nM | - |
| CHEMBL38288 | — | Kb | = | 6.6 | nM | - |