Assay Detail
Binding
CHEMBL1949347
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Displacement of [3H]8-OH-DPAT from 5HT1A receptor in cerebral cortex homogenates after 15 mins
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Cerebral cortex |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Synthesis, in vitro binding studies and docking of long-chain arylpiperazine nitroquipazine analogues, as potential serotonin transporter inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 6.55 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL297702 | — | — | 1 | 7.96 |
| CHEMBL485540 | — | — | 1 | 7.89 |
| CHEMBL1945686 | — | — | 1 | 7.82 |
| CHEMBL485542 | — | — | 1 | 7.62 |
| CHEMBL485541 | — | — | 1 | 7.43 |
| CHEMBL299638 | — | — | 1 | 7.41 |
| CHEMBL483176 | — | — | 1 | 7.41 |
| CHEMBL1945681 | — | — | 1 | 6.66 |
| CHEMBL18772 | QUIPAZINE | 2.0 | 1 | 6.64 |
| CHEMBL520024 | — | — | 1 | 6.56 |
| CHEMBL1945475 | — | — | 1 | 6.15 |
| CHEMBL1945679 | — | — | 1 | 6.11 |
| CHEMBL1945680 | — | — | 1 | 5.96 |
| CHEMBL1945684 | — | — | 1 | 5.85 |
| CHEMBL1945682 | — | — | 1 | 5.68 |
| CHEMBL1945685 | — | — | 1 | 5.50 |
| CHEMBL1945678 | — | — | 1 | 4.97 |
| CHEMBL1945683 | — | — | 1 | 4.23 |
| CHEMBL41140 | 6-NITROQUIPAZINE | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL297702 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL485540 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL1945686 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL485542 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL485541 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL299638 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL483176 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL1945681 | — | Ki | = | 221.0 | nM | 6.66 |
| CHEMBL18772 | QUIPAZINE | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL520024 | — | Ki | = | 275.0 | nM | 6.56 |
| CHEMBL1945475 | — | Ki | = | 711.0 | nM | 6.15 |
| CHEMBL1945679 | — | Ki | = | 776.5 | nM | 6.11 |
| CHEMBL1945680 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL1945684 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL1945682 | — | Ki | = | 2100.0 | nM | 5.68 |
| CHEMBL1945685 | — | Ki | = | 3200.0 | nM | 5.50 |
| CHEMBL1945678 | — | Ki | = | 10600.0 | nM | 4.97 |
| CHEMBL1945683 | — | Ki | = | 59000.0 | nM | 4.23 |
| CHEMBL41140 | 6-NITROQUIPAZINE | Ki | - | — | - |