Assay Detail
Binding
CHEMBL847751
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Binding affinity against sigma receptor using radioligand ([3H](+)-pentazocine) binding assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL287) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Development of novel, potent, and selective dopamine reuptake inhibitors through alteration of the piperazine ring of 1-[2-(diphenylmethoxy)ethyl]-and 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines (GBR 12935 and GBR 12909).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 6.69 | 8.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL348432 | — | — | 1 | 8.07 |
| CHEMBL142953 | — | — | 1 | 7.58 |
| CHEMBL142041 | — | — | 1 | 7.47 |
| CHEMBL142518 | — | — | 1 | 7.19 |
| CHEMBL358758 | — | — | 1 | 7.17 |
| CHEMBL141876 | — | — | 1 | 7.11 |
| CHEMBL357008 | — | — | 1 | 7.08 |
| CHEMBL342121 | — | — | 1 | 6.75 |
| CHEMBL143648 | — | — | 1 | 6.64 |
| CHEMBL142617 | — | — | 1 | 6.01 |
| CHEMBL140104 | — | — | 1 | 5.98 |
| CHEMBL142522 | — | — | 1 | 5.83 |
| CHEMBL142337 | — | — | 1 | 5.44 |
| CHEMBL342120 | — | — | 1 | 5.40 |
| CHEMBL143612 | — | — | 1 | - |
| CHEMBL143846 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL348432 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL142953 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL142041 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL142518 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL358758 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL141876 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL357008 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL342121 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL143648 | — | IC50 | = | 231.0 | nM | 6.64 |
| CHEMBL142617 | — | IC50 | = | 965.0 | nM | 6.01 |
| CHEMBL140104 | — | IC50 | = | 1050.0 | nM | 5.98 |
| CHEMBL142522 | — | IC50 | = | 1480.0 | nM | 5.83 |
| CHEMBL142337 | — | IC50 | = | 3640.0 | nM | 5.44 |
| CHEMBL342120 | — | IC50 | = | 4001.0 | nM | 5.40 |
| CHEMBL143612 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL143846 | — | IC50 | > | 10000.0 | nM | - |