Assay Detail
Binding
CHEMBL754231
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Inhibition of [3H]-NE reuptake at Norepinephrine transporter in rat parietal/occipital cortex
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Thiophene derivatives: a new series of potent norepinephrine and serotonin reuptake inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 6.75 | 8.31 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL117047 | — | — | 1 | 8.31 |
| CHEMBL119477 | — | — | 1 | 8.30 |
| CHEMBL331565 | — | — | 1 | 7.58 |
| CHEMBL174854 | — | — | 1 | 7.28 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 6.97 |
| CHEMBL367744 | — | — | 1 | 6.55 |
| CHEMBL366383 | — | — | 1 | 6.05 |
| CHEMBL173834 | — | — | 1 | 5.93 |
| CHEMBL369497 | — | — | 1 | 5.91 |
| CHEMBL366993 | — | — | 1 | 5.77 |
| CHEMBL175338 | — | — | 1 | 5.61 |
| CHEMBL173835 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL117047 | — | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL119477 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL331565 | — | Ki | = | 26.4 | nM | 7.58 |
| CHEMBL174854 | — | Ki | = | 52.3 | nM | 7.28 |
| CHEMBL370805 | COCAINE | Ki | = | 108.0 | nM | 6.97 |
| CHEMBL367744 | — | Ki | = | 283.0 | nM | 6.55 |
| CHEMBL366383 | — | Ki | = | 894.0 | nM | 6.05 |
| CHEMBL173834 | — | Ki | = | 1180.0 | nM | 5.93 |
| CHEMBL369497 | — | Ki | = | 1234.0 | nM | 5.91 |
| CHEMBL366993 | — | Ki | = | 1700.0 | nM | 5.77 |
| CHEMBL175338 | — | Ki | = | 2430.0 | nM | 5.61 |
| CHEMBL173835 | — | Ki | ~ | 300.0 | nM | - |