Assay Detail
Binding
CHEMBL4714158
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-nisoxetine from human NET expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Subcellular | Cell membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent noradrenaline transporter (CHEMBL222) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Bicyclic Diazepinones as Dual Ligands of the α2δ-1 Subunit of Voltage-Gated Calcium Channels and the Norepinephrine Transporter.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 39 | 6.87 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4750411 | — | — | 1 | 8.40 |
| CHEMBL4779959 | — | — | 1 | 7.54 |
| CHEMBL383921 | — | — | 1 | 7.41 |
| CHEMBL4790212 | — | — | 1 | 7.39 |
| CHEMBL4745144 | — | — | 1 | 7.23 |
| CHEMBL4764742 | — | — | 1 | 7.22 |
| CHEMBL4743954 | — | — | 1 | 7.16 |
| CHEMBL4748644 | — | — | 1 | 7.12 |
| CHEMBL4740331 | — | — | 1 | 7.11 |
| CHEMBL4744681 | — | — | 1 | 7.09 |
| CHEMBL4761288 | — | — | 1 | 6.98 |
| CHEMBL4785616 | — | — | 1 | 6.74 |
| CHEMBL4744472 | — | — | 1 | 6.52 |
| CHEMBL4747442 | — | — | 1 | 6.47 |
| CHEMBL4746870 | — | — | 1 | 6.45 |
| CHEMBL4753306 | — | — | 1 | 6.42 |
| CHEMBL4792765 | — | — | 1 | 6.42 |
| CHEMBL4757946 | — | — | 1 | 6.25 |
| CHEMBL4794892 | — | — | 1 | 6.21 |
| CHEMBL4756591 | — | — | 1 | 6.08 |
| CHEMBL4748656 | — | — | 1 | 6.00 |
| CHEMBL4790988 | — | — | 1 | - |
| CHEMBL4744000 | — | — | 1 | - |
| CHEMBL4746713 | — | — | 1 | - |
| CHEMBL4782498 | — | — | 1 | - |
| CHEMBL4790433 | — | — | 1 | - |
| CHEMBL4747320 | — | — | 1 | - |
| CHEMBL4761964 | — | — | 1 | - |
| CHEMBL4755653 | — | — | 1 | - |
| CHEMBL4744196 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4750411 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL4779959 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL383921 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL4790212 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL4745144 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL4764742 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL4743954 | — | Ki | = | 69.0 | nM | 7.16 |
| CHEMBL4748644 | — | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL4740331 | — | Ki | = | 77.0 | nM | 7.11 |
| CHEMBL4744681 | — | Ki | = | 82.0 | nM | 7.09 |
| CHEMBL4761288 | — | Ki | = | 105.0 | nM | 6.98 |
| CHEMBL4785616 | — | Ki | = | 182.0 | nM | 6.74 |
| CHEMBL4744472 | — | Ki | = | 305.0 | nM | 6.52 |
| CHEMBL4747442 | — | Ki | = | 341.0 | nM | 6.47 |
| CHEMBL4746870 | — | Ki | = | 356.0 | nM | 6.45 |
| CHEMBL4753306 | — | Ki | = | 382.0 | nM | 6.42 |
| CHEMBL4792765 | — | Ki | = | 383.0 | nM | 6.42 |
| CHEMBL4757946 | — | Ki | = | 556.0 | nM | 6.25 |
| CHEMBL4794892 | — | Ki | = | 610.0 | nM | 6.21 |
| CHEMBL4756591 | — | Ki | = | 842.0 | nM | 6.08 |
| CHEMBL4748656 | — | Ki | = | 995.0 | nM | 6.00 |
| CHEMBL4744196 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL1059 | PREGABALIN | Ki | > | 10000.0 | nM | - |
| CHEMBL4799404 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4750920 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4762006 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4799032 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4748556 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4798113 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4787604 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4791954 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4755653 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4761964 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4747320 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4790433 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4782498 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4746713 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4744000 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4790988 | — | Ki | > | 10000.0 | nM | - |