Assay Detail
Binding
CHEMBL1031548
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]serotonin reuptake at human SERT expressed in HEK cells
36
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent serotonin transporter (CHEMBL228) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
2,5-Disubstituted tetrahydrofurans as selective serotonin re-uptake inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 36 | 7.07 | 8.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL460407 | — | — | 1 | 8.68 |
| CHEMBL450907 | — | — | 2 | 8.64 |
| CHEMBL511500 | — | — | 1 | 8.60 |
| CHEMBL462311 | — | — | 1 | 8.60 |
| CHEMBL459367 | — | — | 1 | 8.59 |
| CHEMBL504028 | — | — | 1 | 8.40 |
| CHEMBL456223 | — | — | 1 | 7.93 |
| CHEMBL460406 | — | — | 1 | 7.76 |
| CHEMBL450769 | — | — | 1 | 7.64 |
| CHEMBL511163 | — | — | 1 | 7.64 |
| CHEMBL456638 | — | — | 1 | 7.62 |
| CHEMBL456222 | — | — | 1 | 7.57 |
| CHEMBL457968 | — | — | 1 | 7.52 |
| CHEMBL460204 | — | — | 1 | 7.51 |
| CHEMBL447825 | — | — | 1 | 7.50 |
| CHEMBL461268 | — | — | 1 | 7.30 |
| CHEMBL455221 | — | — | 1 | 7.08 |
| CHEMBL450987 | — | — | 1 | 6.96 |
| CHEMBL456221 | — | — | 1 | 6.91 |
| CHEMBL456639 | — | — | 1 | 6.89 |
| CHEMBL452928 | — | — | 1 | 6.65 |
| CHEMBL451652 | — | — | 1 | 6.21 |
| CHEMBL447750 | — | — | 1 | 6.20 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 6.19 |
| CHEMBL512736 | — | — | 1 | 5.95 |
| CHEMBL458639 | — | — | 1 | 5.77 |
| CHEMBL442843 | — | — | 1 | 5.68 |
| CHEMBL448912 | — | — | 1 | 5.65 |
| CHEMBL456017 | — | — | 1 | 5.59 |
| CHEMBL508678 | — | — | 1 | 5.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL460407 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL450907 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL511500 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL462311 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL459367 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL504028 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL450907 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL456223 | — | IC50 | = | 11.7 | nM | 7.93 |
| CHEMBL460406 | — | IC50 | = | 17.5 | nM | 7.76 |
| CHEMBL511163 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL450769 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL456638 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL456222 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL457968 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL460204 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL447825 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL461268 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL455221 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL450987 | — | IC50 | = | 111.0 | nM | 6.96 |
| CHEMBL456221 | — | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL456639 | — | IC50 | = | 129.0 | nM | 6.89 |
| CHEMBL452928 | — | IC50 | = | 225.0 | nM | 6.65 |
| CHEMBL451652 | — | IC50 | = | 617.0 | nM | 6.21 |
| CHEMBL447750 | — | IC50 | = | 636.0 | nM | 6.20 |
| CHEMBL370805 | COCAINE | IC50 | = | 642.0 | nM | 6.19 |
| CHEMBL512736 | — | IC50 | = | 1117.0 | nM | 5.95 |
| CHEMBL458639 | — | IC50 | = | 1714.0 | nM | 5.77 |
| CHEMBL442843 | — | IC50 | = | 2071.0 | nM | 5.68 |
| CHEMBL448912 | — | IC50 | = | 2260.0 | nM | 5.65 |
| CHEMBL456017 | — | IC50 | = | 2576.0 | nM | 5.59 |
| CHEMBL508678 | — | IC50 | = | 2721.0 | nM | 5.57 |
| CHEMBL457966 | — | IC50 | = | 4041.0 | nM | 5.39 |
| CHEMBL457967 | — | IC50 | = | 9029.0 | nM | 5.04 |
| CHEMBL451837 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL459390 | — | IC50 | - | — | - | |
| CHEMBL459391 | — | IC50 | - | — | - |