Assay Detail
Functional
CHEMBL800376
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of uptake of [3H]5-HT in synaptosomes from rat cortex
58
Total Activities
58
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sodium-dependent serotonin transporter (CHEMBL313) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Structure-activity studies for a novel series of N-(arylethyl)-N-(1,2,3,4-tetrahydronaphthalen-1-ylmethyl)-N-methylamine s possessing dual 5-HT uptake inhibiting and alpha2-antagonistic activities.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 58 | 7.21 | 8.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL10425 | — | — | 1 | 8.28 |
| CHEMBL10410 | — | — | 1 | 8.24 |
| CHEMBL490 | PAROXETINE | 4.0 | 1 | 8.19 |
| CHEMBL9970 | — | — | 1 | 8.18 |
| CHEMBL274867 | — | — | 1 | 8.05 |
| CHEMBL273874 | — | — | 1 | 8.02 |
| CHEMBL9896 | — | — | 1 | 7.95 |
| CHEMBL430314 | — | — | 1 | 7.94 |
| CHEMBL9783 | — | — | 1 | 7.90 |
| CHEMBL268258 | — | — | 1 | 7.88 |
| CHEMBL9912 | — | — | 1 | 7.84 |
| CHEMBL9886 | — | — | 1 | 7.79 |
| CHEMBL9925 | — | — | 1 | 7.78 |
| CHEMBL10102 | — | — | 1 | 7.75 |
| CHEMBL274391 | — | — | 1 | 7.74 |
| CHEMBL9938 | — | — | 1 | 7.74 |
| CHEMBL10115 | — | — | 1 | 7.71 |
| CHEMBL9831 | — | — | 1 | 7.69 |
| CHEMBL10409 | — | — | 1 | 7.69 |
| CHEMBL9869 | — | — | 1 | 7.65 |
| CHEMBL10369 | — | — | 1 | 7.61 |
| CHEMBL10052 | — | — | 1 | 7.57 |
| CHEMBL276236 | — | — | 1 | 7.50 |
| CHEMBL10066 | — | — | 1 | 7.47 |
| CHEMBL10170 | — | — | 1 | 7.46 |
| CHEMBL418337 | — | — | 1 | 7.42 |
| CHEMBL269402 | — | — | 1 | 7.41 |
| CHEMBL10385 | — | — | 1 | 7.37 |
| CHEMBL9924 | — | — | 1 | 7.35 |
| CHEMBL10411 | — | — | 1 | 7.33 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL10425 | — | IC50 | = | 5.25 | nM | 8.28 |
| CHEMBL10410 | — | IC50 | = | 5.81 | nM | 8.24 |
| CHEMBL490 | PAROXETINE | IC50 | = | 6.43 | nM | 8.19 |
| CHEMBL9970 | — | IC50 | = | 6.67 | nM | 8.18 |
| CHEMBL274867 | — | IC50 | = | 8.94 | nM | 8.05 |
| CHEMBL273874 | — | IC50 | = | 9.47 | nM | 8.02 |
| CHEMBL9896 | — | IC50 | = | 11.3 | nM | 7.95 |
| CHEMBL430314 | — | IC50 | = | 11.6 | nM | 7.94 |
| CHEMBL9783 | — | IC50 | = | 12.7 | nM | 7.90 |
| CHEMBL268258 | — | IC50 | = | 13.1 | nM | 7.88 |
| CHEMBL9912 | — | IC50 | = | 14.6 | nM | 7.84 |
| CHEMBL9886 | — | IC50 | = | 16.3 | nM | 7.79 |
| CHEMBL9925 | — | IC50 | = | 16.7 | nM | 7.78 |
| CHEMBL10102 | — | IC50 | = | 17.6 | nM | 7.75 |
| CHEMBL9938 | — | IC50 | = | 18.1 | nM | 7.74 |
| CHEMBL274391 | — | IC50 | = | 18.1 | nM | 7.74 |
| CHEMBL10115 | — | IC50 | = | 19.4 | nM | 7.71 |
| CHEMBL9831 | — | IC50 | = | 20.6 | nM | 7.69 |
| CHEMBL10409 | — | IC50 | = | 20.5 | nM | 7.69 |
| CHEMBL9869 | — | IC50 | = | 22.2 | nM | 7.65 |
| CHEMBL10369 | — | IC50 | = | 24.3 | nM | 7.61 |
| CHEMBL10052 | — | IC50 | = | 26.7 | nM | 7.57 |
| CHEMBL276236 | — | IC50 | = | 31.8 | nM | 7.50 |
| CHEMBL10066 | — | IC50 | = | 33.7 | nM | 7.47 |
| CHEMBL10170 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL418337 | — | IC50 | = | 38.2 | nM | 7.42 |
| CHEMBL269402 | — | IC50 | = | 38.9 | nM | 7.41 |
| CHEMBL10385 | — | IC50 | = | 42.8 | nM | 7.37 |
| CHEMBL9924 | — | IC50 | = | 44.4 | nM | 7.35 |
| CHEMBL10411 | — | IC50 | = | 46.7 | nM | 7.33 |
| CHEMBL10152 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL400421 | — | IC50 | = | 52.8 | nM | 7.28 |
| CHEMBL268463 | — | IC50 | = | 53.9 | nM | 7.27 |
| CHEMBL418336 | — | IC50 | = | 59.8 | nM | 7.22 |
| CHEMBL276667 | — | IC50 | = | 60.3 | nM | 7.22 |
| CHEMBL269452 | — | IC50 | = | 68.3 | nM | 7.17 |
| CHEMBL274055 | — | IC50 | = | 79.1 | nM | 7.10 |
| CHEMBL10304 | — | IC50 | = | 86.7 | nM | 7.06 |
| CHEMBL10068 | — | IC50 | = | 101.0 | nM | 7.00 |
| CHEMBL9860 | — | IC50 | = | 117.0 | nM | 6.93 |
| CHEMBL9755 | — | IC50 | = | 132.0 | nM | 6.88 |
| CHEMBL10187 | — | IC50 | = | 158.0 | nM | 6.80 |
| CHEMBL9974 | — | IC50 | = | 183.0 | nM | 6.74 |
| CHEMBL9894 | — | IC50 | = | 198.0 | nM | 6.70 |
| CHEMBL269171 | — | IC50 | = | 229.0 | nM | 6.64 |
| CHEMBL9944 | — | IC50 | = | 414.0 | nM | 6.38 |
| CHEMBL10317 | — | IC50 | = | 436.0 | nM | 6.36 |
| CHEMBL268749 | — | IC50 | = | 469.0 | nM | 6.33 |
| CHEMBL10216 | — | IC50 | = | 658.0 | nM | 6.18 |
| CHEMBL276826 | — | IC50 | = | 757.0 | nM | 6.12 |