Assay Detail
Functional
CHEMBL859244
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H] norepinephrine uptake into human NET expressed in HEK293 cells
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sodium-dependent noradrenaline transporter (CHEMBL222) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
1-(4-Methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one (Pyrovalerone) analogues: a promising class of monoamine uptake inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 7.19 | 8.12 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL202846 | — | — | 1 | 8.12 |
| CHEMBL204254 | — | — | 1 | 8.03 |
| CHEMBL372312 | — | — | 1 | 7.95 |
| CHEMBL204759 | — | — | 1 | 7.93 |
| CHEMBL203562 | — | — | 1 | 7.91 |
| CHEMBL202409 | — | — | 1 | 7.75 |
| CHEMBL201978 | — | — | 1 | 7.73 |
| CHEMBL204538 | — | — | 1 | 7.71 |
| CHEMBL203403 | — | — | 1 | 7.71 |
| CHEMBL203488 | — | — | 1 | 7.68 |
| CHEMBL201666 | — | — | 1 | 7.64 |
| CHEMBL202348 | — | — | 1 | 7.60 |
| CHEMBL201960 | PYROVALERONE | 4.0 | 1 | 7.55 |
| CHEMBL202479 | — | — | 1 | 7.33 |
| CHEMBL205082 | — | — | 1 | 7.25 |
| CHEMBL426304 | — | — | 1 | 7.09 |
| CHEMBL202420 | — | — | 1 | 7.08 |
| CHEMBL202410 | — | — | 1 | 7.06 |
| CHEMBL203563 | — | — | 1 | 7.06 |
| CHEMBL201976 | — | — | 1 | 7.03 |
| CHEMBL203640 | — | — | 1 | 6.77 |
| CHEMBL381127 | — | — | 1 | 6.63 |
| CHEMBL369997 | — | — | 1 | 6.58 |
| CHEMBL379679 | — | — | 1 | 6.50 |
| CHEMBL2113217 | — | — | 1 | 6.46 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 6.42 |
| CHEMBL379446 | — | — | 1 | 6.28 |
| CHEMBL204288 | — | — | 1 | 6.10 |
| CHEMBL205028 | — | — | 1 | 5.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL202846 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL204254 | — | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL372312 | — | IC50 | = | 11.3 | nM | 7.95 |
| CHEMBL204759 | — | IC50 | = | 11.7 | nM | 7.93 |
| CHEMBL203562 | — | IC50 | = | 12.4 | nM | 7.91 |
| CHEMBL202409 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL201978 | — | IC50 | = | 18.5 | nM | 7.73 |
| CHEMBL204538 | — | IC50 | = | 19.3 | nM | 7.71 |
| CHEMBL203403 | — | IC50 | = | 19.7 | nM | 7.71 |
| CHEMBL203488 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL201666 | — | IC50 | = | 22.8 | nM | 7.64 |
| CHEMBL202348 | — | IC50 | = | 24.9 | nM | 7.60 |
| CHEMBL201960 | PYROVALERONE | IC50 | = | 28.3 | nM | 7.55 |
| CHEMBL202479 | — | IC50 | = | 46.5 | nM | 7.33 |
| CHEMBL205082 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL426304 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL202420 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL202410 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL203563 | — | IC50 | = | 86.7 | nM | 7.06 |
| CHEMBL201976 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL203640 | — | IC50 | = | 171.0 | nM | 6.77 |
| CHEMBL381127 | — | IC50 | = | 235.0 | nM | 6.63 |
| CHEMBL369997 | — | IC50 | = | 263.0 | nM | 6.58 |
| CHEMBL379679 | — | IC50 | = | 317.0 | nM | 6.50 |
| CHEMBL2113217 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL370805 | COCAINE | IC50 | = | 378.0 | nM | 6.42 |
| CHEMBL379446 | — | IC50 | = | 531.0 | nM | 6.28 |
| CHEMBL204288 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL205028 | — | IC50 | = | 2520.0 | nM | 5.60 |