Assay Detail
Binding
CHEMBL859233
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Displacement of [125I]RTI-55 from human DAT expressed in HEK293 cells
39
Total Activities
39
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 | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL238) ↗| 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 |
|---|---|---|---|
| Ki | 39 | 6.84 | 7.94 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL203488 | — | — | 1 | 7.94 |
| CHEMBL202409 | — | — | 1 | 7.86 |
| CHEMBL372312 | — | — | 1 | 7.74 |
| CHEMBL204759 | — | — | 1 | 7.70 |
| CHEMBL201960 | PYROVALERONE | 4.0 | 1 | 7.67 |
| CHEMBL201978 | — | — | 1 | 7.54 |
| CHEMBL379679 | — | — | 1 | 7.52 |
| CHEMBL205082 | — | — | 1 | 7.47 |
| CHEMBL202348 | — | — | 1 | 7.40 |
| CHEMBL203562 | — | — | 1 | 7.31 |
| CHEMBL204254 | — | — | 1 | 7.29 |
| CHEMBL202420 | — | — | 1 | 7.29 |
| CHEMBL203403 | — | — | 1 | 7.22 |
| CHEMBL204538 | — | — | 1 | 7.21 |
| CHEMBL203640 | — | — | 1 | 7.09 |
| CHEMBL202479 | — | — | 1 | 7.09 |
| CHEMBL202846 | — | — | 1 | 7.08 |
| CHEMBL202410 | — | — | 1 | 7.04 |
| CHEMBL201976 | — | — | 1 | 6.98 |
| CHEMBL426304 | — | — | 1 | 6.96 |
| CHEMBL203563 | — | — | 1 | 6.90 |
| CHEMBL204288 | — | — | 1 | 6.84 |
| CHEMBL379446 | — | — | 1 | 6.58 |
| CHEMBL381127 | — | — | 1 | 6.48 |
| CHEMBL201666 | — | — | 1 | 6.44 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 6.37 |
| CHEMBL369997 | — | — | 1 | 6.34 |
| CHEMBL205028 | — | — | 1 | 6.28 |
| CHEMBL380699 | — | — | 1 | 5.88 |
| CHEMBL201977 | — | — | 1 | 5.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL203488 | — | Ki | = | 11.5 | nM | 7.94 |
| CHEMBL202409 | — | Ki | = | 13.7 | nM | 7.86 |
| CHEMBL372312 | — | Ki | = | 18.1 | nM | 7.74 |
| CHEMBL204759 | — | Ki | = | 20.1 | nM | 7.70 |
| CHEMBL201960 | PYROVALERONE | Ki | = | 21.4 | nM | 7.67 |
| CHEMBL201978 | — | Ki | = | 28.8 | nM | 7.54 |
| CHEMBL379679 | — | Ki | = | 30.2 | nM | 7.52 |
| CHEMBL205082 | — | Ki | = | 33.7 | nM | 7.47 |
| CHEMBL202348 | — | Ki | = | 39.9 | nM | 7.40 |
| CHEMBL203562 | — | Ki | = | 48.7 | nM | 7.31 |
| CHEMBL202420 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL204254 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL203403 | — | Ki | = | 59.7 | nM | 7.22 |
| CHEMBL204538 | — | Ki | = | 61.0 | nM | 7.21 |
| CHEMBL202479 | — | Ki | = | 81.4 | nM | 7.09 |
| CHEMBL203640 | — | Ki | = | 82.0 | nM | 7.09 |
| CHEMBL202846 | — | Ki | = | 84.0 | nM | 7.08 |
| CHEMBL202410 | — | Ki | = | 90.5 | nM | 7.04 |
| CHEMBL201976 | — | Ki | = | 105.0 | nM | 6.98 |
| CHEMBL426304 | — | Ki | = | 109.0 | nM | 6.96 |
| CHEMBL203563 | — | Ki | = | 125.0 | nM | 6.90 |
| CHEMBL204288 | — | Ki | = | 144.0 | nM | 6.84 |
| CHEMBL379446 | — | Ki | = | 266.0 | nM | 6.58 |
| CHEMBL381127 | — | Ki | = | 329.0 | nM | 6.48 |
| CHEMBL201666 | — | Ki | = | 360.0 | nM | 6.44 |
| CHEMBL370805 | COCAINE | Ki | = | 432.0 | nM | 6.37 |
| CHEMBL369997 | — | Ki | = | 460.0 | nM | 6.34 |
| CHEMBL205028 | — | Ki | = | 520.0 | nM | 6.28 |
| CHEMBL380699 | — | Ki | = | 1330.0 | nM | 5.88 |
| CHEMBL201977 | — | Ki | = | 1530.0 | nM | 5.82 |
| CHEMBL2113217 | — | Ki | = | 2310.0 | nM | 5.64 |
| CHEMBL377510 | — | Ki | = | 3850.0 | nM | 5.42 |
| CHEMBL202518 | — | Ki | = | 5900.0 | nM | 5.23 |
| CHEMBL377498 | — | Ki | = | 8440.0 | nM | 5.07 |
| CHEMBL202055 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL204490 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL202565 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL382768 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL202939 | — | Ki | > | 10000.0 | nM | - |