Assay Detail
Binding
CHEMBL904957
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Inhibition of [3H]DA uptake at DAT in Sprague-Dawley rat striatum
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Striatum |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis and pharmacology of site-specific cocaine abuse treatment agents: restricted rotation analogues of methylphenidate.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 32 | 6.21 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54134 | — | — | 1 | 8.15 |
| CHEMBL556365 | — | — | 1 | 7.96 |
| CHEMBL537653 | — | — | 1 | 7.65 |
| CHEMBL537874 | — | — | 1 | 7.21 |
| CHEMBL559186 | — | — | 1 | 7.06 |
| CHEMBL904 | DEXMETHYLPHENIDATE HYDROCHLORIDE | 4.0 | 1 | 6.64 |
| CHEMBL541896 | — | — | 1 | 6.61 |
| CHEMBL537206 | — | — | 1 | 6.61 |
| CHEMBL537431 | — | — | 1 | 6.55 |
| CHEMBL537654 | — | — | 1 | 6.50 |
| CHEMBL541895 | — | — | 1 | 6.43 |
| CHEMBL529437 | COCAINE HYDROCHLORIDE | 4.0 | 1 | 6.39 |
| CHEMBL557356 | — | — | 1 | 6.17 |
| CHEMBL556366 | — | — | 1 | 5.97 |
| CHEMBL537429 | — | — | 1 | 5.90 |
| CHEMBL537209 | — | — | 1 | 5.82 |
| CHEMBL1203942 | — | — | 1 | 5.73 |
| CHEMBL534500 | — | — | 1 | 5.58 |
| CHEMBL537430 | — | — | 1 | 5.10 |
| CHEMBL541898 | — | — | 1 | 5.07 |
| CHEMBL534502 | — | — | 1 | 5.06 |
| CHEMBL553859 | — | — | 1 | 4.98 |
| CHEMBL553921 | — | — | 1 | 4.97 |
| CHEMBL541134 | — | — | 1 | 4.91 |
| CHEMBL537652 | — | — | 1 | - |
| CHEMBL558394 | — | — | 1 | - |
| CHEMBL558182 | — | — | 1 | - |
| CHEMBL540625 | — | — | 1 | - |
| CHEMBL534501 | — | — | 1 | - |
| CHEMBL553714 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54134 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL556365 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL537653 | — | IC50 | = | 22.5 | nM | 7.65 |
| CHEMBL537874 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL559186 | — | IC50 | = | 87.6 | nM | 7.06 |
| CHEMBL904 | DEXMETHYLPHENIDATE HYDROCHLORIDE | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL541896 | — | IC50 | = | 248.0 | nM | 6.61 |
| CHEMBL537206 | — | IC50 | = | 244.0 | nM | 6.61 |
| CHEMBL537431 | — | IC50 | = | 281.0 | nM | 6.55 |
| CHEMBL537654 | — | IC50 | = | 317.0 | nM | 6.50 |
| CHEMBL541895 | — | IC50 | = | 368.0 | nM | 6.43 |
| CHEMBL529437 | COCAINE HYDROCHLORIDE | IC50 | = | 404.0 | nM | 6.39 |
| CHEMBL557356 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL556366 | — | IC50 | = | 1060.0 | nM | 5.97 |
| CHEMBL537429 | — | IC50 | = | 1260.0 | nM | 5.90 |
| CHEMBL537209 | — | IC50 | = | 1520.0 | nM | 5.82 |
| CHEMBL1203942 | — | IC50 | = | 1850.0 | nM | 5.73 |
| CHEMBL534500 | — | IC50 | = | 2660.0 | nM | 5.58 |
| CHEMBL537430 | — | IC50 | = | 7960.0 | nM | 5.10 |
| CHEMBL541898 | — | IC50 | = | 8490.0 | nM | 5.07 |
| CHEMBL534502 | — | IC50 | = | 8800.0 | nM | 5.06 |
| CHEMBL553859 | — | IC50 | = | 10400.0 | nM | 4.98 |
| CHEMBL553921 | — | IC50 | = | 10700.0 | nM | 4.97 |
| CHEMBL541134 | — | IC50 | = | 12400.0 | nM | 4.91 |
| CHEMBL537652 | — | IC50 | - | — | - | |
| CHEMBL558394 | — | IC50 | - | — | - | |
| CHEMBL558182 | — | IC50 | - | — | - | |
| CHEMBL540625 | — | IC50 | - | — | - | |
| CHEMBL534501 | — | IC50 | - | — | - | |
| CHEMBL553714 | — | IC50 | - | — | - | |
| CHEMBL558395 | — | IC50 | - | — | - | |
| CHEMBL537875 | — | IC50 | - | — | - |