Assay Detail
Binding
CHEMBL675907
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Inhibitory activity in displacing [125I]- RTI-55 binding to dopamine transporter in rat striatal membranes
23
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Striatum |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis of 2beta-acyl-3beta-(substituted naphthyl)-8-azabicyclo[3.2.1]octanes and their binding affinities at dopamine and serotonin transport sites.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 8.39 | 10.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL36720 | — | — | 1 | 10.52 |
| CHEMBL418190 | — | — | 2 | 9.92 |
| CHEMBL39990 | — | — | 1 | 9.89 |
| CHEMBL34243 | — | — | 1 | 9.82 |
| CHEMBL39589 | — | — | 1 | 9.60 |
| CHEMBL287945 | — | — | 1 | 9.46 |
| CHEMBL416058 | — | — | 1 | 9.41 |
| CHEMBL435371 | — | — | 1 | 9.35 |
| CHEMBL22930 | — | — | 1 | 8.90 |
| CHEMBL290412 | — | — | 1 | 8.88 |
| CHEMBL278572 | — | — | 1 | 8.28 |
| CHEMBL23142 | — | — | 1 | 8.09 |
| CHEMBL23672 | — | — | 2 | 8.00 |
| CHEMBL289849 | — | — | 1 | 7.90 |
| CHEMBL39340 | — | — | 1 | 7.60 |
| CHEMBL287940 | — | — | 1 | 7.51 |
| CHEMBL39764 | — | — | 1 | 7.35 |
| CHEMBL285039 | — | — | 1 | 7.12 |
| CHEMBL39330 | — | — | 1 | 6.83 |
| CHEMBL290662 | — | — | 1 | 6.65 |
| CHEMBL278122 | — | — | 1 | 6.36 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL36720 | — | IC50 | = | 0.03 | nM | 10.52 |
| CHEMBL418190 | — | IC50 | = | 0.12 | nM | 9.92 |
| CHEMBL39990 | — | IC50 | = | 0.13 | nM | 9.89 |
| CHEMBL34243 | — | IC50 | = | 0.15 | nM | 9.82 |
| CHEMBL39589 | — | IC50 | = | 0.25 | nM | 9.60 |
| CHEMBL287945 | — | IC50 | = | 0.35 | nM | 9.46 |
| CHEMBL416058 | — | IC50 | = | 0.39 | nM | 9.41 |
| CHEMBL435371 | — | IC50 | = | 0.45 | nM | 9.35 |
| CHEMBL22930 | — | IC50 | = | 1.27 | nM | 8.90 |
| CHEMBL290412 | — | IC50 | = | 1.31 | nM | 8.88 |
| CHEMBL418190 | — | IC50 | = | 2.51 | nM | 8.60 |
| CHEMBL278572 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL23142 | — | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL23672 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL289849 | — | IC50 | = | 12.6 | nM | 7.90 |
| CHEMBL39340 | — | IC50 | = | 25.1 | nM | 7.60 |
| CHEMBL287940 | — | IC50 | = | 30.8 | nM | 7.51 |
| CHEMBL39764 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL285039 | — | IC50 | = | 75.1 | nM | 7.12 |
| CHEMBL23672 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL39330 | — | IC50 | = | 148.0 | nM | 6.83 |
| CHEMBL290662 | — | IC50 | = | 225.0 | nM | 6.65 |
| CHEMBL278122 | — | IC50 | = | 436.0 | nM | 6.36 |