Assay Detail
Binding
CHEMBL670040
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Inhibition of [125I]RTI-55 binding to dopamine transport sites in rat striatal membranes.
21
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 2 beta-acyl-3 beta-aryl-8-azabicyclo[3.2.1]octanes and their binding affinities at dopamine and serotonin transport sites in rat striatum and frontal cortex.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 7.57 | 10.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL418190 | — | — | 3 | 10.37 |
| CHEMBL22930 | — | — | 1 | 9.55 |
| CHEMBL22518 | — | — | 1 | 8.64 |
| CHEMBL23142 | — | — | 3 | 8.38 |
| CHEMBL278572 | — | — | 1 | 8.27 |
| CHEMBL23141 | — | — | 1 | 8.01 |
| CHEMBL23672 | — | — | 1 | 8.00 |
| CHEMBL23655 | — | — | 1 | 7.82 |
| CHEMBL23875 | — | — | 1 | 7.32 |
| CHEMBL22665 | — | — | 1 | 7.15 |
| CHEMBL416007 | — | — | 1 | 6.94 |
| CHEMBL23974 | — | — | 1 | 6.82 |
| CHEMBL278122 | — | — | 1 | 6.36 |
| CHEMBL277200 | — | — | 1 | 5.89 |
| CHEMBL22377 | — | — | 1 | 5.67 |
| CHEMBL280382 | — | — | 1 | 5.34 |
| CHEMBL281413 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL418190 | — | IC50 | = | 0.043 | nM | 10.37 |
| CHEMBL418190 | — | IC50 | = | 0.115 | nM | 9.94 |
| CHEMBL22930 | — | IC50 | = | 0.28 | nM | 9.55 |
| CHEMBL22518 | — | IC50 | = | 2.29 | nM | 8.64 |
| CHEMBL23142 | — | IC50 | = | 4.21 | nM | 8.38 |
| CHEMBL278572 | — | IC50 | = | 5.34 | nM | 8.27 |
| CHEMBL23142 | — | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL23141 | — | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL23672 | — | IC50 | = | 10.1 | nM | 8.00 |
| CHEMBL23655 | — | IC50 | = | 15.3 | nM | 7.82 |
| CHEMBL23875 | — | IC50 | = | 48.3 | nM | 7.32 |
| CHEMBL22665 | — | IC50 | = | 70.8 | nM | 7.15 |
| CHEMBL418190 | — | IC50 | = | 113.0 | nM | 6.95 |
| CHEMBL416007 | — | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL23974 | — | IC50 | = | 152.0 | nM | 6.82 |
| CHEMBL278122 | — | IC50 | = | 436.0 | nM | 6.36 |
| CHEMBL277200 | — | IC50 | = | 1287.0 | nM | 5.89 |
| CHEMBL23142 | — | IC50 | = | 1337.0 | nM | 5.87 |
| CHEMBL22377 | — | IC50 | = | 2120.0 | nM | 5.67 |
| CHEMBL280382 | — | IC50 | = | 4610.0 | nM | 5.34 |
| CHEMBL281413 | — | IC50 | > | 50000.0 | nM | - |