Assay Detail
Binding
CHEMBL673261
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Inhibition of [3H]WIN-35428 binding to Dopamine transporter in rhesus (Macaca mulatta) or cynomolgus monkey (Macaca fascicularis) caudate-putamen
51
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cercopithecidae |
| Tissue | Caudate-putamen |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL238) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis of 6- and 7- hydroxy-8-azabicyclo[3.2.1]octanes and their binding affinity for the dopamine and serotonin transporters.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 51 | 7.48 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL91184 | — | — | 1 | 9.52 |
| CHEMBL87031 | — | — | 2 | 9.42 |
| CHEMBL87567 | — | — | 2 | 9.31 |
| CHEMBL606929 | — | — | 1 | 9.12 |
| CHEMBL86590 | — | — | 2 | 9.09 |
| CHEMBL88915 | — | — | 1 | 8.94 |
| CHEMBL330228 | — | — | 3 | 8.92 |
| CHEMBL86654 | — | — | 2 | 8.90 |
| CHEMBL84680 | — | — | 1 | 8.53 |
| CHEMBL89476 | — | — | 1 | 8.52 |
| CHEMBL421167 | — | — | 2 | 8.52 |
| CHEMBL606930 | — | — | 1 | 8.13 |
| CHEMBL315172 | — | — | 2 | 8.11 |
| CHEMBL2079586 | — | — | 2 | 7.96 |
| CHEMBL2115225 | — | — | 1 | 7.85 |
| CHEMBL2114227 | — | — | 1 | 7.85 |
| CHEMBL86710 | — | — | 1 | 7.71 |
| CHEMBL88246 | — | — | 1 | 7.48 |
| CHEMBL421546 | — | — | 1 | 7.35 |
| CHEMBL432571 | — | — | 1 | 7.26 |
| CHEMBL1790051 | — | — | 1 | 7.19 |
| CHEMBL89709 | — | — | 2 | 6.96 |
| CHEMBL88563 | — | — | 2 | 6.63 |
| CHEMBL316428 | — | — | 1 | 6.61 |
| CHEMBL606928 | — | — | 1 | 6.58 |
| CHEMBL89469 | — | — | 1 | 6.39 |
| CHEMBL89906 | — | — | 1 | 6.35 |
| CHEMBL314887 | — | — | 2 | 6.32 |
| CHEMBL2310846 | — | — | 2 | 6.32 |
| CHEMBL89662 | — | — | 1 | 5.59 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL91184 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL87031 | — | IC50 | = | 0.38 | nM | 9.42 |
| CHEMBL87567 | — | IC50 | = | 0.49 | nM | 9.31 |
| CHEMBL87567 | — | IC50 | = | 0.57 | nM | 9.24 |
| CHEMBL606929 | — | IC50 | = | 0.76 | nM | 9.12 |
| CHEMBL86590 | — | IC50 | = | 0.81 | nM | 9.09 |
| CHEMBL86590 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL87031 | — | IC50 | = | 1.09 | nM | 8.96 |
| CHEMBL88915 | — | IC50 | = | 1.16 | nM | 8.94 |
| CHEMBL330228 | — | IC50 | = | 1.19 | nM | 8.92 |
| CHEMBL86654 | — | IC50 | = | 1.26 | nM | 8.90 |
| CHEMBL330228 | — | IC50 | = | 1.42 | nM | 8.85 |
| CHEMBL86654 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL84680 | — | IC50 | = | 2.94 | nM | 8.53 |
| CHEMBL421167 | — | IC50 | = | 3.02 | nM | 8.52 |
| CHEMBL89476 | — | IC50 | = | 3.04 | nM | 8.52 |
| CHEMBL421167 | — | IC50 | = | 6.09 | nM | 8.21 |
| CHEMBL606930 | — | IC50 | = | 7.37 | nM | 8.13 |
| CHEMBL315172 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL2079586 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2115225 | — | IC50 | = | 14.2 | nM | 7.85 |
| CHEMBL2114227 | — | IC50 | = | 14.1 | nM | 7.85 |
| CHEMBL2079586 | — | IC50 | = | 17.9 | nM | 7.75 |
| CHEMBL86710 | — | IC50 | = | 19.4 | nM | 7.71 |
| CHEMBL315172 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL88246 | — | IC50 | = | 33.2 | nM | 7.48 |
| CHEMBL421546 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL330228 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL432571 | — | IC50 | = | 55.1 | nM | 7.26 |
| CHEMBL1790051 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL89709 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL89709 | — | IC50 | = | 123.0 | nM | 6.91 |
| CHEMBL88563 | — | IC50 | = | 235.0 | nM | 6.63 |
| CHEMBL316428 | — | IC50 | = | 246.0 | nM | 6.61 |
| CHEMBL606928 | — | IC50 | = | 265.0 | nM | 6.58 |
| CHEMBL89469 | — | IC50 | = | 408.0 | nM | 6.39 |
| CHEMBL89906 | — | IC50 | = | 448.0 | nM | 6.35 |
| CHEMBL314887 | — | IC50 | = | 477.0 | nM | 6.32 |
| CHEMBL2310846 | — | IC50 | = | 482.0 | nM | 6.32 |
| CHEMBL88563 | — | IC50 | = | 518.0 | nM | 6.29 |
| CHEMBL314887 | — | IC50 | = | 739.0 | nM | 6.13 |
| CHEMBL89662 | — | IC50 | = | 2590.0 | nM | 5.59 |
| CHEMBL2310846 | — | IC50 | = | 2690.0 | nM | 5.57 |
| CHEMBL89208 | — | IC50 | = | 3530.0 | nM | 5.45 |
| CHEMBL89208 | — | IC50 | = | 6150.0 | nM | 5.21 |
| CHEMBL314912 | — | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL314138 | — | IC50 | = | 7730.0 | nM | 5.11 |
| CHEMBL89208 | — | IC50 | = | 32600.0 | nM | 4.49 |
| CHEMBL330250 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL89756 | — | IC50 | > | 150000.0 | nM | - |