Assay Detail
Binding
CHEMBL802527
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of the uptake of tritiated dopamine (DA) in rat synaptosomes
87
Total Activities
79
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Pyrroloisoquinoline antidepressants. 2. In-depth exploration of structure-activity relationships.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 87 | 7.37 | 9.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1743810 | — | — | 1 | 9.07 |
| CHEMBL287474 | — | — | 1 | 9.00 |
| CHEMBL1743782 | — | — | 1 | 8.77 |
| CHEMBL1743786 | — | — | 1 | 8.60 |
| CHEMBL1743790 | — | — | 1 | 8.60 |
| CHEMBL286312 | — | — | 1 | 8.59 |
| CHEMBL32726 | — | — | 1 | 8.55 |
| CHEMBL1743805 | — | — | 1 | 8.54 |
| CHEMBL35013 | — | — | 1 | 8.49 |
| CHEMBL35184 | — | — | 3 | 8.36 |
| CHEMBL1743785 | — | — | 1 | 8.29 |
| CHEMBL1743767 | — | — | 1 | 8.28 |
| CHEMBL1743794 | — | — | 1 | 8.28 |
| CHEMBL35337 | AMFONELIC ACID | 2.0 | 1 | 8.14 |
| CHEMBL1743824 | — | — | 1 | 8.13 |
| CHEMBL32797 | — | — | 1 | 8.12 |
| CHEMBL1743798 | — | — | 1 | 8.11 |
| CHEMBL287859 | — | — | 1 | 8.08 |
| CHEMBL32720 | — | — | 1 | 8.06 |
| CHEMBL1743807 | — | — | 1 | 8.01 |
| CHEMBL35492 | — | — | 1 | 8.01 |
| CHEMBL1743819 | — | — | 1 | 8.00 |
| CHEMBL1743793 | — | — | 1 | 8.00 |
| CHEMBL287257 | DICLOFENSINE | 2.0 | 1 | 7.96 |
| CHEMBL35166 | — | — | 1 | 7.95 |
| CHEMBL36030 | — | — | 1 | 7.91 |
| CHEMBL34875 | — | — | 1 | 7.82 |
| CHEMBL431299 | — | — | 1 | 7.80 |
| CHEMBL1743803 | — | — | 3 | 7.76 |
| CHEMBL34990 | — | — | 3 | 7.63 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1743810 | — | Ki | = | 0.86 | nM | 9.07 |
| CHEMBL287474 | — | Ki | = | 0.99 | nM | 9.00 |
| CHEMBL1743782 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL1743786 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL1743790 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL286312 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL32726 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL1743805 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL35013 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL35184 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL1743785 | — | Ki | = | 5.1 | nM | 8.29 |
| CHEMBL1743767 | — | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL1743794 | — | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL35337 | AMFONELIC ACID | Ki | = | 7.2 | nM | 8.14 |
| CHEMBL1743824 | — | Ki | = | 7.4 | nM | 8.13 |
| CHEMBL32797 | — | Ki | = | 7.6 | nM | 8.12 |
| CHEMBL1743798 | — | Ki | = | 7.7 | nM | 8.11 |
| CHEMBL287859 | — | Ki | = | 8.4 | nM | 8.08 |
| CHEMBL32720 | — | Ki | = | 8.8 | nM | 8.06 |
| CHEMBL1743807 | — | Ki | = | 9.8 | nM | 8.01 |
| CHEMBL35492 | — | Ki | = | 9.8 | nM | 8.01 |
| CHEMBL1743793 | — | Ki | = | 10.1 | nM | 8.00 |
| CHEMBL1743819 | — | Ki | = | 10.1 | nM | 8.00 |
| CHEMBL287257 | DICLOFENSINE | Ki | = | 10.9 | nM | 7.96 |
| CHEMBL35184 | — | Ki | = | 11.3 | nM | 7.95 |
| CHEMBL35166 | — | Ki | = | 11.2 | nM | 7.95 |
| CHEMBL36030 | — | Ki | = | 12.3 | nM | 7.91 |
| CHEMBL34875 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL431299 | — | Ki | = | 15.8 | nM | 7.80 |
| CHEMBL1743803 | — | Ki | = | 17.5 | nM | 7.76 |
| CHEMBL34990 | — | Ki | = | 23.5 | nM | 7.63 |
| CHEMBL33246 | — | Ki | = | 24.5 | nM | 7.61 |
| CHEMBL33769 | — | Ki | = | 25.3 | nM | 7.60 |
| CHEMBL286849 | — | Ki | = | 25.7 | nM | 7.59 |
| CHEMBL1743791 | — | Ki | = | 26.5 | nM | 7.58 |
| CHEMBL285277 | — | Ki | = | 28.5 | nM | 7.54 |
| CHEMBL35071 | — | Ki | = | 30.8 | nM | 7.51 |
| CHEMBL1743817 | — | Ki | = | 32.6 | nM | 7.49 |
| CHEMBL1743803 | — | Ki | = | 35.9 | nM | 7.45 |
| CHEMBL286455 | — | Ki | = | 36.4 | nM | 7.44 |
| CHEMBL1743777 | — | Ki | = | 38.9 | nM | 7.41 |
| CHEMBL416959 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL285403 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL1743823 | — | Ki | = | 39.8 | nM | 7.40 |
| CHEMBL34990 | — | Ki | = | 41.2 | nM | 7.38 |
| CHEMBL1743765 | — | Ki | = | 43.7 | nM | 7.36 |
| CHEMBL1743799 | — | Ki | = | 43.5 | nM | 7.36 |
| CHEMBL1743781 | — | Ki | = | 44.8 | nM | 7.35 |
| CHEMBL286849 | — | Ki | = | 54.3 | nM | 7.26 |
| CHEMBL32270 | — | Ki | = | 65.1 | nM | 7.19 |