Assay Detail
Binding
CHEMBL802855
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Inhibition of uptake of tritiated norepinephrine (NE) in rat synaptosomes
90
Total Activities
82
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Pyrroloisoquinoline antidepressants. 2. In-depth exploration of structure-activity relationships.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 90 | 8.05 | 9.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1743782 | — | — | 1 | 9.80 |
| CHEMBL1743810 | — | — | 1 | 9.70 |
| CHEMBL35184 | — | — | 3 | 9.43 |
| CHEMBL1743790 | — | — | 1 | 9.35 |
| CHEMBL1743798 | — | — | 1 | 9.26 |
| CHEMBL1743786 | — | — | 1 | 9.21 |
| CHEMBL431299 | — | — | 1 | 9.19 |
| CHEMBL72 | DESIPRAMINE | 4.0 | 1 | 9.19 |
| CHEMBL287474 | — | — | 1 | 9.17 |
| CHEMBL1743785 | — | — | 1 | 9.13 |
| CHEMBL1743794 | — | — | 1 | 9.10 |
| CHEMBL1743819 | — | — | 1 | 9.09 |
| CHEMBL1743793 | — | — | 1 | 9.07 |
| CHEMBL286312 | — | — | 1 | 9.03 |
| CHEMBL286849 | — | — | 3 | 9.02 |
| CHEMBL1743803 | — | — | 3 | 8.96 |
| CHEMBL1743824 | — | — | 1 | 8.90 |
| CHEMBL287859 | — | — | 1 | 8.85 |
| CHEMBL1743767 | — | — | 1 | 8.85 |
| CHEMBL1743791 | — | — | 1 | 8.82 |
| CHEMBL34990 | — | — | 3 | 8.74 |
| CHEMBL32726 | — | — | 1 | 8.66 |
| CHEMBL1743805 | — | — | 1 | 8.64 |
| CHEMBL35166 | — | — | 1 | 8.51 |
| CHEMBL35013 | — | — | 1 | 8.49 |
| CHEMBL284981 | — | — | 1 | 8.48 |
| CHEMBL1743812 | — | — | 1 | 8.47 |
| CHEMBL1743820 | — | — | 1 | 8.47 |
| CHEMBL273575 | NOMIFENSINE | 4.0 | 1 | 8.42 |
| CHEMBL32797 | — | — | 1 | 8.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1743782 | — | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL1743810 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL35184 | — | Ki | = | 0.37 | nM | 9.43 |
| CHEMBL1743790 | — | Ki | = | 0.45 | nM | 9.35 |
| CHEMBL1743798 | — | Ki | = | 0.55 | nM | 9.26 |
| CHEMBL35184 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL1743786 | — | Ki | = | 0.62 | nM | 9.21 |
| CHEMBL431299 | — | Ki | = | 0.65 | nM | 9.19 |
| CHEMBL72 | DESIPRAMINE | Ki | = | 0.65 | nM | 9.19 |
| CHEMBL287474 | — | Ki | = | 0.68 | nM | 9.17 |
| CHEMBL1743785 | — | Ki | = | 0.74 | nM | 9.13 |
| CHEMBL1743794 | — | Ki | = | 0.79 | nM | 9.10 |
| CHEMBL1743819 | — | Ki | = | 0.81 | nM | 9.09 |
| CHEMBL1743793 | — | Ki | = | 0.85 | nM | 9.07 |
| CHEMBL286312 | — | Ki | = | 0.94 | nM | 9.03 |
| CHEMBL286849 | — | Ki | = | 0.95 | nM | 9.02 |
| CHEMBL1743803 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL1743824 | — | Ki | = | 1.25 | nM | 8.90 |
| CHEMBL1743767 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL287859 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL286849 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL1743791 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL34990 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL1743803 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL32726 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL1743805 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL34990 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL35166 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL35013 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL284981 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL1743820 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL1743812 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL273575 | NOMIFENSINE | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL32797 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL416777 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL431898 | — | Ki | = | 5.6 | nM | 8.25 |
| CHEMBL286455 | — | Ki | = | 5.6 | nM | 8.25 |
| CHEMBL284367 | — | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL1743807 | — | Ki | = | 7.5 | nM | 8.12 |
| CHEMBL285277 | — | Ki | = | 8.1 | nM | 8.09 |
| CHEMBL1743778 | — | Ki | = | 8.8 | nM | 8.06 |
| CHEMBL287257 | DICLOFENSINE | Ki | = | 8.8 | nM | 8.06 |
| CHEMBL1743799 | — | Ki | = | 10.5 | nM | 7.98 |
| CHEMBL36064 | — | Ki | = | 10.5 | nM | 7.98 |
| CHEMBL33364 | — | Ki | = | 10.6 | nM | 7.97 |
| CHEMBL36030 | — | Ki | = | 11.5 | nM | 7.94 |
| CHEMBL33769 | — | Ki | = | 11.6 | nM | 7.94 |
| CHEMBL32209 | — | Ki | = | 11.5 | nM | 7.94 |
| CHEMBL11 | IMIPRAMINE | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL35441 | — | Ki | = | 13.8 | nM | 7.86 |