Assay Detail
Functional
CHEMBL890278
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Agonist activity at rat striatal tissue assessed as dopamine release
36
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Tissue | Striatum |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Structure-activity studies and analgesic efficacy of N-(3-pyridinyl)-bridged bicyclic diamines, exceptionally potent agonists at nicotinic acetylcholine receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 36 | 7.77 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL242910 | — | — | 4 | 9.10 |
| CHEMBL6623 | EPIBATIDINE | — | 2 | 9.08 |
| CHEMBL395804 | — | — | 4 | 8.80 |
| CHEMBL245243 | — | — | 4 | 8.60 |
| CHEMBL242487 | — | — | 4 | 8.42 |
| CHEMBL436827 | — | — | 4 | 8.24 |
| CHEMBL388699 | — | — | 2 | 7.80 |
| CHEMBL242864 | — | — | 4 | 7.70 |
| CHEMBL395323 | — | — | 2 | 7.52 |
| CHEMBL389964 | — | — | 2 | 6.86 |
| CHEMBL3 | NICOTINE | 4.0 | 2 | 6.70 |
| CHEMBL243344 | — | — | 2 | 6.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL242910 | — | EC50 | = | 0.7943 | nM | 9.10 |
| CHEMBL242910 | — | EC50 | = | 0.8 | nM | 9.10 |
| CHEMBL6623 | EPIBATIDINE | EC50 | = | 0.8318 | nM | 9.08 |
| CHEMBL6623 | EPIBATIDINE | EC50 | = | 0.83 | nM | 9.08 |
| CHEMBL395804 | — | EC50 | = | 1.6 | nM | 8.80 |
| CHEMBL245243 | — | EC50 | = | 2.512 | nM | 8.60 |
| CHEMBL245243 | — | EC50 | = | 2.5 | nM | 8.60 |
| CHEMBL242487 | — | EC50 | = | 3.802 | nM | 8.42 |
| CHEMBL242487 | — | EC50 | = | 3.8 | nM | 8.42 |
| CHEMBL245243 | — | EC50 | = | 5.248 | nM | 8.28 |
| CHEMBL245243 | — | EC50 | = | 5.3 | nM | 8.28 |
| CHEMBL436827 | — | EC50 | = | 5.7 | nM | 8.24 |
| CHEMBL436827 | — | EC50 | = | 5.754 | nM | 8.24 |
| CHEMBL388699 | — | EC50 | = | 16.0 | nM | 7.80 |
| CHEMBL388699 | — | EC50 | = | 16.22 | nM | 7.79 |
| CHEMBL395804 | — | EC50 | = | 19.05 | nM | 7.72 |
| CHEMBL395804 | — | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL242864 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL242864 | — | EC50 | = | 19.95 | nM | 7.70 |
| CHEMBL242910 | — | EC50 | = | 22.91 | nM | 7.64 |
| CHEMBL242910 | — | EC50 | = | 23.0 | nM | 7.64 |
| CHEMBL436827 | — | EC50 | = | 25.12 | nM | 7.60 |
| CHEMBL436827 | — | EC50 | = | 28.0 | nM | 7.55 |
| CHEMBL395323 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL395323 | — | EC50 | = | 30.2 | nM | 7.52 |
| CHEMBL242487 | — | EC50 | = | 50.12 | nM | 7.30 |
| CHEMBL242487 | — | EC50 | = | 51.0 | nM | 7.29 |
| CHEMBL242864 | — | EC50 | = | 81.0 | nM | 7.09 |
| CHEMBL242864 | — | EC50 | = | 81.28 | nM | 7.09 |
| CHEMBL389964 | — | EC50 | = | 138.0 | nM | 6.86 |
| CHEMBL389964 | — | EC50 | = | 138.04 | nM | 6.86 |
| CHEMBL395804 | — | EC50 | = | 199.53 | nM | 6.70 |
| CHEMBL3 | NICOTINE | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3 | NICOTINE | EC50 | = | 199.53 | nM | 6.70 |
| CHEMBL243344 | — | EC50 | = | 350.0 | nM | 6.46 |
| CHEMBL243344 | — | EC50 | = | 346.74 | nM | 6.46 |