Assay Detail
Functional
CHEMBL1648232
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at alpha6 nAChR in rat striatum assessed as inhibition of nicotine-induced [3H]dopamine release
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Tissue | Striatum |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor subunit alpha-6 (CHEMBL4747) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Novel bis-, tris-, and tetrakis-tertiary amino analogs as antagonists at neuronal nicotinic receptors that mediate nicotine-evoked dopamine release.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.96 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL239844 | — | — | 1 | 9.70 |
| CHEMBL1643948 | — | — | 1 | 9.46 |
| CHEMBL1643941 | — | — | 1 | 9.02 |
| CHEMBL54331 | — | — | 1 | 8.70 |
| CHEMBL451671 | — | — | 1 | 8.52 |
| CHEMBL1643942 | — | — | 1 | 8.49 |
| CHEMBL1643946 | — | — | 1 | 8.07 |
| CHEMBL1643947 | — | — | 1 | 8.00 |
| CHEMBL1643950 | — | — | 1 | 7.52 |
| CHEMBL1643940 | — | — | 1 | 7.43 |
| CHEMBL105537 | — | — | 1 | 7.40 |
| CHEMBL499947 | — | — | 1 | 7.25 |
| CHEMBL1643943 | — | — | 1 | 7.20 |
| CHEMBL1643944 | — | — | 1 | 7.16 |
| CHEMBL1643939 | — | — | 1 | 6.75 |
| CHEMBL1643949 | — | — | 1 | 6.69 |
| CHEMBL1643945 | — | — | 1 | - |
| CHEMBL241120 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL239844 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL1643948 | — | IC50 | = | 0.35 | nM | 9.46 |
| CHEMBL1643941 | — | IC50 | = | 0.95 | nM | 9.02 |
| CHEMBL54331 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL451671 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1643942 | — | IC50 | = | 3.22 | nM | 8.49 |
| CHEMBL1643946 | — | IC50 | = | 8.59 | nM | 8.07 |
| CHEMBL1643947 | — | IC50 | = | 9.91 | nM | 8.00 |
| CHEMBL1643950 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL1643940 | — | IC50 | = | 37.4 | nM | 7.43 |
| CHEMBL105537 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL499947 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL1643943 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL1643944 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL1643939 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL1643949 | — | IC50 | = | 205.0 | nM | 6.69 |
| CHEMBL1643945 | — | IC50 | - | — | - | |
| CHEMBL241120 | — | IC50 | - | — | - |