Assay Detail
Binding
CHEMBL1120675
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Displacement of [3H]epibatidine from rat alpha4beta2 nAChR
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907596) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
In silico characterization of cytisinoids docked into an acetylcholine binding protein.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 7.57 | 9.61 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL187394 | — | — | 1 | 9.61 |
| CHEMBL365956 | — | — | 1 | 9.51 |
| CHEMBL497939 | CYTISINICLINE | 3.0 | 1 | 7.16 |
| CHEMBL1083905 | — | — | 1 | 6.99 |
| CHEMBL1085045 | — | — | 1 | 6.95 |
| CHEMBL1084011 | — | — | 1 | 6.43 |
| CHEMBL1084012 | — | — | 1 | 6.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL187394 | — | IC50 | = | 0.2455 | nM | 9.61 |
| CHEMBL365956 | — | IC50 | = | 0.309 | nM | 9.51 |
| CHEMBL497939 | CYTISINICLINE | IC50 | = | 69.18 | nM | 7.16 |
| CHEMBL1083905 | — | IC50 | = | 102.33 | nM | 6.99 |
| CHEMBL1085045 | — | IC50 | = | 112.2 | nM | 6.95 |
| CHEMBL1084011 | — | IC50 | = | 371.54 | nM | 6.43 |
| CHEMBL1084012 | — | IC50 | = | 457.09 | nM | 6.34 |