Assay Detail
Binding
CHEMBL636099
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Ability to enhance the binding of (+/-)-[3H]nicotine to the rat brain P2 fraction at binding site 3.
17
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor (CHEMBL2094110) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Structure-activity relationships of some pyridine, piperidine, and pyrrolidine analogues for enhancing and inhibiting the binding of (+/-)-[3H]nicotine to the rat brain P2 preparation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 17 | 6.27 | 8.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3 | NICOTINE | 4.0 | 2 | 8.28 |
| CHEMBL15487 | PIPERIDINE | -1.0 | 1 | 4.16 |
| CHEMBL665 | N-METHYL PYRROLIDINE (NMP) | — | 1 | - |
| CHEMBL25053 | — | — | 1 | - |
| CHEMBL21619 | 2-AMINOPYRIDINE | — | 1 | - |
| CHEMBL25541 | — | — | 1 | - |
| CHEMBL284022 | — | — | 1 | - |
| CHEMBL662 | — | — | 1 | - |
| CHEMBL23025 | — | — | 1 | - |
| CHEMBL21824 | — | — | 1 | - |
| CHEMBL277887 | — | — | 1 | - |
| CHEMBL266158 | PYRIDINE | — | 1 | - |
| CHEMBL15732 | — | — | 1 | - |
| CHEMBL21531 | — | — | 1 | - |
| CHEMBL21867 | — | — | 1 | - |
| CHEMBL22977 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3 | NICOTINE | Kd | = | 5.2 | nM | 8.28 |
| CHEMBL3 | NICOTINE | Kd | = | 430.0 | nM | 6.37 |
| CHEMBL15487 | PIPERIDINE | Kd | = | 69000.0 | nM | 4.16 |
| CHEMBL25053 | — | Kd | = | 2100000000.0 | nM | - |
| CHEMBL21619 | 2-AMINOPYRIDINE | Kd | = | 34000000.0 | nM | - |
| CHEMBL25541 | — | Kd | = | 22000000.0 | nM | - |
| CHEMBL284022 | — | Kd | = | 320000000.0 | nM | - |
| CHEMBL662 | — | Kd | = | 160000000.0 | nM | - |
| CHEMBL23025 | — | Kd | = | 2800000.0 | nM | - |
| CHEMBL21824 | — | Kd | = | 370000.0 | nM | - |
| CHEMBL277887 | — | Kd | = | 57000000.0 | nM | - |
| CHEMBL266158 | PYRIDINE | Kd | = | 86000000.0 | nM | - |
| CHEMBL15732 | — | Kd | = | 890000.0 | nM | - |
| CHEMBL21531 | — | Kd | = | 160000000.0 | nM | - |
| CHEMBL21867 | — | Kd | = | 980000.0 | nM | - |
| CHEMBL665 | N-METHYL PYRROLIDINE (NMP) | Kd | = | 590000.0 | nM | - |
| CHEMBL22977 | — | Kd | = | 1500000.0 | nM | - |