Assay Detail
Binding
CHEMBL632853
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Ability to enhance the binding of (+/-)-[3H]nicotine to the rat brain P2 fraction at binding site 2
32
Total Activities
29
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 | 32 | 5.87 | 11.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3 | NICOTINE | 4.0 | 2 | 11.00 |
| CHEMBL15732 | — | — | 1 | 7.30 |
| CHEMBL15487 | PIPERIDINE | -1.0 | 1 | 6.92 |
| CHEMBL21824 | — | — | 1 | 5.77 |
| CHEMBL25053 | — | — | 1 | 5.48 |
| CHEMBL23025 | — | — | 1 | 5.02 |
| CHEMBL22830 | PYRROLIDINE | — | 3 | 4.60 |
| CHEMBL665 | N-METHYL PYRROLIDINE (NMP) | — | 1 | 4.28 |
| CHEMBL22977 | — | — | 1 | 4.06 |
| CHEMBL21867 | — | — | 1 | 4.01 |
| CHEMBL279305 | — | — | 1 | 4.00 |
| CHEMBL662 | — | — | 1 | - |
| CHEMBL284022 | — | — | 1 | - |
| CHEMBL279512 | — | — | 1 | - |
| CHEMBL22463 | — | — | 1 | - |
| CHEMBL22976 | — | — | 1 | - |
| CHEMBL25541 | — | — | 1 | - |
| CHEMBL277887 | — | — | 1 | - |
| CHEMBL266158 | PYRIDINE | — | 1 | - |
| CHEMBL21619 | 2-AMINOPYRIDINE | — | 1 | - |
| CHEMBL664 | — | — | 1 | - |
| CHEMBL21531 | — | — | 1 | - |
| CHEMBL281417 | N-METHYLPIPERIDINE | — | 1 | - |
| CHEMBL21533 | — | — | 1 | - |
| CHEMBL21454 | — | — | 1 | - |
| CHEMBL22270 | — | — | 1 | - |
| CHEMBL22332 | — | — | 1 | - |
| CHEMBL280963 | DL-ANABASINE | — | 1 | - |
| CHEMBL15544 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3 | NICOTINE | Kd | = | 0.01 | nM | 11.00 |
| CHEMBL3 | NICOTINE | Kd | = | 10.0 | nM | 8.00 |
| CHEMBL15732 | — | Kd | = | 50.0 | nM | 7.30 |
| CHEMBL15487 | PIPERIDINE | Kd | = | 120.0 | nM | 6.92 |
| CHEMBL21824 | — | Kd | = | 1700.0 | nM | 5.77 |
| CHEMBL25053 | — | Kd | = | 3300.0 | nM | 5.48 |
| CHEMBL23025 | — | Kd | = | 9500.0 | nM | 5.02 |
| CHEMBL22830 | PYRROLIDINE | Kd | = | 25000.0 | nM | 4.60 |
| CHEMBL665 | N-METHYL PYRROLIDINE (NMP) | Kd | = | 52000.0 | nM | 4.28 |
| CHEMBL22977 | — | Kd | = | 87000.0 | nM | 4.06 |
| CHEMBL21867 | — | Kd | = | 97000.0 | nM | 4.01 |
| CHEMBL279305 | — | Kd | = | 100000.0 | nM | 4.00 |
| CHEMBL21619 | 2-AMINOPYRIDINE | Kd | = | 200000.0 | nM | - |
| CHEMBL25541 | — | Kd | = | 380000.0 | nM | - |
| CHEMBL22463 | — | Kd | = | 820000.0 | nM | - |
| CHEMBL284022 | — | Kd | = | 3000000.0 | nM | - |
| CHEMBL664 | — | Kd | = | 4700000.0 | nM | - |
| CHEMBL662 | — | Kd | = | 880000.0 | nM | - |
| CHEMBL279512 | — | Kd | = | 890000.0 | nM | - |
| CHEMBL22976 | — | Kd | = | 10000000.0 | nM | - |
| CHEMBL22830 | PYRROLIDINE | Kd | = | 330000.0 | nM | - |
| CHEMBL22830 | PYRROLIDINE | Kd | = | 41000000.0 | nM | - |
| CHEMBL277887 | — | Kd | = | 6000000.0 | nM | - |
| CHEMBL266158 | PYRIDINE | Kd | = | 3300000.0 | nM | - |
| CHEMBL22332 | — | Kd | = | 3400000.0 | nM | - |
| CHEMBL22270 | — | Kd | = | 7900000.0 | nM | - |
| CHEMBL21454 | — | Kd | = | 3200000.0 | nM | - |
| CHEMBL281417 | N-METHYLPIPERIDINE | Kd | = | 1200000.0 | nM | - |
| CHEMBL21531 | — | Kd | = | 2700000.0 | nM | - |
| CHEMBL15544 | — | Kd | = | 2200000.0 | nM | - |
| CHEMBL280963 | DL-ANABASINE | Kd | = | 1300000.0 | nM | - |
| CHEMBL21533 | — | Kd | = | 3900000.0 | nM | - |