Assay Detail
Binding
CHEMBL2187477
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]nicotine from human alpha4beta2 nAChR expressed in human SH-EP1 cells
53
Total Activities
53
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | SH-EP1 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907589) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Structure-activity studies of 7-heteroaryl-3-azabicyclo[3.3.1]non-6-enes: a novel class of highly potent nicotinic receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 53 | 8.73 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2177537 | — | — | 1 | 10.00 |
| CHEMBL2177512 | — | — | 1 | 10.00 |
| CHEMBL2177536 | — | — | 1 | 9.70 |
| CHEMBL2177538 | — | — | 1 | 9.70 |
| CHEMBL2177552 | — | — | 1 | 9.70 |
| CHEMBL2177553 | — | — | 1 | 9.70 |
| CHEMBL2177518 | — | — | 1 | 9.70 |
| CHEMBL2177543 | — | — | 1 | 9.59 |
| CHEMBL2177535 | — | — | 1 | 9.52 |
| CHEMBL2177528 | — | — | 1 | 9.52 |
| CHEMBL2178156 | — | — | 1 | 9.52 |
| CHEMBL2177551 | — | — | 1 | 9.52 |
| CHEMBL2177541 | — | — | 1 | 9.52 |
| CHEMBL2177526 | — | — | 1 | 9.40 |
| CHEMBL2177522 | — | — | 1 | 9.40 |
| CHEMBL2177524 | — | — | 1 | 9.40 |
| CHEMBL2177555 | — | — | 1 | 9.40 |
| CHEMBL2177516 | — | — | 1 | 9.40 |
| CHEMBL2177549 | — | — | 1 | 9.40 |
| CHEMBL2177542 | — | — | 1 | 9.22 |
| CHEMBL2177514 | — | — | 1 | 9.22 |
| CHEMBL2178155 | — | — | 1 | 9.22 |
| CHEMBL2177545 | — | — | 1 | 9.15 |
| CHEMBL2177547 | — | — | 1 | 9.15 |
| CHEMBL2177533 | — | — | 1 | 9.15 |
| CHEMBL2177532 | — | — | 1 | 9.10 |
| CHEMBL2178160 | — | — | 1 | 9.05 |
| CHEMBL2178158 | — | — | 1 | 9.05 |
| CHEMBL2178157 | — | — | 1 | 9.00 |
| CHEMBL2177109 | — | — | 1 | 9.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2177537 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL2177512 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL2177538 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL2177552 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL2177553 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL2177518 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL2177536 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL2177543 | — | Ki | = | 0.26 | nM | 9.59 |
| CHEMBL2177535 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL2177528 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL2178156 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL2177551 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL2177541 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL2177516 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL2177522 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL2177524 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL2177555 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL2177526 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL2177549 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL2177542 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL2177514 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL2178155 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL2177545 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL2177547 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL2177533 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL2177532 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL2178158 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL2178160 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL2178157 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL2177109 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL2177517 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL2177546 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL2178159 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL2177548 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL2177513 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL2177540 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL2177544 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL2177521 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL2177530 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL2177550 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL2177539 | — | Ki | = | 9.4 | nM | 8.03 |
| CHEMBL2178154 | — | Ki | = | 9.6 | nM | 8.02 |
| CHEMBL2177554 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL2177523 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL2177525 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL2177534 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL132966 | RIVANICLINE | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL2177519 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL2177515 | — | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL2177529 | — | Ki | = | 105.0 | nM | 6.98 |