Assay Detail
Binding
CHEMBL2187475
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]epibatidine from human alpha3beta4 nAChR expressed in human SH-SY5Y cells
53
Total Activities
53
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | SH-SY5Y |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha3/beta4 (CHEMBL1907594) ↗| 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 | 7.05 | 8.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2177545 | — | — | 1 | 8.72 |
| CHEMBL2177538 | — | — | 1 | 8.40 |
| CHEMBL2177543 | — | — | 1 | 8.32 |
| CHEMBL2177553 | — | — | 1 | 8.27 |
| CHEMBL2177524 | — | — | 1 | 8.21 |
| CHEMBL2177512 | — | — | 1 | 8.18 |
| CHEMBL2177549 | — | — | 1 | 8.15 |
| CHEMBL2177546 | — | — | 1 | 8.09 |
| CHEMBL2177552 | — | — | 1 | 8.08 |
| CHEMBL2177536 | — | — | 1 | 7.92 |
| CHEMBL2177541 | — | — | 1 | 7.84 |
| CHEMBL2178160 | — | — | 1 | 7.82 |
| CHEMBL2178156 | — | — | 1 | 7.82 |
| CHEMBL2177535 | — | — | 1 | 7.77 |
| CHEMBL2177532 | — | — | 1 | 7.77 |
| CHEMBL2178157 | — | — | 1 | 7.66 |
| CHEMBL2177537 | — | — | 1 | 7.64 |
| CHEMBL2177528 | — | — | 1 | 7.60 |
| CHEMBL2178158 | — | — | 1 | 7.58 |
| CHEMBL2178159 | — | — | 1 | 7.57 |
| CHEMBL2177522 | — | — | 1 | 7.55 |
| CHEMBL2177514 | — | — | 1 | 7.51 |
| CHEMBL2177551 | — | — | 1 | 7.41 |
| CHEMBL2177513 | — | — | 1 | 7.40 |
| CHEMBL2177555 | — | — | 1 | 7.40 |
| CHEMBL2177547 | — | — | 1 | 7.36 |
| CHEMBL2178155 | — | — | 1 | 7.33 |
| CHEMBL2177109 | — | — | 1 | 7.25 |
| CHEMBL2177518 | — | — | 1 | 7.24 |
| CHEMBL2177516 | — | — | 1 | 7.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2177545 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL2177538 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL2177543 | — | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL2177553 | — | Ki | = | 5.4 | nM | 8.27 |
| CHEMBL2177524 | — | Ki | = | 6.2 | nM | 8.21 |
| CHEMBL2177512 | — | Ki | = | 6.6 | nM | 8.18 |
| CHEMBL2177549 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL2177546 | — | Ki | = | 8.2 | nM | 8.09 |
| CHEMBL2177552 | — | Ki | = | 8.3 | nM | 8.08 |
| CHEMBL2177536 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL2177541 | — | Ki | = | 14.3 | nM | 7.84 |
| CHEMBL2178160 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL2178156 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL2177532 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL2177535 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL2178157 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL2177537 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL2177528 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL2178158 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL2178159 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL2177522 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL2177514 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL2177551 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL2177513 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL2177555 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL2177547 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL2178155 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL2177109 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL2177518 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL2177516 | — | Ki | = | 73.0 | nM | 7.14 |
| CHEMBL2177533 | — | Ki | = | 79.0 | nM | 7.10 |
| CHEMBL2177521 | — | Ki | = | 103.0 | nM | 6.99 |
| CHEMBL2177530 | — | Ki | = | 128.0 | nM | 6.89 |
| CHEMBL2177526 | — | Ki | = | 328.0 | nM | 6.48 |
| CHEMBL2177519 | — | Ki | = | 459.0 | nM | 6.34 |
| CHEMBL2177529 | — | Ki | = | 507.0 | nM | 6.29 |
| CHEMBL2177540 | — | Ki | = | 534.0 | nM | 6.27 |
| CHEMBL2177542 | — | Ki | = | 596.0 | nM | 6.22 |
| CHEMBL2177548 | — | Ki | = | 711.0 | nM | 6.15 |
| CHEMBL2177517 | — | Ki | = | 828.0 | nM | 6.08 |
| CHEMBL2177525 | — | Ki | = | 986.0 | nM | 6.01 |
| CHEMBL2177523 | — | Ki | = | 1305.0 | nM | 5.88 |
| CHEMBL2177550 | — | Ki | = | 1431.0 | nM | 5.84 |
| CHEMBL2177554 | — | Ki | = | 1639.0 | nM | 5.79 |
| CHEMBL2177544 | — | Ki | = | 1726.0 | nM | 5.76 |
| CHEMBL2177539 | — | Ki | = | 1796.0 | nM | 5.75 |
| CHEMBL2178154 | — | Ki | = | 1831.0 | nM | 5.74 |
| CHEMBL2177534 | — | Ki | = | 4502.0 | nM | 5.35 |
| CHEMBL132966 | RIVANICLINE | Ki | = | 5400.0 | nM | 5.27 |
| CHEMBL2177515 | — | Ki | = | 5736.0 | nM | 5.24 |