Assay Detail
Functional
CHEMBL953564
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human recombinant alpha7 nAChR expressed in rat GH3 cells by calcium influx assay
61
Total Activities
31
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | GH3 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor subunit alpha-7 (CHEMBL2492) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Gamma-lactams--a novel scaffold for highly potent and selective alpha 7 nicotinic acetylcholine receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 31 | 6.60 | 8.10 |
| Emax | 30 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL459900 | — | — | 2 | 8.10 |
| CHEMBL459689 | — | — | 2 | 8.10 |
| CHEMBL503427 | — | — | 2 | 8.10 |
| CHEMBL454407 | — | — | 2 | 8.00 |
| CHEMBL459904 | — | — | 2 | 7.80 |
| CHEMBL503573 | — | — | 2 | 7.60 |
| CHEMBL516818 | — | — | 2 | 7.60 |
| CHEMBL462449 | — | — | 2 | 7.50 |
| CHEMBL298517 | (+)-EPIBATIDINE | — | 2 | 7.40 |
| CHEMBL499536 | — | — | 1 | 7.00 |
| CHEMBL462236 | — | — | 2 | 6.90 |
| CHEMBL460541 | — | — | 2 | 6.50 |
| CHEMBL462235 | — | — | 2 | 6.50 |
| CHEMBL517411 | — | — | 2 | 6.50 |
| CHEMBL193016 | — | — | 2 | 6.40 |
| CHEMBL512768 | — | — | 2 | 6.20 |
| CHEMBL459903 | — | — | 2 | 6.20 |
| CHEMBL459475 | — | — | 2 | 6.20 |
| CHEMBL452455 | — | — | 2 | 6.20 |
| CHEMBL490959 | — | — | 2 | 6.10 |
| CHEMBL503637 | — | — | 2 | 6.00 |
| CHEMBL465540 | — | — | 2 | 6.00 |
| CHEMBL516658 | — | — | 2 | 5.90 |
| CHEMBL491495 | — | — | 2 | 5.90 |
| CHEMBL447505 | — | — | 2 | 5.90 |
| CHEMBL491494 | — | — | 2 | 5.90 |
| CHEMBL522965 | — | — | 2 | 5.90 |
| CHEMBL3 | NICOTINE | 4.0 | 2 | 5.80 |
| CHEMBL523647 | — | — | 2 | 5.70 |
| CHEMBL134713 | GTS-21 | 2.0 | 2 | 5.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL459689 | — | EC50 | = | 7.943 | nM | 8.10 |
| CHEMBL459900 | — | EC50 | = | 7.943 | nM | 8.10 |
| CHEMBL503427 | — | EC50 | = | 7.943 | nM | 8.10 |
| CHEMBL454407 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL459904 | — | EC50 | = | 15.85 | nM | 7.80 |
| CHEMBL503573 | — | EC50 | = | 25.12 | nM | 7.60 |
| CHEMBL516818 | — | EC50 | = | 25.12 | nM | 7.60 |
| CHEMBL462449 | — | EC50 | = | 31.62 | nM | 7.50 |
| CHEMBL298517 | (+)-EPIBATIDINE | EC50 | = | 39.81 | nM | 7.40 |
| CHEMBL499536 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL462236 | — | EC50 | = | 125.89 | nM | 6.90 |
| CHEMBL460541 | — | EC50 | = | 316.23 | nM | 6.50 |
| CHEMBL462235 | — | EC50 | = | 316.23 | nM | 6.50 |
| CHEMBL517411 | — | EC50 | = | 316.23 | nM | 6.50 |
| CHEMBL193016 | — | EC50 | = | 398.11 | nM | 6.40 |
| CHEMBL512768 | — | EC50 | = | 630.96 | nM | 6.20 |
| CHEMBL452455 | — | EC50 | = | 630.96 | nM | 6.20 |
| CHEMBL459475 | — | EC50 | = | 630.96 | nM | 6.20 |
| CHEMBL459903 | — | EC50 | = | 630.96 | nM | 6.20 |
| CHEMBL490959 | — | EC50 | = | 794.33 | nM | 6.10 |
| CHEMBL503637 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL465540 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL522965 | — | EC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL491494 | — | EC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL491495 | — | EC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL516658 | — | EC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL447505 | — | EC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL3 | NICOTINE | EC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL134713 | GTS-21 | EC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL523647 | — | EC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL490958 | — | EC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL503637 | — | Emax | = | 110.0 | % | - |
| CHEMBL452455 | — | Emax | = | 89.0 | % | - |
| CHEMBL512768 | — | Emax | = | 114.0 | % | - |
| CHEMBL517411 | — | Emax | = | 60.0 | % | - |
| CHEMBL459900 | — | Emax | = | 90.0 | % | - |
| CHEMBL459689 | — | Emax | = | 100.0 | % | - |
| CHEMBL454407 | — | Emax | = | 104.0 | % | - |
| CHEMBL459904 | — | Emax | = | 83.0 | % | - |
| CHEMBL503573 | — | Emax | = | 89.0 | % | - |
| CHEMBL459903 | — | Emax | = | 47.0 | % | - |
| CHEMBL447505 | — | Emax | = | 61.0 | % | - |
| CHEMBL459475 | — | Emax | = | 81.0 | % | - |
| CHEMBL462449 | — | Emax | = | 79.0 | % | - |
| CHEMBL516818 | — | Emax | = | 89.0 | % | - |
| CHEMBL462236 | — | Emax | = | 62.0 | % | - |
| CHEMBL462235 | — | Emax | = | 47.0 | % | - |
| CHEMBL516658 | — | Emax | = | 61.0 | % | - |
| CHEMBL503427 | — | Emax | = | 80.0 | % | - |
| CHEMBL460541 | — | Emax | = | 28.0 | % | - |