Assay Detail
Functional
CHEMBL1763282
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at alpha7 nAChR expressed in Xenopus oocyte assessed as inhibition of ACh-gated current by voltage clamp electrophysiology assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor subunit alpha-7 (CHEMBL2492) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of non-peptide, small molecule antagonists of α9α10 nicotinic acetylcholine receptors as novel analgesics for the treatment of neuropathic and tonic inflammatory pain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 6.57 | 8.06 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL267841 | — | — | 1 | 8.06 |
| CHEMBL241120 | — | — | 1 | 7.04 |
| CHEMBL454767 | — | — | 1 | 7.00 |
| CHEMBL268074 | — | — | 1 | 6.77 |
| CHEMBL451442 | — | — | 1 | 6.73 |
| CHEMBL1761821 | — | — | 1 | 5.92 |
| CHEMBL599735 | — | — | 1 | 5.82 |
| CHEMBL238979 | — | — | 1 | 5.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL267841 | — | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL241120 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL454767 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL268074 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL451442 | — | IC50 | = | 185.0 | nM | 6.73 |
| CHEMBL1761821 | — | IC50 | = | 1190.0 | nM | 5.92 |
| CHEMBL599735 | — | IC50 | = | 1510.0 | nM | 5.82 |
| CHEMBL238979 | — | IC50 | = | 6010.0 | nM | 5.22 |