Assay Detail
Binding
CHEMBL5034632
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human alpha9alpha10 nAChR expressed in Xenopus laevis oocytes assessed as inhibition of acetylcholine-induced current response by two-electrode voltage-clamp method
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Oocyte |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha9/alpha10 (CHEMBL2109238) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Discovery of Methylene Thioacetal-Incorporated α-RgIA Analogues as Potent and Stable Antagonists of the Human α9α10 Nicotinic Acetylcholine Receptor for the Treatment of Neuropathic Pain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 8.04 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5086734 | — | — | 1 | 9.30 |
| CHEMBL5090753 | — | — | 1 | 9.05 |
| CHEMBL5089881 | — | — | 1 | 8.82 |
| CHEMBL5073182 | — | — | 1 | 8.54 |
| CHEMBL5080428 | — | — | 1 | 8.21 |
| CHEMBL1836968 | — | — | 1 | 6.29 |
| CHEMBL5091401 | — | — | 1 | 6.05 |
| CHEMBL5090616 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5086734 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL5090753 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL5089881 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL5073182 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL5080428 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL1836968 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL5091401 | — | IC50 | = | 882.0 | nM | 6.05 |
| CHEMBL5090616 | — | IC50 | > | 1000.0 | nM | - |