Assay Detail
Binding
CHEMBL4202177
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at rat alpha6/alpha3beta4 nAChR nACHR expressed in Xenopus laevis oocytes assessed as inhibition of acetyl choline-induced membrane currents pre-incubated for 5 mins prior to acetyl choline pulse at -70 mV potential by two-electrode voltage clamp assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 7 — Homologous single protein target |
| Curated By | Intermediate |
Target
Nicotinic acetylcholine receptor alpha6/alpha3/beta4 (CHEMBL3137276) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Single Amino Acid Substitution in α-Conotoxin TxID Reveals a Specific α3β4 Nicotinic Acetylcholine Receptor Antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 7.26 | 8.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4218406 | — | — | 1 | 8.21 |
| CHEMBL4206157 | — | — | 1 | 8.00 |
| CHEMBL4214931 | — | — | 1 | 7.72 |
| CHEMBL4211045 | — | — | 1 | 7.68 |
| CHEMBL4215453 | — | — | 1 | 7.64 |
| CHEMBL3104245 | — | — | 1 | 7.47 |
| CHEMBL4206670 | — | — | 1 | 7.30 |
| CHEMBL4214003 | — | — | 1 | 6.75 |
| CHEMBL4210514 | — | — | 1 | 6.46 |
| CHEMBL4208491 | — | — | 1 | 6.37 |
| CHEMBL4203617 | — | — | 1 | 6.30 |
| CHEMBL4203278 | — | — | 1 | - |
| CHEMBL4215824 | — | — | 1 | - |
| CHEMBL4204149 | — | — | 1 | - |
| CHEMBL4207977 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4218406 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL4206157 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4214931 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4211045 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4215453 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3104245 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL4206670 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4214003 | — | IC50 | = | 178.0 | nM | 6.75 |
| CHEMBL4210514 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL4208491 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL4203617 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4203278 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4215824 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4204149 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4207977 | — | IC50 | > | 10000.0 | nM | - |