Assay Detail
Binding
CHEMBL4202175
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Antagonist activity at rat alpha3beta4 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
Neuronal acetylcholine receptor; alpha3/beta4 (CHEMBL1907593) ↗| 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 | 7.86 | 8.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4218406 | — | — | 1 | 8.72 |
| CHEMBL4214931 | — | — | 1 | 8.70 |
| CHEMBL3104245 | — | — | 1 | 8.44 |
| CHEMBL4214003 | — | — | 1 | 8.41 |
| CHEMBL4210514 | — | — | 1 | 8.27 |
| CHEMBL4215824 | — | — | 1 | 8.16 |
| CHEMBL4206670 | — | — | 1 | 8.13 |
| CHEMBL4215453 | — | — | 1 | 8.10 |
| CHEMBL4211045 | — | — | 1 | 8.00 |
| CHEMBL4206157 | — | — | 1 | 7.96 |
| CHEMBL4208491 | — | — | 1 | 7.28 |
| CHEMBL4203617 | — | — | 1 | 6.92 |
| CHEMBL4204149 | — | — | 1 | 6.50 |
| CHEMBL4203278 | — | — | 1 | 6.42 |
| CHEMBL4207977 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4218406 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL4214931 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3104245 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL4214003 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL4210514 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL4215824 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL4206670 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL4215453 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL4211045 | — | IC50 | = | 9.9 | nM | 8.00 |
| CHEMBL4206157 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4208491 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL4203617 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4204149 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL4203278 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL4207977 | — | IC50 | > | 10000.0 | nM | - |