Assay Detail
Functional
CHEMBL753100
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Antagonist activity against Nicotinic acetylcholine receptor (nAChR) of isolated Frog rectus Abdominis Muscle
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | frog |
| Tissue | Rectus abdominis muscle |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Expert |
Publication
Structure-activity relationships of methoctramine-related polyamines as muscular nicotinic receptor noncompetitive antagonists. 3. Effect of inserting the tetraamine backbone into a macrocyclic structure.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 6.31 | 7.02 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL55587 | — | — | 1 | 7.02 |
| CHEMBL323655 | — | — | 1 | 6.80 |
| CHEMBL324975 | — | — | 1 | 6.77 |
| CHEMBL430708 | — | — | 1 | 6.72 |
| CHEMBL110308 | — | — | 1 | 6.64 |
| CHEMBL325740 | — | — | 1 | 6.62 |
| CHEMBL111404 | — | — | 1 | 6.49 |
| CHEMBL326532 | — | — | 1 | 6.48 |
| CHEMBL324001 | — | — | 1 | 6.35 |
| CHEMBL300930 | — | — | 1 | 6.30 |
| CHEMBL110045 | — | — | 1 | 6.28 |
| CHEMBL327100 | — | — | 1 | 6.23 |
| CHEMBL325505 | — | — | 1 | 6.15 |
| CHEMBL298833 | TRIPHENYLMETHYLPHOSPHONIUM BROMIDE | — | 1 | 6.05 |
| CHEMBL27673 | METHOCTRAMINE | — | 1 | 5.93 |
| CHEMBL111324 | — | — | 1 | 5.92 |
| CHEMBL325994 | — | — | 1 | 5.46 |
| CHEMBL322731 | — | — | 1 | 5.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL55587 | — | IC50 | = | 95.5 | nM | 7.02 |
| CHEMBL323655 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL324975 | — | IC50 | = | 169.82 | nM | 6.77 |
| CHEMBL430708 | — | IC50 | = | 190.55 | nM | 6.72 |
| CHEMBL110308 | — | IC50 | = | 229.09 | nM | 6.64 |
| CHEMBL325740 | — | IC50 | = | 239.88 | nM | 6.62 |
| CHEMBL111404 | — | IC50 | = | 323.59 | nM | 6.49 |
| CHEMBL326532 | — | IC50 | = | 331.13 | nM | 6.48 |
| CHEMBL324001 | — | IC50 | = | 446.68 | nM | 6.35 |
| CHEMBL300930 | — | IC50 | = | 501.19 | nM | 6.30 |
| CHEMBL110045 | — | IC50 | = | 524.81 | nM | 6.28 |
| CHEMBL327100 | — | IC50 | = | 588.84 | nM | 6.23 |
| CHEMBL325505 | — | IC50 | = | 707.95 | nM | 6.15 |
| CHEMBL298833 | TRIPHENYLMETHYLPHOSPHONIUM BROMIDE | IC50 | = | 891.25 | nM | 6.05 |
| CHEMBL27673 | METHOCTRAMINE | IC50 | = | 1174.9 | nM | 5.93 |
| CHEMBL111324 | — | IC50 | = | 1202.26 | nM | 5.92 |
| CHEMBL325994 | — | IC50 | = | 3467.37 | nM | 5.46 |
| CHEMBL322731 | — | IC50 | = | 4265.8 | nM | 5.37 |