Assay Detail
Binding
CHEMBL745919
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity against Muscarinic receptor from rat brain membranes using [3H]pirenzepine
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Muscarinic acetylcholine receptor M1 (CHEMBL276) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis and biological evaluation of tropane-like 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine (GBR 12909) analogues.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 6.68 | 9.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1201203 | BENZTROPINE | 4.0 | 1 | 9.23 |
| CHEMBL3084922 | — | — | 1 | 7.25 |
| CHEMBL3084920 | — | — | 1 | 7.11 |
| CHEMBL130643 | — | — | 1 | 7.03 |
| CHEMBL126235 | — | — | 1 | 6.89 |
| CHEMBL3084919 | — | — | 1 | 6.77 |
| CHEMBL129193 | — | — | 1 | 6.70 |
| CHEMBL126735 | — | — | 1 | 6.47 |
| CHEMBL3084921 | — | — | 1 | 6.20 |
| CHEMBL3084918 | — | — | 1 | 5.92 |
| CHEMBL127053 | — | — | 1 | 5.92 |
| CHEMBL415721 | — | — | 1 | 5.77 |
| CHEMBL339614 | — | — | 1 | 5.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1201203 | BENZTROPINE | Ki | = | 0.59 | nM | 9.23 |
| CHEMBL3084922 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL3084920 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL130643 | — | Ki | = | 94.0 | nM | 7.03 |
| CHEMBL126235 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL3084919 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL129193 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL126735 | — | Ki | = | 340.0 | nM | 6.47 |
| CHEMBL3084921 | — | Ki | = | 630.0 | nM | 6.20 |
| CHEMBL3084918 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL127053 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL415721 | — | Ki | = | 1700.0 | nM | 5.77 |
| CHEMBL339614 | — | Ki | = | 2500.0 | nM | 5.60 |