Assay Detail
Binding
CHEMBL866004
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Agonist like activity at skeletal junction sarcoplasmic reticulum RyR1/FKBP12 complex assessed as increase in [3H]ryanodine binding
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Simplified cyclic analogues of bastadin-5. Structure-activity relationships for modulation of the RyR1/FKBP12 Ca2+ channel complex.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 13 | 4.83 | 5.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL439151 | BASTADIN 5 | — | 1 | 5.66 |
| CHEMBL377812 | — | — | 1 | 5.19 |
| CHEMBL386905 | — | — | 1 | 4.96 |
| CHEMBL209427 | — | — | 1 | 4.70 |
| CHEMBL212154 | — | — | 1 | 4.68 |
| CHEMBL386432 | — | — | 1 | 4.68 |
| CHEMBL376941 | — | — | 1 | 4.62 |
| CHEMBL378025 | — | — | 1 | 4.54 |
| CHEMBL213687 | — | — | 1 | 4.48 |
| CHEMBL377464 | — | — | 1 | - |
| CHEMBL377741 | — | — | 1 | - |
| CHEMBL210076 | — | — | 1 | - |
| CHEMBL380242 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL439151 | BASTADIN 5 | EC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL377812 | — | EC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL386905 | — | EC50 | = | 10900.0 | nM | 4.96 |
| CHEMBL209427 | — | EC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL212154 | — | EC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL386432 | — | EC50 | = | 20900.0 | nM | 4.68 |
| CHEMBL376941 | — | EC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL378025 | — | EC50 | = | 28600.0 | nM | 4.54 |
| CHEMBL213687 | — | EC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL377464 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL377741 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL210076 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL380242 | — | EC50 | > | 100000.0 | nM | - |