Assay Detail
Binding
CHEMBL866005
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Antagonist like activity at skeletal junction sarcoplasmic reticulum RyR1/FKBP12 complex assessed as decrease in [3H]ryanodine binding
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 0 — Uncurated / Unknown |
| 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 |
|---|---|---|---|
| IC50 | 3 | 4.58 | 5.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL213853 | — | — | 1 | 5.21 |
| CHEMBL209335 | — | — | 1 | 4.33 |
| CHEMBL379795 | — | — | 1 | 4.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL213853 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL209335 | — | IC50 | = | 47000.0 | nM | 4.33 |
| CHEMBL379795 | — | IC50 | = | 63000.0 | nM | 4.20 |