Assay Detail
Binding
CHEMBL4729685
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human N type calcium channel Cav2.2 endogenously expressed in SH-SY5Y cells assessed as calcium influx by FRIPR assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | SH-SY5Y |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Voltage-dependent N-type calcium channel subunit alpha-1B (CHEMBL4478) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The neuronal calcium ion channel activity of constrained analogues of MONIRO-1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 4.34 | 5.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4227475 | — | — | 1 | 5.16 |
| CHEMBL452076 | CILNIDIPINE | 3.0 | 1 | 4.58 |
| CHEMBL4794579 | — | — | 1 | 4.44 |
| CHEMBL4742798 | — | — | 1 | 4.36 |
| CHEMBL4741422 | — | — | 1 | 4.31 |
| CHEMBL4764424 | — | — | 1 | 4.21 |
| CHEMBL4781385 | — | — | 1 | 4.11 |
| CHEMBL4794057 | — | — | 1 | 4.11 |
| CHEMBL4791782 | — | — | 1 | 4.06 |
| CHEMBL4741821 | — | — | 1 | 4.01 |
| CHEMBL4754749 | — | — | 1 | - |
| CHEMBL4740547 | — | — | 1 | - |
| CHEMBL4759180 | — | — | 1 | - |
| CHEMBL4800369 | — | — | 1 | - |
| CHEMBL4749090 | — | — | 1 | - |
| CHEMBL4741805 | — | — | 1 | - |
| CHEMBL4749956 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4227475 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL452076 | CILNIDIPINE | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL4794579 | — | IC50 | = | 36000.0 | nM | 4.44 |
| CHEMBL4742798 | — | IC50 | = | 44000.0 | nM | 4.36 |
| CHEMBL4741422 | — | IC50 | = | 49000.0 | nM | 4.31 |
| CHEMBL4764424 | — | IC50 | = | 62000.0 | nM | 4.21 |
| CHEMBL4781385 | — | IC50 | = | 78000.0 | nM | 4.11 |
| CHEMBL4794057 | — | IC50 | = | 78000.0 | nM | 4.11 |
| CHEMBL4791782 | — | IC50 | = | 87000.0 | nM | 4.06 |
| CHEMBL4741821 | — | IC50 | = | 98000.0 | nM | 4.01 |
| CHEMBL4754749 | — | IC50 | = | 404000.0 | nM | - |
| CHEMBL4740547 | — | IC50 | = | 102000.0 | nM | - |
| CHEMBL4759180 | — | IC50 | = | 591000.0 | nM | - |
| CHEMBL4800369 | — | IC50 | = | 185000.0 | nM | - |
| CHEMBL4749090 | — | IC50 | = | 107000.0 | nM | - |
| CHEMBL4741805 | — | IC50 | = | 129000.0 | nM | - |
| CHEMBL4749956 | — | IC50 | = | 259000.0 | nM | - |