Assay Detail
Binding
CHEMBL4729686
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Inhibition of human T type calcium channel Cav3.2 expressed in HEK-293T 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 | HEK-293T |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Voltage-dependent T-type calcium channel subunit alpha-1H (CHEMBL1859) ↗| 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 | 4.52 | 5.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4227475 | — | — | 1 | 5.70 |
| CHEMBL4741422 | — | — | 1 | 4.72 |
| CHEMBL452076 | CILNIDIPINE | 3.0 | 1 | 4.62 |
| CHEMBL4759180 | — | — | 1 | 4.40 |
| CHEMBL4794579 | — | — | 1 | 4.31 |
| CHEMBL4740547 | — | — | 1 | 4.27 |
| CHEMBL4742798 | — | — | 1 | 4.26 |
| CHEMBL4764424 | — | — | 1 | 4.26 |
| CHEMBL4794057 | — | — | 1 | 4.10 |
| CHEMBL4754749 | — | — | 1 | - |
| CHEMBL4791782 | — | — | 1 | - |
| CHEMBL4781385 | — | — | 1 | - |
| CHEMBL4800369 | — | — | 1 | - |
| CHEMBL4741821 | — | — | 1 | - |
| CHEMBL4749090 | — | — | 1 | - |
| CHEMBL4741805 | — | — | 1 | - |
| CHEMBL4749956 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4227475 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL4741422 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL452076 | CILNIDIPINE | IC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL4759180 | — | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL4794579 | — | IC50 | = | 49000.0 | nM | 4.31 |
| CHEMBL4740547 | — | IC50 | = | 54000.0 | nM | 4.27 |
| CHEMBL4742798 | — | IC50 | = | 55000.0 | nM | 4.26 |
| CHEMBL4764424 | — | IC50 | = | 55000.0 | nM | 4.26 |
| CHEMBL4794057 | — | IC50 | = | 80000.0 | nM | 4.10 |
| CHEMBL4754749 | — | IC50 | = | 164000.0 | nM | - |
| CHEMBL4791782 | — | IC50 | = | 108000.0 | nM | - |
| CHEMBL4781385 | — | IC50 | = | 102000.0 | nM | - |
| CHEMBL4800369 | — | IC50 | - | — | - | |
| CHEMBL4741821 | — | IC50 | = | 110000.0 | nM | - |
| CHEMBL4749090 | — | IC50 | = | 113000.0 | nM | - |
| CHEMBL4741805 | — | IC50 | = | 133000.0 | nM | - |
| CHEMBL4749956 | — | IC50 | = | 193000.0 | nM | - |