Assay Detail
Binding
CHEMBL5520037
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at TRPC6 (unknown origin) assessed as inhibition of channel activity
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Short transient receptor potential channel 6 (CHEMBL2417347) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of N-alkyl-N-benzyl thiazoles as novel TRPC antagonists for the treatment of glioblastoma multiforme.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 7.45 | 9.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5567030 | — | — | 1 | 9.66 |
| CHEMBL2418809 | — | — | 1 | 8.40 |
| CHEMBL5532633 | — | — | 1 | 8.24 |
| CHEMBL4129809 | — | — | 1 | 8.10 |
| CHEMBL5558723 | — | — | 1 | 8.00 |
| CHEMBL5567783 | — | — | 1 | 7.89 |
| CHEMBL2418811 | — | — | 1 | 7.68 |
| CHEMBL5561836 | — | — | 1 | 6.00 |
| CHEMBL1740853 | — | — | 1 | 5.38 |
| CHEMBL6206 | BROMOENOL LACTONE | — | 1 | 5.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5567030 | — | IC50 | = | 0.22 | nM | 9.66 |
| CHEMBL2418809 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5532633 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL4129809 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL5558723 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5567783 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL2418811 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL5561836 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL1740853 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL6206 | BROMOENOL LACTONE | IC50 | = | 7200.0 | nM | 5.14 |