Assay Detail
Binding
CHEMBL881696
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Apparent dissociation constant against Cyclic nucleotide gated channel alpha 1 at 0 mV
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Bos taurus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Cyclic nucleotide-gated channel alpha-1 (CHEMBL4907) ↗| Type | SINGLE PROTEIN |
| Organism | Bos taurus |
Publication
Modifications to the tetracaine scaffold produce cyclic nucleotide-gated channel blockers with widely varying efficacies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 7 | 6.05 | 8.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1917652 | — | — | 1 | 8.16 |
| CHEMBL3559600 | — | — | 1 | 5.85 |
| CHEMBL195005 | — | — | 1 | 5.27 |
| CHEMBL698 | TETRACAINE | 4.0 | 1 | 4.92 |
| CHEMBL611483 | — | — | 1 | - |
| CHEMBL611746 | — | — | 1 | - |
| CHEMBL611747 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1917652 | — | Kd | = | 6.9 | nM | 8.16 |
| CHEMBL3559600 | — | Kd | = | 1400.0 | nM | 5.85 |
| CHEMBL195005 | — | Kd | = | 5400.0 | nM | 5.27 |
| CHEMBL698 | TETRACAINE | Kd | = | 12000.0 | nM | 4.92 |
| CHEMBL611483 | — | Kd | = | 970000.0 | nM | - |
| CHEMBL611746 | — | Kd | = | 4000000.0 | nM | - |
| CHEMBL611747 | — | Kd | = | 10000000.0 | nM | - |