Assay Detail
Binding
CHEMBL881697
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 +40 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 | 7.08 | 10.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1917652 | — | — | 1 | 10.52 |
| CHEMBL3559600 | — | — | 1 | 7.13 |
| CHEMBL195005 | — | — | 1 | 5.51 |
| CHEMBL698 | TETRACAINE | 4.0 | 1 | 5.17 |
| CHEMBL611483 | — | — | 1 | - |
| CHEMBL611746 | — | — | 1 | - |
| CHEMBL611747 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1917652 | — | Kd | = | 0.03 | nM | 10.52 |
| CHEMBL3559600 | — | Kd | = | 74.0 | nM | 7.13 |
| CHEMBL195005 | — | Kd | = | 3100.0 | nM | 5.51 |
| CHEMBL698 | TETRACAINE | Kd | = | 6800.0 | nM | 5.17 |
| CHEMBL611483 | — | Kd | = | 210000.0 | nM | - |
| CHEMBL611746 | — | Kd | = | 2500000.0 | nM | - |
| CHEMBL611747 | — | Kd | = | 2300000.0 | nM | - |