Assay Detail
Binding
CHEMBL3880755
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at rat alpha1B N-type Ca2+ channel expressed in HEK293 cells assessed as 0.2 Hz current frequency dependent channel blocking for 2 mins in presence of Ba2+ by whole-cell patch clamp assay
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Voltage-dependent N-type calcium channel subunit alpha-1B (CHEMBL5107) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Calcium channel inhibitors comprising benzhydril spaced from piperazine
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 33 | 6.64 | 7.13 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL597585 | — | — | 1 | 7.13 |
| CHEMBL597788 | — | — | 1 | 6.98 |
| CHEMBL3930176 | — | — | 1 | 6.96 |
| CHEMBL3927466 | — | — | 1 | 6.94 |
| CHEMBL3978555 | — | — | 1 | 6.92 |
| CHEMBL596946 | — | — | 1 | 6.92 |
| CHEMBL3939633 | — | — | 1 | 6.86 |
| CHEMBL3915774 | — | — | 1 | 6.85 |
| CHEMBL598806 | — | — | 1 | 6.77 |
| CHEMBL3967577 | — | — | 1 | 6.72 |
| CHEMBL3927871 | — | — | 1 | 6.72 |
| CHEMBL3896085 | — | — | 1 | 6.72 |
| CHEMBL3935114 | — | — | 1 | 6.68 |
| CHEMBL599016 | — | — | 1 | 6.68 |
| CHEMBL599832 | — | — | 1 | 6.66 |
| CHEMBL3972049 | — | — | 1 | 6.66 |
| CHEMBL3949401 | — | — | 1 | 6.63 |
| CHEMBL599015 | — | — | 1 | 6.62 |
| CHEMBL598603 | — | — | 1 | 6.60 |
| CHEMBL606175 | — | — | 1 | 6.60 |
| CHEMBL3942862 | — | — | 1 | 6.60 |
| CHEMBL598990 | — | — | 1 | 6.52 |
| CHEMBL597970 | — | — | 1 | 6.51 |
| CHEMBL597969 | — | — | 1 | 6.42 |
| CHEMBL3918151 | — | — | 1 | 6.35 |
| CHEMBL589285 | — | — | 1 | 6.29 |
| CHEMBL3950908 | — | — | 1 | 6.27 |
| CHEMBL3956949 | — | — | 1 | 6.26 |
| CHEMBL3916031 | — | — | 1 | 6.17 |
| CHEMBL3918918 | — | — | 1 | 6.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL597585 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL597788 | — | IC50 | = | 105.0 | nM | 6.98 |
| CHEMBL3930176 | — | IC50 | = | 111.0 | nM | 6.96 |
| CHEMBL3927466 | — | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL3978555 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL596946 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3939633 | — | IC50 | = | 137.0 | nM | 6.86 |
| CHEMBL3915774 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL598806 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL3967577 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL3927871 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL3896085 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL3935114 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL599016 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL3972049 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL599832 | — | IC50 | = | 217.0 | nM | 6.66 |
| CHEMBL3949401 | — | IC50 | = | 233.0 | nM | 6.63 |
| CHEMBL599015 | — | IC50 | = | 237.0 | nM | 6.62 |
| CHEMBL598603 | — | IC50 | = | 249.0 | nM | 6.60 |
| CHEMBL606175 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL3942862 | — | IC50 | = | 252.0 | nM | 6.60 |
| CHEMBL598990 | — | IC50 | = | 301.0 | nM | 6.52 |
| CHEMBL597970 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL597969 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL3918151 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL589285 | — | IC50 | = | 513.0 | nM | 6.29 |
| CHEMBL3950908 | — | IC50 | = | 533.0 | nM | 6.27 |
| CHEMBL3956949 | — | IC50 | = | 552.0 | nM | 6.26 |
| CHEMBL3916031 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL3918918 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL3956201 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL599833 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL599014 | — | IC50 | > | 1000.0 | nM | - |