Assay Detail
Binding
CHEMBL1116628
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Blocking of rat Voltage-dependent L-type calcium channel alpha1c/alpha2delta-1/beta1b activity expressed in HEK293 cells assessed as whole cell current by whole cell patch clamp assay
11
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | HEK293 |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Scaffold-based design and synthesis of potent N-type calcium channel blockers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 6.20 | 6.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1087660 | — | — | 1 | 6.92 |
| CHEMBL29188 | LOMERIZINE | 2.0 | 1 | 6.82 |
| CHEMBL1087275 | — | — | 1 | 6.60 |
| CHEMBL30008 | FLUNARIZINE | 2.0 | 1 | 6.51 |
| CHEMBL1088309 | — | — | 2 | 6.48 |
| CHEMBL1088610 | — | — | 1 | 6.13 |
| CHEMBL1087237 | — | — | 1 | 6.08 |
| CHEMBL599217 | — | — | 1 | 5.74 |
| CHEMBL1086621 | — | — | 1 | 5.55 |
| CHEMBL604710 | Z160 | 2.0 | 1 | 4.91 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1087660 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL29188 | LOMERIZINE | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL1087275 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL30008 | FLUNARIZINE | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL1088309 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL1088309 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL1088610 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL1087237 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL599217 | — | IC50 | = | 1840.0 | nM | 5.74 |
| CHEMBL1086621 | — | IC50 | = | 2840.0 | nM | 5.55 |
| CHEMBL604710 | Z160 | IC50 | = | 12200.0 | nM | 4.91 |