Assay Detail
Binding
CHEMBL666571
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro ability to displace the specific binding of [3H]diltiazem to diltiazem receptor in guinea pig skeletal muscle.
38
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Voltage-dependent L-type calcium channel subunit alpha-1S (CHEMBL3805) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Benzazepinone calcium channel blockers. 4. Structure-activity overview and intracellular binding site.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 38 | 6.08 | 7.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL163740 | — | — | 1 | 7.28 |
| CHEMBL167935 | — | — | 1 | 7.12 |
| CHEMBL353757 | — | — | 1 | 6.92 |
| CHEMBL165086 | — | — | 1 | 6.92 |
| CHEMBL168066 | — | — | 1 | 6.92 |
| CHEMBL353566 | — | — | 1 | 6.89 |
| CHEMBL164399 | — | — | 1 | 6.80 |
| CHEMBL163771 | — | — | 1 | 6.66 |
| CHEMBL350321 | — | — | 1 | 6.60 |
| CHEMBL349753 | — | — | 1 | 6.50 |
| CHEMBL168099 | — | — | 1 | 6.40 |
| CHEMBL164134 | — | — | 1 | 6.38 |
| CHEMBL165444 | — | — | 1 | 6.28 |
| CHEMBL167987 | — | — | 2 | 6.27 |
| CHEMBL355684 | — | — | 1 | 6.24 |
| CHEMBL349193 | — | — | 1 | 6.22 |
| CHEMBL98189 | — | — | 1 | 6.19 |
| CHEMBL351235 | — | — | 1 | 6.18 |
| CHEMBL352750 | — | — | 1 | 6.08 |
| CHEMBL165049 | — | — | 1 | 6.00 |
| CHEMBL167384 | — | — | 1 | 5.96 |
| CHEMBL164917 | — | — | 1 | 5.85 |
| CHEMBL315809 | — | — | 1 | 5.85 |
| CHEMBL354933 | — | — | 1 | 5.80 |
| CHEMBL167512 | — | — | 1 | 5.80 |
| CHEMBL167147 | — | — | 1 | 5.75 |
| CHEMBL165217 | — | — | 1 | 5.75 |
| CHEMBL163719 | — | — | 1 | 5.70 |
| CHEMBL410539 | — | — | 1 | 5.70 |
| CHEMBL354353 | — | — | 1 | 5.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL163740 | — | Kd | = | 52.0 | nM | 7.28 |
| CHEMBL167935 | — | Kd | = | 75.0 | nM | 7.12 |
| CHEMBL353757 | — | Kd | = | 120.0 | nM | 6.92 |
| CHEMBL168066 | — | Kd | = | 120.0 | nM | 6.92 |
| CHEMBL165086 | — | Kd | = | 120.0 | nM | 6.92 |
| CHEMBL353566 | — | Kd | = | 130.0 | nM | 6.89 |
| CHEMBL164399 | — | Kd | = | 160.0 | nM | 6.80 |
| CHEMBL163771 | — | Kd | = | 220.0 | nM | 6.66 |
| CHEMBL350321 | — | Kd | = | 250.0 | nM | 6.60 |
| CHEMBL349753 | — | Kd | = | 320.0 | nM | 6.50 |
| CHEMBL168099 | — | Kd | = | 400.0 | nM | 6.40 |
| CHEMBL164134 | — | Kd | = | 420.0 | nM | 6.38 |
| CHEMBL165444 | — | Kd | = | 520.0 | nM | 6.28 |
| CHEMBL167987 | — | Kd | = | 540.0 | nM | 6.27 |
| CHEMBL355684 | — | Kd | = | 570.0 | nM | 6.24 |
| CHEMBL349193 | — | Kd | = | 600.0 | nM | 6.22 |
| CHEMBL167987 | — | Kd | = | 610.0 | nM | 6.21 |
| CHEMBL98189 | — | Kd | = | 650.0 | nM | 6.19 |
| CHEMBL351235 | — | Kd | = | 660.0 | nM | 6.18 |
| CHEMBL352750 | — | Kd | = | 840.0 | nM | 6.08 |
| CHEMBL165049 | — | Kd | = | 1000.0 | nM | 6.00 |
| CHEMBL167384 | — | Kd | = | 1100.0 | nM | 5.96 |
| CHEMBL315809 | — | Kd | = | 1400.0 | nM | 5.85 |
| CHEMBL164917 | — | Kd | = | 1400.0 | nM | 5.85 |
| CHEMBL167512 | — | Kd | = | 1600.0 | nM | 5.80 |
| CHEMBL354933 | — | Kd | = | 1600.0 | nM | 5.80 |
| CHEMBL167147 | — | Kd | = | 1800.0 | nM | 5.75 |
| CHEMBL165217 | — | Kd | = | 1800.0 | nM | 5.75 |
| CHEMBL410539 | — | Kd | = | 2000.0 | nM | 5.70 |
| CHEMBL163719 | — | Kd | = | 2000.0 | nM | 5.70 |
| CHEMBL354353 | — | Kd | = | 3500.0 | nM | 5.46 |
| CHEMBL89099 | — | Kd | = | 5100.0 | nM | 5.29 |
| CHEMBL348940 | — | Kd | = | 5800.0 | nM | 5.24 |
| CHEMBL164760 | — | Kd | = | 5800.0 | nM | 5.24 |
| CHEMBL349140 | — | Kd | = | 12000.0 | nM | 4.92 |
| CHEMBL165445 | — | Kd | = | 13000.0 | nM | 4.89 |
| CHEMBL351402 | — | Kd | = | 15000.0 | nM | 4.82 |
| CHEMBL164346 | — | Kd | = | 155000.0 | nM | - |