Assay Detail
Binding
CHEMBL1909102
Review assay metadata, readout intent, target linkage, and publication context from the same page.
DRUGMATRIX: Calcium Channel Type L, Benzothiazepine radioligand binding (ligand: [3H] Diltiazem)
1742
Total Activities
871
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
DrugMatrix in vitro pharmacology data
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 871 | 5.94 | 8.80 |
| Ki | 871 | 5.99 | 8.86 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL475534 | NITRENDIPINE | 3.0 | 2 | 8.86 |
| CHEMBL1428 | NIMODIPINE | 4.0 | 2 | 8.73 |
| CHEMBL1726 | NISOLDIPINE | 4.0 | 2 | 8.66 |
| CHEMBL460291 | LACIDIPINE | 3.0 | 2 | 8.31 |
| CHEMBL193 | NIFEDIPINE | 4.0 | 2 | 8.11 |
| CHEMBL6966 | VERAPAMIL | 4.0 | 2 | 7.92 |
| CHEMBL1480 | FELODIPINE | 4.0 | 2 | 7.70 |
| CHEMBL23 | DILTIAZEM | 4.0 | 2 | 7.60 |
| CHEMBL633 | AMIODARONE | 4.0 | 2 | 7.32 |
| CHEMBL305660 | EBASTINE | 4.0 | 2 | 7.24 |
| CHEMBL1491 | AMLODIPINE | 4.0 | 2 | 7.05 |
| CHEMBL404849 | SULOCTIDIL | 4.0 | 2 | 6.82 |
| CHEMBL841 | LOPERAMIDE | 4.0 | 2 | 6.71 |
| CHEMBL17157 | TERFENADINE | 4.0 | 2 | 6.70 |
| CHEMBL19215 | METERGOLINE | 2.0 | 2 | 6.62 |
| CHEMBL490 | PAROXETINE | 4.0 | 2 | 6.48 |
| CHEMBL81 | RALOXIFENE | 4.0 | 2 | 6.43 |
| CHEMBL479 | THIORIDAZINE | 4.0 | 2 | 6.38 |
| CHEMBL723 | CARVEDILOL | 4.0 | 2 | 6.26 |
| CHEMBL631 | PROPAFENONE | 4.0 | 2 | 6.16 |
| CHEMBL1729 | CISAPRIDE | 4.0 | 2 | 6.15 |
| CHEMBL954 | ENCLOMIPHENE | 3.0 | 2 | 6.15 |
| CHEMBL1419 | SIBUTRAMINE | 4.0 | 2 | 6.14 |
| CHEMBL41 | FLUOXETINE | 4.0 | 2 | 6.13 |
| CHEMBL43064 | CINNARIZINE | 2.0 | 2 | 6.13 |
| CHEMBL75880 | PERHEXILINE | 4.0 | 2 | 6.03 |
| CHEMBL7568 | QUINACRINE | 4.0 | 2 | 6.02 |
| CHEMBL296419 | ASTEMIZOLE | 4.0 | 2 | 6.01 |
| CHEMBL30008 | FLUNARIZINE | 2.0 | 2 | 6.00 |
| CHEMBL221753 | BENZETHONIUM CHLORIDE | 2.0 | 2 | 5.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL475534 | NITRENDIPINE | Ki | = | 1.391 | nM | 8.86 |
| CHEMBL475534 | NITRENDIPINE | IC50 | = | 1.565 | nM | 8.80 |
| CHEMBL1428 | NIMODIPINE | Ki | = | 1.86 | nM | 8.73 |
| CHEMBL1428 | NIMODIPINE | IC50 | = | 2.093 | nM | 8.68 |
| CHEMBL1726 | NISOLDIPINE | Ki | = | 2.208 | nM | 8.66 |
| CHEMBL1726 | NISOLDIPINE | IC50 | = | 2.484 | nM | 8.61 |
| CHEMBL460291 | LACIDIPINE | Ki | = | 4.843 | nM | 8.31 |
| CHEMBL460291 | LACIDIPINE | IC50 | = | 5.449 | nM | 8.26 |
| CHEMBL193 | NIFEDIPINE | Ki | = | 7.707 | nM | 8.11 |
| CHEMBL193 | NIFEDIPINE | IC50 | = | 8.67 | nM | 8.06 |
| CHEMBL6966 | VERAPAMIL | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL6966 | VERAPAMIL | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL1480 | FELODIPINE | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL1480 | FELODIPINE | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL23 | DILTIAZEM | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL23 | DILTIAZEM | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL633 | AMIODARONE | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL633 | AMIODARONE | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL305660 | EBASTINE | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL305660 | EBASTINE | IC50 | = | 65.3 | nM | 7.18 |
| CHEMBL1491 | AMLODIPINE | Ki | = | 90.0 | nM | 7.05 |
| CHEMBL1491 | AMLODIPINE | IC50 | = | 101.0 | nM | 7.00 |
| CHEMBL404849 | SULOCTIDIL | Ki | = | 152.2 | nM | 6.82 |
| CHEMBL404849 | SULOCTIDIL | IC50 | = | 171.2 | nM | 6.77 |
| CHEMBL841 | LOPERAMIDE | Ki | = | 196.0 | nM | 6.71 |
| CHEMBL17157 | TERFENADINE | Ki | = | 201.0 | nM | 6.70 |
| CHEMBL841 | LOPERAMIDE | IC50 | = | 221.0 | nM | 6.66 |
| CHEMBL17157 | TERFENADINE | IC50 | = | 226.0 | nM | 6.65 |
| CHEMBL19215 | METERGOLINE | Ki | = | 238.0 | nM | 6.62 |
| CHEMBL19215 | METERGOLINE | IC50 | = | 268.0 | nM | 6.57 |
| CHEMBL490 | PAROXETINE | Ki | = | 331.0 | nM | 6.48 |
| CHEMBL490 | PAROXETINE | IC50 | = | 373.0 | nM | 6.43 |
| CHEMBL81 | RALOXIFENE | Ki | = | 368.0 | nM | 6.43 |
| CHEMBL479 | THIORIDAZINE | Ki | = | 417.0 | nM | 6.38 |
| CHEMBL81 | RALOXIFENE | IC50 | = | 414.0 | nM | 6.38 |
| CHEMBL479 | THIORIDAZINE | IC50 | = | 469.0 | nM | 6.33 |
| CHEMBL723 | CARVEDILOL | Ki | = | 552.0 | nM | 6.26 |
| CHEMBL723 | CARVEDILOL | IC50 | = | 621.0 | nM | 6.21 |
| CHEMBL631 | PROPAFENONE | Ki | = | 689.0 | nM | 6.16 |
| CHEMBL1729 | CISAPRIDE | Ki | = | 713.0 | nM | 6.15 |
| CHEMBL954 | ENCLOMIPHENE | Ki | = | 701.0 | nM | 6.15 |
| CHEMBL1419 | SIBUTRAMINE | Ki | = | 719.0 | nM | 6.14 |
| CHEMBL41 | FLUOXETINE | Ki | = | 736.0 | nM | 6.13 |
| CHEMBL43064 | CINNARIZINE | Ki | = | 732.0 | nM | 6.13 |
| CHEMBL631 | PROPAFENONE | IC50 | = | 775.0 | nM | 6.11 |
| CHEMBL1729 | CISAPRIDE | IC50 | = | 802.0 | nM | 6.10 |
| CHEMBL954 | ENCLOMIPHENE | IC50 | = | 789.0 | nM | 6.10 |
| CHEMBL1419 | SIBUTRAMINE | IC50 | = | 809.0 | nM | 6.09 |
| CHEMBL41 | FLUOXETINE | IC50 | = | 827.0 | nM | 6.08 |
| CHEMBL43064 | CINNARIZINE | IC50 | = | 823.0 | nM | 6.08 |