Assay Detail
Functional
CHEMBL802806
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of calcium activation was assessed against calcium-induced constriction of potassium-depolarized rat aorta (Negative logarithm of the molar concentration)
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Tissue | Aorta |
| Confidence | 1 — Organism |
| Curated By | Expert |
Publication
A new class of calcium antagonists. 2. Synthesis and biological activity of 11-[[4-[4-(4-fluorophenyl)-1-piperazinyl]butyryl]amino]-6,11- dihydrodibenzo[b,e]-thiepin maleate and related compounds.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 36 | 8.19 | 9.83 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL193 | NIFEDIPINE | 4.0 | 1 | 9.83 |
| CHEMBL1744296 | — | — | 1 | 8.98 |
| CHEMBL1744302 | — | — | 1 | 8.76 |
| CHEMBL1744305 | MONATEPIL MALEATE | -1.0 | 1 | 8.71 |
| CHEMBL425504 | — | — | 1 | 8.68 |
| CHEMBL355755 | — | — | 1 | 8.56 |
| CHEMBL367546 | — | — | 1 | 8.55 |
| CHEMBL369582 | — | — | 1 | 8.55 |
| CHEMBL1744301 | — | — | 1 | 8.54 |
| CHEMBL368396 | — | — | 1 | 8.49 |
| CHEMBL176966 | — | — | 1 | 8.48 |
| CHEMBL174459 | — | — | 1 | 8.47 |
| CHEMBL171576 | — | — | 1 | 8.46 |
| CHEMBL172537 | — | — | 1 | 8.46 |
| CHEMBL1744304 | — | — | 1 | 8.43 |
| CHEMBL435903 | — | — | 1 | 8.35 |
| CHEMBL173408 | — | — | 1 | 8.30 |
| CHEMBL434922 | — | — | 1 | 8.27 |
| CHEMBL1203863 | — | — | 1 | 8.22 |
| CHEMBL6966 | VERAPAMIL | 4.0 | 1 | 8.16 |
| CHEMBL1744299 | — | — | 1 | 8.12 |
| CHEMBL368206 | — | — | 1 | 8.10 |
| CHEMBL436090 | — | — | 1 | 8.05 |
| CHEMBL1744303 | — | — | 1 | 8.03 |
| CHEMBL367689 | — | — | 1 | 7.98 |
| CHEMBL175049 | — | — | 1 | 7.98 |
| CHEMBL1744300 | — | — | 1 | 7.91 |
| CHEMBL1201888 | — | — | 1 | 7.88 |
| CHEMBL1744297 | — | — | 1 | 7.81 |
| CHEMBL1202060 | — | — | 1 | 7.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL193 | NIFEDIPINE | Kd | = | 0.1479 | nM | 9.83 |
| CHEMBL1744296 | — | Kd | = | 1.047 | nM | 8.98 |
| CHEMBL1744302 | — | Kd | = | 1.738 | nM | 8.76 |
| CHEMBL1744305 | MONATEPIL MALEATE | Kd | = | 1.95 | nM | 8.71 |
| CHEMBL425504 | — | Kd | = | 2.089 | nM | 8.68 |
| CHEMBL355755 | — | Kd | = | 2.754 | nM | 8.56 |
| CHEMBL367546 | — | Kd | = | 2.818 | nM | 8.55 |
| CHEMBL369582 | — | Kd | = | 2.818 | nM | 8.55 |
| CHEMBL1744301 | — | Kd | = | 2.884 | nM | 8.54 |
| CHEMBL368396 | — | Kd | = | 3.236 | nM | 8.49 |
| CHEMBL176966 | — | Kd | = | 3.311 | nM | 8.48 |
| CHEMBL174459 | — | Kd | = | 3.388 | nM | 8.47 |
| CHEMBL171576 | — | Kd | = | 3.467 | nM | 8.46 |
| CHEMBL172537 | — | Kd | = | 3.467 | nM | 8.46 |
| CHEMBL1744304 | — | Kd | = | 3.715 | nM | 8.43 |
| CHEMBL435903 | — | Kd | = | 4.467 | nM | 8.35 |
| CHEMBL173408 | — | Kd | = | 5.012 | nM | 8.30 |
| CHEMBL434922 | — | Kd | = | 5.37 | nM | 8.27 |
| CHEMBL1203863 | — | Kd | = | 6.026 | nM | 8.22 |
| CHEMBL6966 | VERAPAMIL | Kd | = | 6.918 | nM | 8.16 |
| CHEMBL1744299 | — | Kd | = | 7.586 | nM | 8.12 |
| CHEMBL368206 | — | Kd | = | 7.943 | nM | 8.10 |
| CHEMBL436090 | — | Kd | = | 8.913 | nM | 8.05 |
| CHEMBL1744303 | — | Kd | = | 9.333 | nM | 8.03 |
| CHEMBL367689 | — | Kd | = | 10.47 | nM | 7.98 |
| CHEMBL175049 | — | Kd | = | 10.47 | nM | 7.98 |
| CHEMBL1744300 | — | Kd | = | 12.3 | nM | 7.91 |
| CHEMBL1201888 | — | Kd | = | 13.18 | nM | 7.88 |
| CHEMBL1744297 | — | Kd | = | 15.49 | nM | 7.81 |
| CHEMBL1202060 | — | Kd | = | 20.89 | nM | 7.68 |
| CHEMBL1744298 | — | Kd | = | 30.9 | nM | 7.51 |
| CHEMBL176793 | — | Kd | = | 33.11 | nM | 7.48 |
| CHEMBL1744306 | — | Kd | = | 36.31 | nM | 7.44 |
| CHEMBL23 | DILTIAZEM | Kd | = | 38.02 | nM | 7.42 |
| CHEMBL171015 | — | Kd | = | 69.18 | nM | 7.16 |
| CHEMBL173556 | — | Kd | = | 69.18 | nM | 7.16 |