Assay Detail
Binding
CHEMBL653022
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Ability to inhibit [3H]-PK 11195 binding to peripheral-type benzodiazepine receptor(PBR) in rat cerebral cortex homogenate.
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Cerebral cortex |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Cardiovascular characterization of pyrrolo[2,1-d][1,5]benzothiazepine derivatives binding selectively to the peripheral-type benzodiazepine receptor (PBR): from dual PBR affinity and calcium antagonist activity to novel and selective calcium entry blockers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 7.44 | 8.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6966 | VERAPAMIL | 4.0 | 1 | 8.85 |
| CHEMBL481537 | PK-11195 | — | 1 | 8.70 |
| CHEMBL33096 | — | — | 1 | 8.05 |
| CHEMBL284532 | — | — | 1 | 7.70 |
| CHEMBL33083 | — | — | 1 | 7.70 |
| CHEMBL284623 | — | — | 1 | 7.66 |
| CHEMBL416214 | — | — | 1 | 7.64 |
| CHEMBL33609 | — | — | 1 | 7.55 |
| CHEMBL33165 | — | — | 1 | 7.47 |
| CHEMBL416040 | — | — | 1 | 7.32 |
| CHEMBL98834 | — | — | 1 | 6.86 |
| CHEMBL33042 | — | — | 1 | 6.82 |
| CHEMBL32657 | — | — | 1 | 6.19 |
| CHEMBL102052 | — | — | 1 | 5.62 |
| CHEMBL277363 | — | — | 1 | - |
| CHEMBL317219 | — | — | 1 | - |
| CHEMBL98948 | — | — | 1 | - |
| CHEMBL430463 | — | — | 1 | - |
| CHEMBL430465 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6966 | VERAPAMIL | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL481537 | PK-11195 | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL33096 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL284532 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL33083 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL284623 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL416214 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL33609 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL33165 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL416040 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL98834 | — | IC50 | = | 139.0 | nM | 6.86 |
| CHEMBL33042 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL32657 | — | IC50 | = | 651.0 | nM | 6.19 |
| CHEMBL102052 | — | IC50 | = | 2407.0 | nM | 5.62 |
| CHEMBL277363 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL317219 | — | IC50 | - | nM | - | |
| CHEMBL98948 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL430463 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL430465 | — | IC50 | > | 2000.0 | nM | - |