Assay Detail
Binding
CHEMBL651678
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In vitro binding affinity (pIC50) was tested against peripheral benzodiazepine receptor (PBR) in rat.
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Mapping the peripheral benzodiazepine receptor binding site by conformationally restrained derivatives of 1-(2-chlorophenyl)-N-methyl-N-(1-methylpropyl)-3- isoquinolinecarboxamide (PK11195).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 7.30 | 8.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL15248 | — | — | 1 | 8.68 |
| CHEMBL276756 | — | — | 1 | 8.68 |
| CHEMBL481537 | PK-11195 | — | 1 | 8.66 |
| CHEMBL15003 | — | — | 1 | 8.54 |
| CHEMBL280482 | — | — | 1 | 8.51 |
| CHEMBL15254 | — | — | 1 | 8.47 |
| CHEMBL275410 | — | — | 1 | 8.19 |
| CHEMBL14956 | — | — | 1 | 8.06 |
| CHEMBL15237 | — | — | 1 | 8.05 |
| CHEMBL276341 | — | — | 1 | 8.01 |
| CHEMBL416713 | — | — | 1 | 8.00 |
| CHEMBL278011 | — | — | 1 | 7.95 |
| CHEMBL280035 | — | — | 1 | 7.89 |
| CHEMBL15714 | — | — | 1 | 7.34 |
| CHEMBL277586 | — | — | 1 | 6.77 |
| CHEMBL14920 | — | — | 1 | 6.64 |
| CHEMBL15584 | — | — | 1 | 6.57 |
| CHEMBL15315 | — | — | 1 | 6.32 |
| CHEMBL15630 | — | — | 1 | 6.31 |
| CHEMBL15239 | — | — | 1 | 6.26 |
| CHEMBL15316 | — | — | 1 | 6.21 |
| CHEMBL15255 | — | — | 1 | 6.10 |
| CHEMBL429386 | — | — | 1 | 6.09 |
| CHEMBL416162 | — | — | 1 | 5.92 |
| CHEMBL15473 | — | — | 1 | 5.92 |
| CHEMBL15709 | — | — | 1 | 5.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL15248 | — | IC50 | = | 2.089 | nM | 8.68 |
| CHEMBL276756 | — | IC50 | = | 2.089 | nM | 8.68 |
| CHEMBL481537 | PK-11195 | IC50 | = | 2.188 | nM | 8.66 |
| CHEMBL15003 | — | IC50 | = | 2.884 | nM | 8.54 |
| CHEMBL280482 | — | IC50 | = | 3.09 | nM | 8.51 |
| CHEMBL15254 | — | IC50 | = | 3.388 | nM | 8.47 |
| CHEMBL275410 | — | IC50 | = | 6.457 | nM | 8.19 |
| CHEMBL14956 | — | IC50 | = | 8.71 | nM | 8.06 |
| CHEMBL15237 | — | IC50 | = | 8.913 | nM | 8.05 |
| CHEMBL276341 | — | IC50 | = | 9.772 | nM | 8.01 |
| CHEMBL416713 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL278011 | — | IC50 | = | 11.22 | nM | 7.95 |
| CHEMBL280035 | — | IC50 | = | 12.88 | nM | 7.89 |
| CHEMBL15714 | — | IC50 | = | 45.71 | nM | 7.34 |
| CHEMBL277586 | — | IC50 | = | 169.82 | nM | 6.77 |
| CHEMBL14920 | — | IC50 | = | 229.09 | nM | 6.64 |
| CHEMBL15584 | — | IC50 | = | 269.15 | nM | 6.57 |
| CHEMBL15315 | — | IC50 | = | 478.63 | nM | 6.32 |
| CHEMBL15630 | — | IC50 | = | 489.78 | nM | 6.31 |
| CHEMBL15239 | — | IC50 | = | 549.54 | nM | 6.26 |
| CHEMBL15316 | — | IC50 | = | 616.6 | nM | 6.21 |
| CHEMBL15255 | — | IC50 | = | 794.33 | nM | 6.10 |
| CHEMBL429386 | — | IC50 | = | 812.83 | nM | 6.09 |
| CHEMBL416162 | — | IC50 | = | 1202.26 | nM | 5.92 |
| CHEMBL15473 | — | IC50 | = | 1202.26 | nM | 5.92 |
| CHEMBL15709 | — | IC50 | = | 1698.24 | nM | 5.77 |