Assay Detail
Binding
CHEMBL650832
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In vitro displacement of [3H]PK11195 from the peripheral benzodiazepine receptor (PBR) in rat cortex
30
Total Activities
30
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 | 30 | 7.31 | 8.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL276756 | — | — | 1 | 8.68 |
| CHEMBL15248 | — | — | 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 | 7.96 |
| CHEMBL280035 | — | — | 1 | 7.89 |
| CHEMBL15714 | — | — | 1 | 7.35 |
| 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 | 6.11 |
| CHEMBL429386 | — | — | 1 | 6.09 |
| CHEMBL416162 | — | — | 1 | 5.92 |
| CHEMBL15473 | — | — | 1 | 5.92 |
| CHEMBL15709 | — | — | 1 | 5.77 |
| CHEMBL317374 | — | — | 1 | - |
| CHEMBL98642 | — | — | 1 | - |
| CHEMBL99194 | — | — | 1 | - |
| CHEMBL101823 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL276756 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL15248 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL481537 | PK-11195 | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL15003 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL280482 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL15254 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL275410 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL14956 | — | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL15237 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL276341 | — | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL416713 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL278011 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL280035 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL15714 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL277586 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL14920 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL15584 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL15315 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL15630 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL15239 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL15316 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL15255 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL429386 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL416162 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL15473 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL15709 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL317374 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL98642 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL99194 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL101823 | — | IC50 | > | 10000.0 | nM | - |