Assay Detail
Binding
CHEMBL652449
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Binding affinity against peripheral-type benzodiazepine receptor (PBR) from rat cortex homogenate using [3H]-PK 11195 as radioligand
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Synthesis, biological activity, and SARs of pyrrolobenzoxazepine derivatives, a new class of specific "peripheral-type" benzodiazepine receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 25 | 8.15 | 9.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL115740 | — | — | 1 | 9.59 |
| CHEMBL325025 | — | — | 1 | 9.44 |
| CHEMBL325953 | — | — | 1 | 9.29 |
| CHEMBL117444 | — | — | 1 | 9.28 |
| CHEMBL481537 | PK-11195 | — | 1 | 9.11 |
| CHEMBL326772 | — | — | 1 | 9.04 |
| CHEMBL115470 | — | — | 1 | 8.85 |
| CHEMBL326302 | — | — | 1 | 8.82 |
| CHEMBL117589 | — | — | 1 | 8.74 |
| CHEMBL325169 | — | — | 1 | 8.70 |
| CHEMBL325649 | — | — | 1 | 8.62 |
| CHEMBL288551 | — | — | 1 | 8.46 |
| CHEMBL326943 | — | — | 1 | 8.33 |
| CHEMBL33083 | — | — | 1 | 8.12 |
| CHEMBL116087 | — | — | 1 | 7.93 |
| CHEMBL114508 | — | — | 1 | 7.84 |
| CHEMBL323793 | — | — | 1 | 7.60 |
| CHEMBL325858 | — | — | 1 | 7.52 |
| CHEMBL325471 | — | — | 1 | 7.50 |
| CHEMBL324500 | — | — | 1 | 7.36 |
| CHEMBL332933 | — | — | 1 | 7.24 |
| CHEMBL117025 | — | — | 1 | 6.97 |
| CHEMBL115704 | — | — | 1 | 6.64 |
| CHEMBL326066 | — | — | 1 | 6.58 |
| CHEMBL115004 | — | — | 1 | 6.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL115740 | — | Ki | = | 0.26 | nM | 9.59 |
| CHEMBL325025 | — | Ki | = | 0.36 | nM | 9.44 |
| CHEMBL325953 | — | Ki | = | 0.51 | nM | 9.29 |
| CHEMBL117444 | — | Ki | = | 0.52 | nM | 9.28 |
| CHEMBL481537 | PK-11195 | Ki | = | 0.78 | nM | 9.11 |
| CHEMBL326772 | — | Ki | = | 0.91 | nM | 9.04 |
| CHEMBL115470 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL326302 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL117589 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL325169 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL325649 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL288551 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL326943 | — | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL33083 | — | Ki | = | 7.6 | nM | 8.12 |
| CHEMBL116087 | — | Ki | = | 11.7 | nM | 7.93 |
| CHEMBL114508 | — | Ki | = | 14.5 | nM | 7.84 |
| CHEMBL323793 | — | Ki | = | 25.2 | nM | 7.60 |
| CHEMBL325858 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL325471 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL324500 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL332933 | — | Ki | = | 57.8 | nM | 7.24 |
| CHEMBL117025 | — | Ki | = | 108.0 | nM | 6.97 |
| CHEMBL115704 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL326066 | — | Ki | = | 263.0 | nM | 6.58 |
| CHEMBL115004 | — | Ki | = | 754.0 | nM | 6.12 |