Assay Detail
Binding
CHEMBL650834
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Inhibition of binding of [3H]-PK 11195 to peripheral-type benzodiazepine receptor (PBR) from rat cortex homogenate
27
Total Activities
27
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 |
|---|---|---|---|
| IC50 | 27 | 7.74 | 9.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL115740 | — | — | 1 | 9.17 |
| CHEMBL325025 | — | — | 1 | 9.03 |
| CHEMBL325953 | — | — | 1 | 8.89 |
| CHEMBL117444 | — | — | 1 | 8.89 |
| CHEMBL481537 | PK-11195 | — | 1 | 8.70 |
| CHEMBL326772 | — | — | 1 | 8.64 |
| CHEMBL115470 | — | — | 1 | 8.44 |
| CHEMBL326302 | — | — | 1 | 8.42 |
| CHEMBL117589 | — | — | 1 | 8.40 |
| CHEMBL325169 | — | — | 1 | 8.29 |
| CHEMBL325649 | — | — | 1 | 8.22 |
| CHEMBL288551 | — | — | 1 | 8.05 |
| CHEMBL326943 | — | — | 1 | 7.92 |
| CHEMBL33083 | — | — | 1 | 7.70 |
| CHEMBL116087 | — | — | 1 | 7.52 |
| CHEMBL114508 | — | — | 1 | 7.43 |
| CHEMBL323793 | — | — | 1 | 7.19 |
| CHEMBL325858 | — | — | 1 | 7.12 |
| CHEMBL325471 | — | — | 1 | 7.09 |
| CHEMBL324500 | — | — | 1 | 6.95 |
| CHEMBL332933 | — | — | 1 | 6.83 |
| CHEMBL117025 | — | — | 1 | 6.56 |
| CHEMBL115704 | — | — | 1 | 6.23 |
| CHEMBL326066 | — | — | 1 | 6.17 |
| CHEMBL115004 | — | — | 1 | 5.71 |
| CHEMBL119905 | — | — | 1 | - |
| CHEMBL284371 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL115740 | — | IC50 | = | 0.68 | nM | 9.17 |
| CHEMBL325025 | — | IC50 | = | 0.94 | nM | 9.03 |
| CHEMBL325953 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL117444 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL481537 | PK-11195 | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL326772 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL115470 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL326302 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL117589 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL325169 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL325649 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL288551 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL326943 | — | IC50 | = | 12.1 | nM | 7.92 |
| CHEMBL33083 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL116087 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL114508 | — | IC50 | = | 37.3 | nM | 7.43 |
| CHEMBL323793 | — | IC50 | = | 64.6 | nM | 7.19 |
| CHEMBL325858 | — | IC50 | = | 76.6 | nM | 7.12 |
| CHEMBL325471 | — | IC50 | = | 81.9 | nM | 7.09 |
| CHEMBL324500 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL332933 | — | IC50 | = | 148.0 | nM | 6.83 |
| CHEMBL117025 | — | IC50 | = | 278.0 | nM | 6.56 |
| CHEMBL115704 | — | IC50 | = | 589.0 | nM | 6.23 |
| CHEMBL326066 | — | IC50 | = | 675.0 | nM | 6.17 |
| CHEMBL115004 | — | IC50 | = | 1930.0 | nM | 5.71 |
| CHEMBL119905 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL284371 | — | IC50 | > | 1000000.0 | nM | - |