Assay Detail
Binding
CHEMBL650999
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Displacement of [3H]flunitrazepam from diazepam-sensitive GABA-A benzodiazepine receptor of rat cortical membrane
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL1907607) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Synthesis and structure-activity relationships of 3,5-disubstituted 4,5-dihydro-6H-imidazo[1,5-a][1,4]benzodiazepin-6-ones at diazepam-sensitive and diazepam-insensitive benzodiazepine receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 7.16 | 8.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54069 | — | — | 1 | 8.62 |
| CHEMBL267665 | RO-147437 | — | 1 | 8.52 |
| CHEMBL301513 | — | — | 1 | 8.03 |
| CHEMBL300027 | — | — | 1 | 7.82 |
| CHEMBL145300 | — | — | 1 | 7.63 |
| CHEMBL53119 | — | — | 1 | 7.46 |
| CHEMBL52934 | — | — | 1 | 7.42 |
| CHEMBL51740 | — | — | 1 | 6.80 |
| CHEMBL356583 | — | — | 1 | 6.79 |
| CHEMBL148068 | — | — | 1 | 6.62 |
| CHEMBL145431 | — | — | 1 | 6.50 |
| CHEMBL53425 | — | — | 1 | 6.47 |
| CHEMBL144497 | — | — | 1 | 6.47 |
| CHEMBL143502 | — | — | 1 | 6.16 |
| CHEMBL358734 | — | — | 1 | 6.13 |
| CHEMBL358804 | — | — | 1 | - |
| CHEMBL356721 | — | — | 1 | - |
| CHEMBL357180 | — | — | 1 | - |
| CHEMBL144266 | — | — | 1 | - |
| CHEMBL358820 | — | — | 1 | - |
| CHEMBL144655 | — | — | 1 | - |
| CHEMBL436072 | — | — | 1 | - |
| CHEMBL291473 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54069 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL267665 | RO-147437 | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL301513 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL300027 | — | IC50 | = | 15.3 | nM | 7.82 |
| CHEMBL145300 | — | IC50 | = | 23.2 | nM | 7.63 |
| CHEMBL53119 | — | IC50 | = | 34.3 | nM | 7.46 |
| CHEMBL52934 | — | IC50 | = | 37.8 | nM | 7.42 |
| CHEMBL51740 | — | IC50 | = | 157.0 | nM | 6.80 |
| CHEMBL356583 | — | IC50 | = | 164.0 | nM | 6.79 |
| CHEMBL148068 | — | IC50 | = | 238.0 | nM | 6.62 |
| CHEMBL145431 | — | IC50 | = | 317.0 | nM | 6.50 |
| CHEMBL53425 | — | IC50 | = | 338.0 | nM | 6.47 |
| CHEMBL144497 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL143502 | — | IC50 | = | 687.0 | nM | 6.16 |
| CHEMBL358734 | — | IC50 | = | 739.0 | nM | 6.13 |
| CHEMBL358804 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL356721 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL357180 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL144266 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL358820 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL144655 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL436072 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL291473 | — | IC50 | > | 1000.0 | nM | - |