Assay Detail
Binding
CHEMBL652363
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Concentration that inhibits binding of 1.5 nM [3H]diazepam to rat brain benzodiazepine receptor
26
Total Activities
26
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
Benzodiazepine receptor binding activity of 6,9-disubstituted purines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 5.28 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 8.22 |
| CHEMBL451 | CHLORDIAZEPOXIDE | 4.0 | 1 | 6.70 |
| CHEMBL7474 | — | — | 1 | 6.36 |
| CHEMBL7344 | — | — | 1 | 6.05 |
| CHEMBL7293 | — | — | 1 | 5.92 |
| CHEMBL7553 | — | — | 1 | 5.80 |
| CHEMBL275514 | — | — | 1 | 5.68 |
| CHEMBL7723 | 9-BENZYL-6-METHYLSULFANYL-9H-PURINE | — | 1 | 5.48 |
| CHEMBL7881 | — | — | 1 | 5.30 |
| CHEMBL6917 | — | — | 1 | 5.27 |
| CHEMBL7141 | — | — | 1 | 5.14 |
| CHEMBL268846 | — | — | 1 | 4.89 |
| CHEMBL6889 | — | — | 1 | 4.89 |
| CHEMBL7729 | — | — | 1 | 4.85 |
| CHEMBL7446 | 9-BENZYL-6-METHOXY-9H-PURINE | — | 1 | 4.85 |
| CHEMBL266675 | — | — | 1 | 4.82 |
| CHEMBL7504 | — | — | 1 | 4.81 |
| CHEMBL7230 | — | — | 1 | 4.80 |
| CHEMBL268102 | — | — | 1 | 4.77 |
| CHEMBL267851 | — | — | 1 | 4.72 |
| CHEMBL266919 | — | — | 1 | 4.72 |
| CHEMBL293310 | — | — | 1 | 4.72 |
| CHEMBL7661 | — | — | 1 | 4.70 |
| CHEMBL7579 | — | — | 1 | 4.66 |
| CHEMBL6565 | — | — | 1 | 4.62 |
| CHEMBL266094 | 9-BENZYL-9H-ADENINE | — | 1 | 4.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL12 | DIAZEPAM | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL451 | CHLORDIAZEPOXIDE | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL7474 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL7344 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL7293 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL7553 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL275514 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL7723 | 9-BENZYL-6-METHYLSULFANYL-9H-PURINE | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL7881 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL6917 | — | IC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL7141 | — | IC50 | = | 7300.0 | nM | 5.14 |
| CHEMBL268846 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL6889 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL7729 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL7446 | 9-BENZYL-6-METHOXY-9H-PURINE | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL266675 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL7504 | — | IC50 | = | 15500.0 | nM | 4.81 |
| CHEMBL7230 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL268102 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL267851 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL266919 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL293310 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL7661 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL7579 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL6565 | — | IC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL266094 | 9-BENZYL-9H-ADENINE | IC50 | = | 37000.0 | nM | 4.43 |