Assay Detail
Binding
CHEMBL652562
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In vitro inhibition of [3H]diazepam binding to benzodiazepine receptor in rat cerebral cortical membrane
52
Total Activities
48
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
Beta-carbolines: synthesis and neurochemical and pharmacological actions on brain benzodiazepine receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 52 | 6.16 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL274847 | — | — | 1 | 9.00 |
| CHEMBL453066 | BETA-CCM | — | 1 | 8.98 |
| CHEMBL11709 | — | — | 1 | 8.96 |
| CHEMBL11575 | — | — | 1 | 8.57 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 8.30 |
| CHEMBL11863 | — | — | 1 | 7.24 |
| CHEMBL12040 | — | — | 1 | 7.21 |
| CHEMBL11901 | — | — | 2 | 6.29 |
| CHEMBL11568 | — | — | 1 | 6.24 |
| CHEMBL417982 | — | — | 1 | 5.83 |
| CHEMBL275224 | NORHARMANE | — | 1 | 5.79 |
| CHEMBL11753 | — | — | 1 | 5.50 |
| CHEMBL273491 | — | — | 1 | 5.41 |
| CHEMBL12065 | — | — | 1 | 5.35 |
| CHEMBL11847 | — | — | 1 | 5.24 |
| CHEMBL442956 | — | — | 1 | 5.21 |
| CHEMBL12044 | — | — | 1 | 5.20 |
| CHEMBL12063 | — | — | 1 | 5.12 |
| CHEMBL12014 | HARMAN | — | 1 | 4.91 |
| CHEMBL416152 | — | — | 1 | 4.88 |
| CHEMBL11908 | — | — | 1 | 4.62 |
| CHEMBL12516 | — | — | 2 | 4.41 |
| CHEMBL12578 | — | — | 2 | 4.27 |
| CHEMBL273939 | — | — | 1 | - |
| CHEMBL268493 | NICOTINALDEHYDE | — | 1 | - |
| CHEMBL11934 | — | — | 1 | - |
| CHEMBL11912 | — | — | 1 | - |
| CHEMBL11945 | — | — | 1 | - |
| CHEMBL12092 | — | — | 1 | - |
| CHEMBL274821 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL274847 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL453066 | BETA-CCM | Ki | = | 1.05 | nM | 8.98 |
| CHEMBL11709 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL11575 | — | Ki | = | 2.66 | nM | 8.57 |
| CHEMBL12 | DIAZEPAM | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL11863 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL12040 | — | Ki | = | 62.3 | nM | 7.21 |
| CHEMBL11901 | — | Ki | = | 510.0 | nM | 6.29 |
| CHEMBL11568 | — | Ki | = | 573.0 | nM | 6.24 |
| CHEMBL417982 | — | Ki | = | 1470.0 | nM | 5.83 |
| CHEMBL275224 | NORHARMANE | Ki | = | 1620.0 | nM | 5.79 |
| CHEMBL11753 | — | Ki | = | 3160.0 | nM | 5.50 |
| CHEMBL273491 | — | Ki | = | 3890.0 | nM | 5.41 |
| CHEMBL12065 | — | Ki | = | 4500.0 | nM | 5.35 |
| CHEMBL11901 | — | Ki | = | 5000.0 | nM | 5.30 |
| CHEMBL11847 | — | Ki | = | 5780.0 | nM | 5.24 |
| CHEMBL442956 | — | Ki | = | 6110.0 | nM | 5.21 |
| CHEMBL12044 | — | Ki | = | 6250.0 | nM | 5.20 |
| CHEMBL12063 | — | Ki | = | 7540.0 | nM | 5.12 |
| CHEMBL12014 | HARMAN | Ki | = | 12400.0 | nM | 4.91 |
| CHEMBL416152 | — | Ki | = | 13200.0 | nM | 4.88 |
| CHEMBL11908 | — | Ki | = | 24000.0 | nM | 4.62 |
| CHEMBL12516 | — | Ki | = | 39000.0 | nM | 4.41 |
| CHEMBL12578 | — | Ki | = | 54000.0 | nM | 4.27 |
| CHEMBL12053 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL273276 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL11852 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL12328 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL12315 | ISOQUINOLINE | Ki | > | 100000.0 | nM | - |
| CHEMBL274794 | 2-PYRIDINECARBOXALDEHYDE | Ki | > | 100000.0 | nM | - |
| CHEMBL12367 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL275098 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL416526 | BUFOTENINE | Ki | > | 100000.0 | nM | - |
| CHEMBL12516 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL11862 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL12327 | — | Ki | > | 50000.0 | nM | - |
| CHEMBL12239 | — | Ki | > | 50000.0 | nM | - |
| CHEMBL12350 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL11991 | — | Ki | = | 250000.0 | nM | - |
| CHEMBL12540 | — | Ki | > | 250000.0 | nM | - |
| CHEMBL12328 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL275804 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL12578 | — | Ki | = | 174000.0 | nM | - |
| CHEMBL274821 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL12092 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL11912 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL268493 | NICOTINALDEHYDE | Ki | > | 100000.0 | nM | - |
| CHEMBL11934 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL11945 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL273939 | — | Ki | > | 100000.0 | nM | - |