Assay Detail
Binding
CHEMBL651949
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In vitro potency measured against [3H]diazepam at the benzodiazepine receptor in rat
38
Total Activities
38
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 of substituted 7,12-dihydropyrido[3,2-b:5,4-b']diindoles: rigid planar benzodiazepine receptor ligands with inverse agonist/antagonist properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 38 | 7.01 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL78766 | — | — | 1 | 8.40 |
| CHEMBL301605 | — | — | 1 | 8.40 |
| CHEMBL310167 | — | — | 1 | 8.22 |
| CHEMBL311776 | — | — | 1 | 8.22 |
| CHEMBL78400 | — | — | 1 | 8.22 |
| CHEMBL79945 | — | — | 1 | 8.15 |
| CHEMBL66273 | — | — | 1 | 8.10 |
| CHEMBL539273 | — | — | 1 | 8.10 |
| CHEMBL439945 | — | — | 1 | 8.00 |
| CHEMBL311747 | — | — | 1 | 7.92 |
| CHEMBL443010 | — | — | 1 | 7.72 |
| CHEMBL554973 | — | — | 1 | 7.55 |
| CHEMBL78434 | — | — | 1 | 7.36 |
| CHEMBL78650 | — | — | 1 | 7.10 |
| CHEMBL542892 | — | — | 1 | 7.08 |
| CHEMBL81512 | — | — | 1 | 7.01 |
| CHEMBL81479 | — | — | 1 | 6.94 |
| CHEMBL79887 | — | — | 1 | 6.90 |
| CHEMBL554853 | — | — | 1 | 6.80 |
| CHEMBL544303 | — | — | 1 | 6.65 |
| CHEMBL67774 | — | — | 1 | 6.60 |
| CHEMBL557822 | — | — | 1 | 6.60 |
| CHEMBL78378 | — | — | 1 | 6.51 |
| CHEMBL312628 | — | — | 1 | 6.24 |
| CHEMBL302056 | — | — | 1 | 6.15 |
| CHEMBL554237 | — | — | 1 | 6.12 |
| CHEMBL541060 | — | — | 1 | 6.05 |
| CHEMBL541562 | — | — | 1 | 5.95 |
| CHEMBL78524 | — | — | 1 | 5.92 |
| CHEMBL82601 | — | — | 1 | 5.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL78766 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL301605 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL311776 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL78400 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL310167 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL79945 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL66273 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL539273 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL439945 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL311747 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL443010 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL554973 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL78434 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL78650 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL542892 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL81512 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL81479 | — | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL79887 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL554853 | — | IC50 | = | 157.0 | nM | 6.80 |
| CHEMBL544303 | — | IC50 | = | 224.0 | nM | 6.65 |
| CHEMBL557822 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL67774 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL78378 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL312628 | — | IC50 | = | 578.0 | nM | 6.24 |
| CHEMBL302056 | — | IC50 | = | 715.0 | nM | 6.15 |
| CHEMBL554237 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL541060 | — | IC50 | = | 890.0 | nM | 6.05 |
| CHEMBL541562 | — | IC50 | = | 1136.0 | nM | 5.95 |
| CHEMBL78524 | — | IC50 | = | 1190.0 | nM | 5.92 |
| CHEMBL82601 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL545709 | — | IC50 | = | 1970.0 | nM | 5.71 |
| CHEMBL312333 | — | IC50 | = | 2150.0 | nM | 5.67 |
| CHEMBL311172 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL552846 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL311594 | — | IC50 | > | 320.0 | nM | - |
| CHEMBL312596 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL422592 | — | IC50 | > | 350.0 | nM | - |
| CHEMBL431973 | — | IC50 | > | 4000.0 | nM | - |