Assay Detail
Binding
CHEMBL650289
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In vitro inhibition of 3[H]Diazepam binding to Benzodiazepine receptor from rat cerebral cortical membranes
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Subcellular | Membrane |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL1907607) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Synthetic and computer-assisted analyses of the pharmacophore for the benzodiazepine receptor inverse agonist site.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 43 | 6.78 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3144739 | — | — | 1 | 10.00 |
| CHEMBL19732 | CGS-8216 | — | 1 | 9.40 |
| CHEMBL20042 | CGS-9896 | — | 1 | 9.22 |
| CHEMBL69719 | — | — | 1 | 8.55 |
| CHEMBL301605 | — | — | 1 | 8.40 |
| CHEMBL11709 | — | — | 1 | 8.30 |
| CHEMBL453066 | BETA-CCM | — | 1 | 8.30 |
| CHEMBL75373 | — | — | 1 | 8.05 |
| CHEMBL66273 | — | — | 1 | 8.00 |
| CHEMBL307783 | — | — | 1 | 8.00 |
| CHEMBL52750 | — | — | 1 | 7.96 |
| CHEMBL299250 | — | — | 1 | 7.62 |
| CHEMBL298561 | — | — | 1 | 7.35 |
| CHEMBL66274 | — | — | 1 | 7.08 |
| CHEMBL66902 | — | — | 1 | 7.01 |
| CHEMBL307061 | — | — | 1 | 7.00 |
| CHEMBL54228 | — | — | 1 | 6.91 |
| CHEMBL53229 | — | — | 1 | 6.90 |
| CHEMBL69336 | — | — | 1 | 6.80 |
| CHEMBL304273 | — | — | 1 | 6.65 |
| CHEMBL69488 | — | — | 1 | 6.61 |
| CHEMBL67774 | — | — | 1 | 6.60 |
| CHEMBL76724 | — | — | 1 | 6.54 |
| CHEMBL67421 | — | — | 1 | 6.30 |
| CHEMBL78162 | — | — | 1 | 6.18 |
| CHEMBL66487 | — | — | 1 | 6.17 |
| CHEMBL302056 | — | — | 1 | 6.15 |
| CHEMBL67951 | — | — | 1 | 6.12 |
| CHEMBL299060 | — | — | 1 | 5.93 |
| CHEMBL275224 | NORHARMANE | — | 1 | 5.79 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3144739 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL19732 | CGS-8216 | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL20042 | CGS-9896 | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL69719 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL301605 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL11709 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL453066 | BETA-CCM | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL75373 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL66273 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL307783 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL52750 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL299250 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL298561 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL66274 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL66902 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL307061 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL54228 | — | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL53229 | — | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL69336 | — | IC50 | = | 157.0 | nM | 6.80 |
| CHEMBL304273 | — | IC50 | = | 224.0 | nM | 6.65 |
| CHEMBL69488 | — | IC50 | = | 245.0 | nM | 6.61 |
| CHEMBL67774 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL76724 | — | IC50 | = | 285.0 | nM | 6.54 |
| CHEMBL67421 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL78162 | — | IC50 | = | 653.0 | nM | 6.18 |
| CHEMBL66487 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL302056 | — | IC50 | = | 715.0 | nM | 6.15 |
| CHEMBL67951 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL299060 | — | IC50 | = | 1163.0 | nM | 5.93 |
| CHEMBL275224 | NORHARMANE | IC50 | = | 1620.0 | nM | 5.79 |
| CHEMBL55630 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL69282 | — | IC50 | = | 1917.0 | nM | 5.72 |
| CHEMBL53230 | — | IC50 | = | 1970.0 | nM | 5.71 |
| CHEMBL66841 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL75803 | — | IC50 | = | 4660.0 | nM | 5.33 |
| CHEMBL303932 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL69006 | — | IC50 | = | 6860.0 | nM | 5.16 |
| CHEMBL12063 | — | IC50 | = | 7540.0 | nM | 5.12 |
| CHEMBL70086 | — | IC50 | = | 9200.0 | nM | 5.04 |
| CHEMBL12014 | HARMAN | IC50 | = | 12400.0 | nM | 4.91 |
| CHEMBL67772 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL12239 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL441986 | — | IC50 | = | 250000.0 | nM | - |