Assay Detail
Binding
CHEMBL858255
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity towards benzodiazepine receptor inverse agonist site by the displacement of [3H]diazepam in rat cerebral cortical membranes.
51
Total Activities
51
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
QSAR's from similarity matrices. Technique validation and application in the comparison of different similarity evaluation methods.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 51 | 7.14 | 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 |
| CHEMBL306208 | — | — | 1 | 8.93 |
| CHEMBL14391 | — | — | 1 | 8.90 |
| CHEMBL82027 | — | — | 1 | 8.77 |
| CHEMBL97887 | — | — | 1 | 8.74 |
| CHEMBL100625 | — | — | 1 | 8.67 |
| CHEMBL69719 | — | — | 1 | 8.55 |
| CHEMBL301605 | — | — | 1 | 8.40 |
| CHEMBL453066 | BETA-CCM | — | 1 | 8.30 |
| CHEMBL11709 | — | — | 1 | 8.30 |
| CHEMBL98271 | — | — | 1 | 8.09 |
| CHEMBL60609 | — | — | 1 | 8.00 |
| CHEMBL66273 | — | — | 1 | 8.00 |
| CHEMBL307783 | — | — | 1 | 8.00 |
| CHEMBL52750 | — | — | 1 | 7.96 |
| CHEMBL317828 | — | — | 1 | 7.88 |
| CHEMBL2079586 | — | — | 1 | 7.80 |
| CHEMBL1790051 | — | — | 1 | 7.64 |
| CHEMBL299250 | — | — | 1 | 7.62 |
| CHEMBL302855 | — | — | 1 | 7.60 |
| CHEMBL298561 | — | — | 1 | 7.35 |
| CHEMBL99750 | — | — | 1 | 7.19 |
| CHEMBL98503 | — | — | 1 | 7.17 |
| CHEMBL66274 | — | — | 1 | 7.08 |
| CHEMBL66902 | — | — | 1 | 7.01 |
| CHEMBL54228 | — | — | 1 | 6.91 |
| CHEMBL53229 | — | — | 1 | 6.90 |
| CHEMBL69336 | — | — | 1 | 6.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3144739 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL19732 | CGS-8216 | IC50 | = | 0.3999 | nM | 9.40 |
| CHEMBL20042 | CGS-9896 | IC50 | = | 0.5998 | nM | 9.22 |
| CHEMBL306208 | — | IC50 | = | 1.175 | nM | 8.93 |
| CHEMBL14391 | — | IC50 | = | 1.259 | nM | 8.90 |
| CHEMBL82027 | — | IC50 | = | 1.698 | nM | 8.77 |
| CHEMBL97887 | — | IC50 | = | 1.82 | nM | 8.74 |
| CHEMBL100625 | — | IC50 | = | 2.138 | nM | 8.67 |
| CHEMBL69719 | — | IC50 | = | 2.799 | nM | 8.55 |
| CHEMBL301605 | — | IC50 | = | 3.999 | nM | 8.40 |
| CHEMBL453066 | BETA-CCM | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL11709 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL98271 | — | IC50 | = | 8.128 | nM | 8.09 |
| CHEMBL66273 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL60609 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL307783 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL52750 | — | IC50 | = | 11.02 | nM | 7.96 |
| CHEMBL317828 | — | IC50 | = | 13.18 | nM | 7.88 |
| CHEMBL2079586 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL1790051 | — | IC50 | = | 22.91 | nM | 7.64 |
| CHEMBL299250 | — | IC50 | = | 23.99 | nM | 7.62 |
| CHEMBL302855 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL298561 | — | IC50 | = | 44.98 | nM | 7.35 |
| CHEMBL99750 | — | IC50 | = | 64.57 | nM | 7.19 |
| CHEMBL98503 | — | IC50 | = | 67.61 | nM | 7.17 |
| CHEMBL66274 | — | IC50 | = | 82.99 | nM | 7.08 |
| CHEMBL66902 | — | IC50 | = | 97.95 | nM | 7.01 |
| CHEMBL54228 | — | IC50 | = | 123.88 | nM | 6.91 |
| CHEMBL53229 | — | IC50 | = | 125.03 | nM | 6.90 |
| CHEMBL69336 | — | IC50 | = | 157.04 | nM | 6.80 |
| CHEMBL304273 | — | IC50 | = | 223.87 | nM | 6.65 |
| CHEMBL69488 | — | IC50 | = | 244.91 | nM | 6.61 |
| CHEMBL67774 | — | IC50 | = | 250.03 | nM | 6.60 |
| CHEMBL99152 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL67421 | — | IC50 | = | 500.03 | nM | 6.30 |
| CHEMBL66487 | — | IC50 | = | 680.77 | nM | 6.17 |
| CHEMBL302056 | — | IC50 | = | 714.5 | nM | 6.15 |
| CHEMBL67951 | — | IC50 | = | 749.89 | nM | 6.12 |
| CHEMBL299060 | — | IC50 | = | 1164.13 | nM | 5.93 |
| CHEMBL275224 | NORHARMANE | IC50 | = | 1621.81 | nM | 5.79 |
| CHEMBL55630 | — | IC50 | = | 1698.24 | nM | 5.77 |
| CHEMBL69282 | — | IC50 | = | 1918.67 | nM | 5.72 |
| CHEMBL53230 | — | IC50 | = | 1972.42 | nM | 5.71 |
| CHEMBL66841 | — | IC50 | = | 2398.83 | nM | 5.62 |
| CHEMBL303932 | — | IC50 | = | 5000.35 | nM | 5.30 |
| CHEMBL69006 | — | IC50 | = | 6854.88 | nM | 5.16 |
| CHEMBL12063 | — | IC50 | = | 7533.56 | nM | 5.12 |
| CHEMBL70086 | — | IC50 | = | 9204.5 | nM | 5.04 |
| CHEMBL12014 | HARMAN | IC50 | = | 12387.97 | nM | 4.91 |
| CHEMBL67772 | — | IC50 | = | 26001.6 | nM | 4.58 |