Assay Detail
Binding
CHEMBL677943
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro affinity for BZD site on GABA-A receptor from rat cerebral cortex using radioligand [3H]flunitrazepam
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Cerebral cortex |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL1907607) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Potential anxiolytic agents. Part 4: novel orally-active N(5)-substituted pyrido[1,2-a]benzimidazoles with high GABA-A receptor affinity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 36 | 8.68 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL80436 | — | — | 1 | 10.00 |
| CHEMBL310775 | — | — | 1 | 9.70 |
| CHEMBL78641 | — | — | 1 | 9.52 |
| CHEMBL421142 | — | — | 1 | 9.52 |
| CHEMBL312696 | — | — | 1 | 9.40 |
| CHEMBL80890 | — | — | 1 | 9.30 |
| CHEMBL445108 | — | — | 1 | 9.30 |
| CHEMBL76097 | — | — | 1 | 9.30 |
| CHEMBL411744 | — | — | 1 | 9.22 |
| CHEMBL306360 | — | — | 1 | 9.15 |
| CHEMBL421707 | — | — | 1 | 9.15 |
| CHEMBL419842 | — | — | 1 | 9.10 |
| CHEMBL310786 | — | — | 1 | 9.05 |
| CHEMBL445109 | — | — | 1 | 9.00 |
| CHEMBL79821 | — | — | 1 | 9.00 |
| CHEMBL309857 | — | — | 1 | 8.96 |
| CHEMBL80957 | — | — | 1 | 8.92 |
| CHEMBL80721 | — | — | 1 | 8.92 |
| CHEMBL80308 | — | — | 1 | 8.85 |
| CHEMBL310299 | — | — | 1 | 8.80 |
| CHEMBL289181 | — | — | 1 | 8.72 |
| CHEMBL75739 | — | — | 1 | 8.66 |
| CHEMBL81528 | — | — | 1 | 8.64 |
| CHEMBL80947 | — | — | 1 | 8.48 |
| CHEMBL76197 | — | — | 1 | 8.37 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 8.31 |
| CHEMBL311396 | — | — | 1 | 8.29 |
| CHEMBL418915 | — | — | 1 | 8.25 |
| CHEMBL368093 | — | — | 1 | 8.21 |
| CHEMBL307736 | — | — | 1 | 8.13 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL80436 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL310775 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL421142 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL78641 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL312696 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL80890 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL445108 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL76097 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL411744 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL421707 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL306360 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL419842 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL310786 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL445109 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL79821 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL309857 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL80957 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL80721 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL80308 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL310299 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL289181 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL75739 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL81528 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL80947 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL76197 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL12 | DIAZEPAM | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL311396 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL418915 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL368093 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL307736 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL75626 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL78477 | — | IC50 | = | 13.3 | nM | 7.88 |
| CHEMBL79382 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL76728 | — | IC50 | = | 49.9 | nM | 7.30 |
| CHEMBL78849 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL311558 | — | IC50 | = | 151.0 | nM | 6.82 |