Assay Detail
Binding
CHEMBL650874
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Binding affinity measured by [3H]diazepam binding assay in rat
32
Total Activities
32
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
2-benzazepines. 5. Synthesis of pyrimido[5,4-d][2]benzazepines and their evaluation as anxiolytic agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 32 | 7.85 | 8.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL40447 | — | — | 1 | 8.64 |
| CHEMBL289742 | — | — | 1 | 8.59 |
| CHEMBL41816 | — | — | 1 | 8.55 |
| CHEMBL296578 | — | — | 1 | 8.55 |
| CHEMBL40906 | — | — | 1 | 8.55 |
| CHEMBL40721 | — | — | 1 | 8.51 |
| CHEMBL39418 | — | — | 1 | 8.47 |
| CHEMBL41553 | — | — | 1 | 8.46 |
| CHEMBL289774 | — | — | 1 | 8.28 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 8.27 |
| CHEMBL40446 | — | — | 1 | 8.15 |
| CHEMBL290057 | — | — | 1 | 8.12 |
| CHEMBL44515 | — | — | 1 | 8.09 |
| CHEMBL43683 | — | — | 1 | 8.04 |
| CHEMBL41856 | — | — | 1 | 8.02 |
| CHEMBL42927 | — | — | 1 | 8.02 |
| CHEMBL288397 | — | — | 1 | 7.82 |
| CHEMBL43572 | — | — | 1 | 7.77 |
| CHEMBL40905 | — | — | 1 | 7.77 |
| CHEMBL40507 | — | — | 1 | 7.73 |
| CHEMBL442346 | — | — | 1 | 7.70 |
| CHEMBL42951 | — | — | 1 | 7.60 |
| CHEMBL289201 | — | — | 1 | 7.60 |
| CHEMBL290905 | — | — | 1 | 7.52 |
| CHEMBL290636 | — | — | 1 | 7.51 |
| CHEMBL39034 | — | — | 1 | 7.42 |
| CHEMBL40660 | — | — | 1 | 7.27 |
| CHEMBL38917 | — | — | 1 | 7.27 |
| CHEMBL289174 | — | — | 1 | 7.22 |
| CHEMBL289819 | — | — | 1 | 6.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL40447 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL289742 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL41816 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL296578 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL40906 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL40721 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL39418 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL41553 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL289774 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL12 | DIAZEPAM | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL40446 | — | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL290057 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL44515 | — | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL43683 | — | IC50 | = | 9.2 | nM | 8.04 |
| CHEMBL42927 | — | IC50 | = | 9.6 | nM | 8.02 |
| CHEMBL41856 | — | IC50 | = | 9.6 | nM | 8.02 |
| CHEMBL288397 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL43572 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL40905 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL40507 | — | IC50 | = | 18.5 | nM | 7.73 |
| CHEMBL442346 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL42951 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL289201 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL290905 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL290636 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL39034 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL40660 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL38917 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL289174 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL289819 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL42809 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL290064 | — | IC50 | = | 490.0 | nM | 6.31 |