Assay Detail
Binding
CHEMBL2351048
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]Ro15-1788 from GABA-A receptor benzodiazepine binding site in bovine cerebral cortex membranes after 1 hr
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Bos taurus |
| Tissue | Cerebral cortex |
| Subcellular | Membrane |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Synthesis of novel cognition enhancers with pyrazolo[5,1-c][1,2,4]benzotriazine core acting at γ-aminobutyric acid type A (GABA(A)) receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 7.24 | 9.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2348443 | — | — | 1 | 9.64 |
| CHEMBL2348440 | — | — | 1 | 9.48 |
| CHEMBL2348441 | — | — | 1 | 9.48 |
| CHEMBL2348442 | — | — | 1 | 9.14 |
| CHEMBL2348447 | — | — | 1 | 8.13 |
| CHEMBL2348444 | — | — | 1 | 7.69 |
| CHEMBL2348446 | — | — | 1 | 7.62 |
| CHEMBL2348448 | — | — | 1 | 7.51 |
| CHEMBL2348533 | — | — | 1 | 7.15 |
| CHEMBL2348539 | — | — | 1 | 7.06 |
| CHEMBL2348543 | — | — | 1 | 6.78 |
| CHEMBL2181577 | — | — | 1 | 6.50 |
| CHEMBL2348536 | — | — | 1 | 6.49 |
| CHEMBL2348542 | — | — | 1 | 6.49 |
| CHEMBL2348445 | — | — | 1 | 6.40 |
| CHEMBL2348534 | — | — | 1 | 6.34 |
| CHEMBL2348540 | — | — | 1 | 6.29 |
| CHEMBL2348541 | — | — | 1 | 6.21 |
| CHEMBL2348538 | — | — | 1 | 6.02 |
| CHEMBL2348537 | — | — | 1 | 5.92 |
| CHEMBL2348535 | — | — | 1 | 5.79 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2348443 | — | Ki | = | 0.23 | nM | 9.64 |
| CHEMBL2348440 | — | Ki | = | 0.33 | nM | 9.48 |
| CHEMBL2348441 | — | Ki | = | 0.33 | nM | 9.48 |
| CHEMBL2348442 | — | Ki | = | 0.72 | nM | 9.14 |
| CHEMBL2348447 | — | Ki | = | 7.49 | nM | 8.13 |
| CHEMBL2348444 | — | Ki | = | 20.4 | nM | 7.69 |
| CHEMBL2348446 | — | Ki | = | 24.1 | nM | 7.62 |
| CHEMBL2348448 | — | Ki | = | 30.9 | nM | 7.51 |
| CHEMBL2348533 | — | Ki | = | 70.7 | nM | 7.15 |
| CHEMBL2348539 | — | Ki | = | 86.6 | nM | 7.06 |
| CHEMBL2348543 | — | Ki | = | 167.9 | nM | 6.78 |
| CHEMBL2181577 | — | Ki | = | 315.0 | nM | 6.50 |
| CHEMBL2348536 | — | Ki | = | 323.7 | nM | 6.49 |
| CHEMBL2348542 | — | Ki | = | 325.2 | nM | 6.49 |
| CHEMBL2348445 | — | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL2348534 | — | Ki | = | 453.2 | nM | 6.34 |
| CHEMBL2348540 | — | Ki | = | 514.8 | nM | 6.29 |
| CHEMBL2348541 | — | Ki | = | 620.0 | nM | 6.21 |
| CHEMBL2348538 | — | Ki | = | 959.6 | nM | 6.02 |
| CHEMBL2348537 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL2348535 | — | Ki | = | 1623.0 | nM | 5.79 |