Assay Detail
Binding
CHEMBL652364
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]flunitrazepam binding to GABA-A benzodiazepine receptor of rat cerebral cortex
62
Total Activities
62
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Cerebral cortex |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL1907607) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Synthesis and structure-activity relationships of a series of anxioselective pyrazolopyridine ester and amide anxiolytic agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 62 | 7.10 | 8.26 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL315351 | — | — | 1 | 8.26 |
| CHEMBL85605 | — | — | 1 | 8.24 |
| CHEMBL312907 | — | — | 1 | 8.24 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 8.22 |
| CHEMBL83571 | — | — | 1 | 8.19 |
| CHEMBL85794 | — | — | 1 | 8.07 |
| CHEMBL314580 | — | — | 1 | 8.01 |
| CHEMBL87790 | — | — | 1 | 8.00 |
| CHEMBL83627 | — | — | 1 | 7.89 |
| CHEMBL87993 | — | — | 1 | 7.80 |
| CHEMBL86444 | — | — | 1 | 7.80 |
| CHEMBL85911 | — | — | 1 | 7.68 |
| CHEMBL87645 | — | — | 1 | 7.68 |
| CHEMBL421157 | — | — | 1 | 7.66 |
| CHEMBL83349 | — | — | 1 | 7.55 |
| CHEMBL86024 | — | — | 1 | 7.51 |
| CHEMBL87973 | — | — | 1 | 7.46 |
| CHEMBL316194 | — | — | 1 | 7.44 |
| CHEMBL314482 | — | — | 1 | 7.41 |
| CHEMBL313549 | — | — | 1 | 7.30 |
| CHEMBL315768 | — | — | 1 | 7.30 |
| CHEMBL314152 | — | — | 1 | 7.29 |
| CHEMBL83085 | — | — | 1 | 7.28 |
| CHEMBL86293 | — | — | 1 | 7.27 |
| CHEMBL87979 | — | — | 1 | 7.24 |
| CHEMBL87662 | — | — | 1 | 7.22 |
| CHEMBL87264 | — | — | 1 | 7.16 |
| CHEMBL431022 | — | — | 1 | 7.10 |
| CHEMBL87358 | — | — | 1 | 7.10 |
| CHEMBL86616 | — | — | 1 | 7.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL315351 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL85605 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL312907 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL12 | DIAZEPAM | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL83571 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL85794 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL314580 | — | IC50 | = | 9.7 | nM | 8.01 |
| CHEMBL87790 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL83627 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL87993 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL86444 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL85911 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL87645 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL421157 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL83349 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL86024 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL87973 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL316194 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL314482 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL313549 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL315768 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL314152 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL83085 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL86293 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL87979 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL87662 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL87264 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL431022 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL87358 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL86616 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL88106 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL431020 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL316149 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL420053 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL85260 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL86463 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL83453 | — | IC50 | = | 113.0 | nM | 6.95 |
| CHEMBL87290 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL86611 | — | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL87272 | — | IC50 | = | 131.0 | nM | 6.88 |
| CHEMBL442753 | — | IC50 | = | 137.0 | nM | 6.86 |
| CHEMBL315700 | — | IC50 | = | 156.0 | nM | 6.81 |
| CHEMBL314648 | — | IC50 | = | 156.0 | nM | 6.81 |
| CHEMBL85701 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL86459 | — | IC50 | = | 174.0 | nM | 6.76 |
| CHEMBL86557 | — | IC50 | = | 271.0 | nM | 6.57 |
| CHEMBL87027 | — | IC50 | = | 302.0 | nM | 6.52 |
| CHEMBL315080 | — | IC50 | = | 312.0 | nM | 6.51 |
| CHEMBL86556 | — | IC50 | = | 315.0 | nM | 6.50 |
| CHEMBL87978 | — | IC50 | = | 320.0 | nM | 6.50 |