Assay Detail
Functional
CHEMBL789194
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity was determined by displacement of [3H]flumazenil from rat cortex homogenates
58
Total Activities
57
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| 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 biological evaluation of 7,8,9,10-tetrahydroimidazo[1,2-c]pyrido[3,4-e]pyrimdin-5(6H)-ones as functionally selective ligands of the benzodiazepine receptor site on the GABA(A) receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 58 | 7.80 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL146302 | — | — | 1 | 9.70 |
| CHEMBL356806 | — | — | 1 | 9.30 |
| CHEMBL147364 | — | — | 1 | 9.30 |
| CHEMBL146390 | — | — | 1 | 9.22 |
| CHEMBL146230 | — | — | 1 | 9.05 |
| CHEMBL342270 | — | — | 1 | 9.05 |
| CHEMBL356161 | — | — | 2 | 8.89 |
| CHEMBL146086 | — | — | 1 | 8.85 |
| CHEMBL344120 | — | — | 1 | 8.82 |
| CHEMBL147842 | — | — | 1 | 8.77 |
| CHEMBL357710 | — | — | 1 | 8.77 |
| CHEMBL343009 | — | — | 1 | 8.70 |
| CHEMBL146356 | — | — | 1 | 8.64 |
| CHEMBL356271 | — | — | 1 | 8.59 |
| CHEMBL356074 | — | — | 1 | 8.54 |
| CHEMBL148043 | — | — | 1 | 8.52 |
| CHEMBL147590 | — | — | 1 | 8.49 |
| CHEMBL661 | ALPRAZOLAM | 4.0 | 1 | 8.48 |
| CHEMBL2112010 | — | — | 1 | 8.19 |
| CHEMBL146317 | — | — | 1 | 8.18 |
| CHEMBL147379 | — | — | 1 | 8.14 |
| CHEMBL148574 | — | — | 1 | 8.08 |
| CHEMBL148740 | — | — | 1 | 8.06 |
| CHEMBL358874 | — | — | 1 | 8.00 |
| CHEMBL145983 | — | — | 1 | 7.95 |
| CHEMBL145910 | — | — | 1 | 7.94 |
| CHEMBL343471 | — | — | 1 | 7.87 |
| CHEMBL149900 | — | — | 1 | 7.83 |
| CHEMBL148044 | — | — | 1 | 7.68 |
| CHEMBL358301 | — | — | 1 | 7.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL146302 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL356806 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL147364 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL146390 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL146230 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL342270 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL356161 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL356161 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL146086 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL344120 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL357710 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL147842 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL343009 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL146356 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL356271 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL356074 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL148043 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL147590 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL661 | ALPRAZOLAM | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL2112010 | — | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL146317 | — | Ki | = | 6.6 | nM | 8.18 |
| CHEMBL147379 | — | Ki | = | 7.3 | nM | 8.14 |
| CHEMBL148574 | — | Ki | = | 8.3 | nM | 8.08 |
| CHEMBL148740 | — | Ki | = | 8.7 | nM | 8.06 |
| CHEMBL358874 | — | Ki | = | 10.1 | nM | 8.00 |
| CHEMBL145983 | — | Ki | = | 11.3 | nM | 7.95 |
| CHEMBL145910 | — | Ki | = | 11.4 | nM | 7.94 |
| CHEMBL343471 | — | Ki | = | 13.6 | nM | 7.87 |
| CHEMBL149900 | — | Ki | = | 14.9 | nM | 7.83 |
| CHEMBL148044 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL358301 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL145970 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL146075 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL149549 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL147312 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL146635 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL911 | ZOLPIDEM | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL147161 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL147217 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL148737 | — | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL147771 | — | Ki | = | 71.0 | nM | 7.15 |
| CHEMBL344534 | — | Ki | = | 73.0 | nM | 7.14 |
| CHEMBL149504 | — | Ki | = | 72.0 | nM | 7.14 |
| CHEMBL357417 | — | Ki | = | 83.0 | nM | 7.08 |
| CHEMBL146051 | — | Ki | = | 83.0 | nM | 7.08 |
| CHEMBL148891 | — | Ki | = | 92.0 | nM | 7.04 |
| CHEMBL359234 | — | Ki | = | 121.0 | nM | 6.92 |
| CHEMBL146577 | — | Ki | = | 123.0 | nM | 6.91 |
| CHEMBL146488 | — | Ki | = | 133.0 | nM | 6.88 |
| CHEMBL342309 | — | Ki | = | 147.0 | nM | 6.83 |