Assay Detail
Binding
CHEMBL5737147
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Electrophysiology: Electrophysiological experiments were performed on days 3 to 5 after the micro-injection of mRNA. During the experiment the oocytes were constantly superfused by a solution containing (in mM) NaCl 90, KCl 1, HEPES 5, MgCl2 1, CaCl2 1 (pH 7.4). Oocytes were impaled by two glass microelectrodes (resistance: 0.4 MΩ) which were filled with a solution containing KCl 1M+K-acetate 1.5 M and voltage-clamped to −80 mV. The recordings were performed at room temperature using the Roboocyte two-electrode voltage clamp system (Multichannelsystem). After an initial equilibration period of 1.5 min GABA was added for 1.5 min at a concentration evoking approximately 20% of a maximal current response (EC20). After another rest interval of 2.5 min GABA was again added evoking a response of similar amplitude and shape. 0.5 min after the onset of this second GABA application the test compound, at a concentration corresponding to approximatively 30 fold its Ki, was added while GABA was still present. Current traces were recorded at a digitization rate of 10 Hz during and shortly before and after the GABA application.
585
Total Activities
193
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Gamma-aminobutyric acid receptor subunit alpha-1 (CHEMBL1962) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Isoxazolyl ether derivatives as GABAA α5 PAM
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 195 | 7.85 | 9.40 |
| kon | 195 | - | - |
| k_off | 195 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5771253 | — | — | 3 | 9.40 |
| CHEMBL6038200 | — | — | 3 | 9.10 |
| CHEMBL6063116 | — | — | 3 | 9.00 |
| CHEMBL5808514 | — | — | 3 | 8.92 |
| CHEMBL6003049 | — | — | 3 | 8.85 |
| CHEMBL6060527 | — | — | 3 | 8.62 |
| CHEMBL5845026 | — | — | 3 | 8.59 |
| CHEMBL6062914 | — | — | 3 | 8.52 |
| CHEMBL5952606 | — | — | 3 | 8.46 |
| CHEMBL5776143 | — | — | 3 | 8.36 |
| CHEMBL6016406 | — | — | 3 | 8.34 |
| CHEMBL5971033 | — | — | 3 | 8.34 |
| CHEMBL5841019 | — | — | 3 | 8.33 |
| CHEMBL5960872 | — | — | 3 | 8.32 |
| CHEMBL5978694 | — | — | 3 | 8.31 |
| CHEMBL5880547 | — | — | 3 | 8.30 |
| CHEMBL5869614 | — | — | 3 | 8.30 |
| CHEMBL5986198 | — | — | 3 | 8.28 |
| CHEMBL6046793 | — | — | 3 | 8.28 |
| CHEMBL5759279 | — | — | 3 | 8.28 |
| CHEMBL5895042 | — | — | 3 | 8.28 |
| CHEMBL6024468 | — | — | 3 | 8.27 |
| CHEMBL5845333 | — | — | 3 | 8.26 |
| CHEMBL5798454 | — | — | 3 | 8.26 |
| CHEMBL6046677 | — | — | 3 | 8.24 |
| CHEMBL5951376 | — | — | 3 | 8.24 |
| CHEMBL6011117 | — | — | 3 | 8.22 |
| CHEMBL5985273 | — | — | 3 | 8.21 |
| CHEMBL5805665 | — | — | 3 | 8.21 |
| CHEMBL5917239 | — | — | 3 | 8.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5771253 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL6038200 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL6063116 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL5808514 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL6003049 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL6060527 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL5845026 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL6062914 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL5952606 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL5776143 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL5971033 | — | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL6016406 | — | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL5841019 | — | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL5960872 | — | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL5978694 | — | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL5880547 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL5869614 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL5895042 | — | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL5986198 | — | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL6046793 | — | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL5759279 | — | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL6024468 | — | Ki | = | 5.4 | nM | 8.27 |
| CHEMBL5798454 | — | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL5845333 | — | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL5951376 | — | Ki | = | 5.8 | nM | 8.24 |
| CHEMBL6046677 | — | Ki | = | 5.8 | nM | 8.24 |
| CHEMBL6011117 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL5805665 | — | Ki | = | 6.1 | nM | 8.21 |
| CHEMBL5985273 | — | Ki | = | 6.2 | nM | 8.21 |
| CHEMBL5917239 | — | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL5822054 | — | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL5899241 | — | Ki | = | 6.6 | nM | 8.18 |
| CHEMBL6021494 | — | Ki | = | 6.8 | nM | 8.17 |
| CHEMBL5741267 | — | Ki | = | 7.1 | nM | 8.15 |
| CHEMBL5771391 | — | Ki | = | 7.2 | nM | 8.14 |
| CHEMBL5805945 | — | Ki | = | 7.3 | nM | 8.14 |
| CHEMBL6014829 | — | Ki | = | 7.2 | nM | 8.14 |
| CHEMBL5980072 | — | Ki | = | 7.2 | nM | 8.14 |
| CHEMBL6013523 | — | Ki | = | 7.6 | nM | 8.12 |
| CHEMBL5926555 | — | Ki | = | 7.6 | nM | 8.12 |
| CHEMBL5911837 | — | Ki | = | 7.6 | nM | 8.12 |
| CHEMBL5751783 | — | Ki | = | 7.5 | nM | 8.12 |
| CHEMBL5747907 | — | Ki | = | 7.8 | nM | 8.11 |
| CHEMBL6063739 | — | Ki | = | 7.7 | nM | 8.11 |
| CHEMBL5934990 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL5956891 | — | Ki | = | 7.9 | nM | 8.10 |
| CHEMBL5764050 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL5812257 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL5965541 | — | Ki | = | 8.1 | nM | 8.09 |
| CHEMBL5920931 | — | Ki | = | 8.3 | nM | 8.08 |