Assay Detail
Binding
CHEMBL853517
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Inhibition of [3H]Ro15-1788 binding to human recombinant GABA-Aalpha3 plus beta-3-gamma-2 receptor expressed in L(tk-) cells
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
GABA-A receptor; alpha-3/beta-3/gamma-2 (CHEMBL2094120) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
2,3,7-Trisubstituted pyrazolo[1,5-d][1,2,4]triazines: functionally selective GABAA alpha3-subtype agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 37 | 8.95 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL378761 | — | — | 1 | 10.00 |
| CHEMBL211704 | — | — | 1 | 10.00 |
| CHEMBL380110 | — | — | 1 | 9.96 |
| CHEMBL212008 | — | — | 1 | 9.85 |
| CHEMBL377556 | — | — | 1 | 9.70 |
| CHEMBL209556 | — | — | 1 | 9.55 |
| CHEMBL208794 | — | — | 1 | 9.44 |
| CHEMBL210510 | — | — | 1 | 9.35 |
| CHEMBL212323 | — | — | 1 | 9.28 |
| CHEMBL208844 | — | — | 1 | 9.27 |
| CHEMBL379973 | — | — | 1 | 9.26 |
| CHEMBL208940 | — | — | 1 | 9.21 |
| CHEMBL382198 | — | — | 1 | 9.11 |
| CHEMBL378217 | — | — | 1 | 9.07 |
| CHEMBL211293 | — | — | 1 | 9.03 |
| CHEMBL377187 | — | — | 1 | 9.01 |
| CHEMBL379317 | — | — | 1 | 8.96 |
| CHEMBL210400 | — | — | 1 | 8.96 |
| CHEMBL212158 | — | — | 1 | 8.92 |
| CHEMBL212273 | — | — | 1 | 8.89 |
| CHEMBL208998 | — | — | 1 | 8.85 |
| CHEMBL211286 | — | — | 1 | 8.82 |
| CHEMBL379996 | — | — | 1 | 8.80 |
| CHEMBL208687 | — | — | 1 | 8.80 |
| CHEMBL376975 | — | — | 1 | 8.70 |
| CHEMBL208863 | — | — | 1 | 8.59 |
| CHEMBL211506 | — | — | 1 | 8.57 |
| CHEMBL212637 | — | — | 1 | 8.57 |
| CHEMBL426860 | — | — | 1 | 8.20 |
| CHEMBL210769 | — | — | 1 | 8.18 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL378761 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL211704 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL380110 | — | Ki | = | 0.11 | nM | 9.96 |
| CHEMBL212008 | — | Ki | = | 0.14 | nM | 9.85 |
| CHEMBL377556 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL209556 | — | Ki | = | 0.28 | nM | 9.55 |
| CHEMBL208794 | — | Ki | = | 0.36 | nM | 9.44 |
| CHEMBL210510 | — | Ki | = | 0.45 | nM | 9.35 |
| CHEMBL212323 | — | Ki | = | 0.52 | nM | 9.28 |
| CHEMBL208844 | — | Ki | = | 0.54 | nM | 9.27 |
| CHEMBL379973 | — | Ki | = | 0.55 | nM | 9.26 |
| CHEMBL208940 | — | Ki | = | 0.61 | nM | 9.21 |
| CHEMBL382198 | — | Ki | = | 0.77 | nM | 9.11 |
| CHEMBL378217 | — | Ki | = | 0.85 | nM | 9.07 |
| CHEMBL211293 | — | Ki | = | 0.94 | nM | 9.03 |
| CHEMBL377187 | — | Ki | = | 0.98 | nM | 9.01 |
| CHEMBL379317 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL210400 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL212158 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL212273 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL208998 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL211286 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL379996 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL208687 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL376975 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL208863 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL211506 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL212637 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL426860 | — | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL210769 | — | Ki | = | 6.6 | nM | 8.18 |
| CHEMBL212052 | — | Ki | = | 8.7 | nM | 8.06 |
| CHEMBL379788 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL377533 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL378216 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL210631 | — | Ki | > | 33.0 | nM | - |
| CHEMBL211115 | — | Ki | > | 33.0 | nM | - |
| CHEMBL378201 | — | Ki | > | 33.0 | nM | - |