Assay Detail
Binding
CHEMBL861280
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]Ro 15-1788 from recombinant human GABA-Aalpha1 receptor plus beta-3-gamma-2 expressed in L(tk-) cells
20
Total Activities
20
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-1/beta-3/gamma-2 (CHEMBL2094121) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Imidazo[1,2-a]pyrimidines as functionally selective GABA(A) ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 20 | 8.70 | 9.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL203769 | — | — | 1 | 9.51 |
| CHEMBL203768 | — | — | 1 | 9.51 |
| CHEMBL203591 | — | — | 1 | 9.44 |
| CHEMBL199689 | — | — | 1 | 9.18 |
| CHEMBL204390 | — | — | 1 | 9.03 |
| CHEMBL204400 | — | — | 1 | 9.00 |
| CHEMBL380945 | — | — | 1 | 9.00 |
| CHEMBL383106 | — | — | 1 | 8.92 |
| CHEMBL381625 | — | — | 1 | 8.72 |
| CHEMBL204041 | — | — | 1 | 8.60 |
| CHEMBL379467 | — | — | 1 | 8.24 |
| CHEMBL445401 | — | — | 1 | 8.08 |
| CHEMBL380715 | — | — | 1 | 8.04 |
| CHEMBL204194 | — | — | 1 | 7.75 |
| CHEMBL383467 | — | — | 1 | 7.54 |
| CHEMBL204142 | — | — | 1 | - |
| CHEMBL383252 | — | — | 1 | - |
| CHEMBL203985 | — | — | 1 | - |
| CHEMBL381352 | — | — | 1 | - |
| CHEMBL203652 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL203769 | — | Ki | = | 0.31 | nM | 9.51 |
| CHEMBL203768 | — | Ki | = | 0.31 | nM | 9.51 |
| CHEMBL203591 | — | Ki | = | 0.36 | nM | 9.44 |
| CHEMBL199689 | — | Ki | = | 0.66 | nM | 9.18 |
| CHEMBL204390 | — | Ki | = | 0.93 | nM | 9.03 |
| CHEMBL204400 | — | Ki | = | 0.99 | nM | 9.00 |
| CHEMBL380945 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL383106 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL381625 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL204041 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL379467 | — | Ki | = | 5.8 | nM | 8.24 |
| CHEMBL445401 | — | Ki | = | 8.3 | nM | 8.08 |
| CHEMBL380715 | — | Ki | = | 9.1 | nM | 8.04 |
| CHEMBL204194 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL383467 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL204142 | — | Ki | > | 33.0 | nM | - |
| CHEMBL383252 | — | Ki | > | 33.0 | nM | - |
| CHEMBL203985 | — | Ki | > | 33.0 | nM | - |
| CHEMBL381352 | — | Ki | > | 33.0 | nM | - |
| CHEMBL203652 | — | Ki | > | 33.0 | nM | - |