Assay Detail
Binding
CHEMBL864004
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]Ro-151788 from human recombinant GABAA alpha3 in combination with beta3gamma2 expressed in L(tk-) cells
19
Total Activities
19
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
Imidazo[1,2-a]pyrimidines as functionally selective and orally bioavailable GABA(A)alpha2/alpha3 binding site agonists for the treatment of anxiety disorders.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 8.66 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL200177 | MK-0777 | 2.0 | 1 | 9.52 |
| CHEMBL199689 | — | — | 1 | 9.48 |
| CHEMBL381380 | — | — | 1 | 9.47 |
| CHEMBL199957 | — | — | 1 | 9.43 |
| CHEMBL382412 | — | — | 1 | 9.42 |
| CHEMBL202768 | — | — | 1 | 9.21 |
| CHEMBL373250 | — | — | 1 | 9.15 |
| CHEMBL369902 | — | — | 1 | 9.14 |
| CHEMBL436768 | — | — | 1 | 8.89 |
| CHEMBL199690 | — | — | 1 | 8.59 |
| CHEMBL199411 | — | — | 1 | 8.44 |
| CHEMBL201472 | — | — | 1 | 8.40 |
| CHEMBL201559 | — | — | 1 | 8.12 |
| CHEMBL366468 | — | — | 1 | 8.10 |
| CHEMBL381625 | — | — | 1 | 8.04 |
| CHEMBL178942 | — | — | 1 | 8.00 |
| CHEMBL383626 | — | — | 1 | 7.85 |
| CHEMBL381987 | — | — | 1 | 7.80 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 7.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL200177 | MK-0777 | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL199689 | — | Ki | = | 0.33 | nM | 9.48 |
| CHEMBL381380 | — | Ki | = | 0.34 | nM | 9.47 |
| CHEMBL199957 | — | Ki | = | 0.37 | nM | 9.43 |
| CHEMBL382412 | — | Ki | = | 0.38 | nM | 9.42 |
| CHEMBL202768 | — | Ki | = | 0.62 | nM | 9.21 |
| CHEMBL373250 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL369902 | — | Ki | = | 0.73 | nM | 9.14 |
| CHEMBL436768 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL199690 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL199411 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL201472 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL201559 | — | Ki | = | 7.6 | nM | 8.12 |
| CHEMBL366468 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL381625 | — | Ki | = | 9.2 | nM | 8.04 |
| CHEMBL178942 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL383626 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL381987 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL12 | DIAZEPAM | Ki | = | 33.0 | nM | 7.48 |