Assay Detail
Binding
CHEMBL864002
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-Ro15-1788 from human recombinant GABAA alpha1 in combination with beta-3-gamma-2 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-1/beta-3/gamma-2 (CHEMBL2094121) ↗| 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 | 8.69 | 9.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL200177 | MK-0777 | 2.0 | 1 | 9.59 |
| CHEMBL199957 | — | — | 1 | 9.41 |
| CHEMBL381380 | — | — | 1 | 9.30 |
| CHEMBL202768 | — | — | 1 | 9.19 |
| CHEMBL199689 | — | — | 1 | 9.18 |
| CHEMBL373250 | — | — | 1 | 9.10 |
| CHEMBL201472 | — | — | 1 | 9.07 |
| CHEMBL382412 | — | — | 1 | 9.06 |
| CHEMBL369902 | — | — | 1 | 8.92 |
| CHEMBL381625 | — | — | 1 | 8.82 |
| CHEMBL199690 | — | — | 1 | 8.57 |
| CHEMBL436768 | — | — | 1 | 8.57 |
| CHEMBL199411 | — | — | 1 | 8.35 |
| CHEMBL201559 | — | — | 1 | 8.34 |
| CHEMBL383626 | — | — | 1 | 8.28 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 7.89 |
| CHEMBL366468 | — | — | 1 | 7.51 |
| CHEMBL178942 | — | — | 1 | 7.25 |
| CHEMBL381987 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL200177 | MK-0777 | Ki | = | 0.26 | nM | 9.59 |
| CHEMBL199957 | — | Ki | = | 0.39 | nM | 9.41 |
| CHEMBL381380 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL202768 | — | Ki | = | 0.65 | nM | 9.19 |
| CHEMBL199689 | — | Ki | = | 0.66 | nM | 9.18 |
| CHEMBL373250 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL201472 | — | Ki | = | 0.85 | nM | 9.07 |
| CHEMBL382412 | — | Ki | = | 0.87 | nM | 9.06 |
| CHEMBL369902 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL381625 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL199690 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL436768 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL199411 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL201559 | — | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL383626 | — | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL12 | DIAZEPAM | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL366468 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL178942 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL381987 | — | Ki | - | — | - |