Assay Detail
Binding
CHEMBL864005
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]Ro-151788 from human recombinant GABAA alpha5 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-5/beta-3/gamma-2 (CHEMBL2094122) ↗| 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 | 9.16 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL436768 | — | — | 1 | 10.00 |
| CHEMBL199957 | — | — | 1 | 9.92 |
| CHEMBL200177 | MK-0777 | 2.0 | 1 | 9.70 |
| CHEMBL381380 | — | — | 1 | 9.70 |
| CHEMBL199689 | — | — | 1 | 9.68 |
| CHEMBL202768 | — | — | 1 | 9.59 |
| CHEMBL382412 | — | — | 1 | 9.30 |
| CHEMBL369902 | — | — | 1 | 9.30 |
| CHEMBL201472 | — | — | 1 | 9.28 |
| CHEMBL199690 | — | — | 1 | 9.03 |
| CHEMBL178942 | — | — | 1 | 9.00 |
| CHEMBL199411 | — | — | 1 | 8.92 |
| CHEMBL383626 | — | — | 1 | 8.80 |
| CHEMBL381625 | — | — | 1 | 8.80 |
| CHEMBL366468 | — | — | 1 | 8.68 |
| CHEMBL373250 | — | — | 1 | 8.64 |
| CHEMBL201559 | — | — | 1 | 8.55 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 7.96 |
| CHEMBL381987 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL436768 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL199957 | — | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL200177 | MK-0777 | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL381380 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL199689 | — | Ki | = | 0.21 | nM | 9.68 |
| CHEMBL202768 | — | Ki | = | 0.26 | nM | 9.59 |
| CHEMBL382412 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL369902 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL201472 | — | Ki | = | 0.53 | nM | 9.28 |
| CHEMBL199690 | — | Ki | = | 0.94 | nM | 9.03 |
| CHEMBL178942 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL199411 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL383626 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL381625 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL366468 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL373250 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL201559 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL12 | DIAZEPAM | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL381987 | — | Ki | - | — | - |