Assay Detail
Binding
CHEMBL1111355
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]Flumazenil from cloned human GABA alpha-5-beta-3-gamma-2 receptor expressed in HEK293 cells
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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
The discovery and unique pharmacological profile of RO4938581 and RO4882224 as potent and selective GABAA alpha5 inverse agonists for the treatment of cognitive dysfunction.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 38 | 8.31 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1078299 | — | — | 1 | 9.70 |
| CHEMBL1078959 | — | — | 1 | 9.52 |
| CHEMBL1078957 | — | — | 1 | 9.00 |
| CHEMBL1079089 | — | — | 1 | 8.96 |
| CHEMBL1078958 | — | — | 1 | 8.92 |
| CHEMBL1079090 | — | — | 1 | 8.92 |
| CHEMBL1078985 | — | — | 1 | 8.85 |
| CHEMBL1079300 | — | — | 1 | 8.80 |
| CHEMBL1078781 | — | — | 1 | 8.74 |
| CHEMBL1079088 | — | — | 1 | 8.74 |
| CHEMBL1077391 | — | — | 1 | 8.70 |
| CHEMBL1081492 | — | — | 1 | 8.66 |
| CHEMBL1078606 | — | — | 1 | 8.66 |
| CHEMBL1078986 | — | — | 1 | 8.62 |
| CHEMBL1078500 | — | — | 1 | 8.59 |
| CHEMBL1081493 | — | — | 1 | 8.54 |
| CHEMBL1078501 | — | — | 1 | 8.52 |
| CHEMBL1077381 | — | — | 1 | 8.52 |
| CHEMBL1079299 | — | — | 1 | 8.49 |
| CHEMBL1078472 | — | — | 1 | 8.40 |
| CHEMBL1077397 | — | — | 1 | 8.36 |
| CHEMBL1080588 | — | — | 1 | 8.34 |
| CHEMBL1080412 | — | — | 1 | 8.25 |
| CHEMBL1078580 | — | — | 1 | 8.21 |
| CHEMBL1079691 | — | — | 1 | 8.20 |
| CHEMBL1078780 | — | — | 1 | 8.11 |
| CHEMBL1078581 | — | — | 1 | 8.04 |
| CHEMBL1079301 | — | — | 1 | 8.03 |
| CHEMBL1078473 | — | — | 1 | 8.01 |
| CHEMBL1081496 | — | — | 1 | 7.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1078299 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL1078959 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL1078957 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL1079089 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL1078958 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL1079090 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL1078985 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL1079300 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL1078781 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL1079088 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL1077391 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL1081492 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL1078606 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL1078986 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL1078500 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL1081493 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL1078501 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL1077381 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL1079299 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL1078472 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL1077397 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL1080588 | — | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL1080412 | — | Ki | = | 5.6 | nM | 8.25 |
| CHEMBL1078580 | — | Ki | = | 6.2 | nM | 8.21 |
| CHEMBL1079691 | — | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL1078780 | — | Ki | = | 7.7 | nM | 8.11 |
| CHEMBL1078581 | — | Ki | = | 9.2 | nM | 8.04 |
| CHEMBL1079301 | — | Ki | = | 9.4 | nM | 8.03 |
| CHEMBL1078473 | — | Ki | = | 9.7 | nM | 8.01 |
| CHEMBL1081496 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL1081494 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL1078607 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL1078298 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL1078782 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL1081495 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL1077409 | — | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL1079871 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL1079519 | — | Ki | = | 215.0 | nM | 6.67 |