Assay Detail
Binding
CHEMBL4701822
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-Ro15-1788 from human GABAA alpha5beta3gamma2 by scintillation proximity assay
35
Total Activities
35
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
Discovery of ONO-8590580: A novel, potent and selective GABA α negative allosteric modulator for the treatment of cognitive disorders.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 35 | 7.78 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4746471 | — | — | 1 | 9.30 |
| CHEMBL4758608 | — | — | 1 | 9.00 |
| CHEMBL4749423 | — | — | 1 | 8.70 |
| CHEMBL4785208 | — | — | 1 | 8.70 |
| CHEMBL4746482 | — | — | 1 | 8.70 |
| CHEMBL4756857 | — | — | 1 | 8.70 |
| CHEMBL4799496 | — | — | 1 | 8.40 |
| CHEMBL4757188 | — | — | 1 | 8.40 |
| CHEMBL4744361 | — | — | 1 | 8.15 |
| CHEMBL4760677 | — | — | 1 | 8.15 |
| CHEMBL4581355 | — | — | 1 | 8.10 |
| CHEMBL4754539 | — | — | 1 | 8.05 |
| CHEMBL4753738 | — | — | 1 | 7.96 |
| CHEMBL4761336 | — | — | 1 | 7.96 |
| CHEMBL4800521 | — | — | 1 | 7.92 |
| CHEMBL4785991 | — | — | 1 | 7.85 |
| CHEMBL4747220 | — | — | 1 | 7.82 |
| CHEMBL4785872 | — | — | 1 | 7.80 |
| CHEMBL4764668 | — | — | 1 | 7.77 |
| CHEMBL4748984 | — | — | 1 | 7.77 |
| CHEMBL4794600 | — | — | 1 | 7.77 |
| CHEMBL4796770 | — | — | 1 | 7.72 |
| CHEMBL4761610 | — | — | 1 | 7.42 |
| CHEMBL4759403 | — | — | 1 | 7.38 |
| CHEMBL4794167 | — | — | 1 | 7.35 |
| CHEMBL4759785 | — | — | 1 | 7.24 |
| CHEMBL4741416 | — | — | 1 | 7.21 |
| CHEMBL4760815 | — | — | 1 | 7.19 |
| CHEMBL4778552 | — | — | 1 | 7.12 |
| CHEMBL4776208 | — | — | 1 | 7.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4746471 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL4758608 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL4749423 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL4785208 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL4746482 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL4756857 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL4799496 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL4757188 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL4744361 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL4760677 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL4581355 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL4754539 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL4753738 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL4761336 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL4800521 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL4785991 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL4747220 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL4785872 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL4748984 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL4794600 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL4764668 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL4796770 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL4761610 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL4759403 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL4794167 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL4759785 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL4741416 | — | Ki | = | 62.0 | nM | 7.21 |
| CHEMBL4760815 | — | Ki | = | 65.0 | nM | 7.19 |
| CHEMBL4778552 | — | Ki | = | 76.0 | nM | 7.12 |
| CHEMBL4776208 | — | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL4747349 | — | Ki | = | 119.0 | nM | 6.92 |
| CHEMBL4585261 | — | Ki | = | 319.0 | nM | 6.50 |
| CHEMBL4792380 | — | Ki | = | 459.0 | nM | 6.34 |
| CHEMBL4798572 | — | Ki | = | 972.0 | nM | 6.01 |
| CHEMBL4796860 | — | Ki | > | 15000.0 | nM | - |