Assay Detail
Binding
CHEMBL3089691
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]AMPA from homomeric recombinant GluA2 receptor (unknown origin)
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
GluK1 antagonists from 6-(tetrazolyl)phenyl decahydroisoquinoline derivatives: in vitro profile and in vivo analgesic efficacy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 31 | 5.34 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3088070 | — | — | 1 | 8.52 |
| CHEMBL3088060 | — | — | 1 | 6.40 |
| CHEMBL3088069 | — | — | 1 | 5.77 |
| CHEMBL3088063 | — | — | 1 | 5.70 |
| CHEMBL3088071 | — | — | 1 | 5.66 |
| CHEMBL3088064 | — | — | 1 | 5.64 |
| CHEMBL3088059 | — | — | 1 | 5.57 |
| CHEMBL14935 | TEZAMPANEL ANHYDROUS | 2.0 | 1 | 5.52 |
| CHEMBL3088066 | — | — | 1 | 5.46 |
| CHEMBL3088072 | — | — | 1 | 5.36 |
| CHEMBL3088062 | — | — | 1 | 5.28 |
| CHEMBL191249 | — | — | 1 | 5.22 |
| CHEMBL3088065 | — | — | 1 | 5.21 |
| CHEMBL3088058 | — | — | 1 | 5.19 |
| CHEMBL3085838 | — | — | 1 | 5.02 |
| CHEMBL3085837 | — | — | 1 | 5.02 |
| CHEMBL3088061 | — | — | 1 | 4.92 |
| CHEMBL3088074 | — | — | 1 | 4.92 |
| CHEMBL3088068 | — | — | 1 | 4.89 |
| CHEMBL3087684 | — | — | 1 | 4.89 |
| CHEMBL189985 | — | — | 1 | 4.80 |
| CHEMBL3085836 | — | — | 1 | 4.77 |
| CHEMBL3088073 | — | — | 1 | 4.70 |
| CHEMBL3087685 | — | — | 1 | 4.66 |
| CHEMBL3088054 | — | — | 1 | 4.52 |
| CHEMBL3088067 | — | — | 1 | - |
| CHEMBL3085835 | — | — | 1 | - |
| CHEMBL3088057 | — | — | 1 | - |
| CHEMBL3088056 | — | — | 1 | - |
| CHEMBL3088055 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3088070 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL3088060 | — | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL3088069 | — | Ki | = | 1700.0 | nM | 5.77 |
| CHEMBL3088063 | — | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL3088071 | — | Ki | = | 2200.0 | nM | 5.66 |
| CHEMBL3088064 | — | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL3088059 | — | Ki | = | 2700.0 | nM | 5.57 |
| CHEMBL14935 | TEZAMPANEL ANHYDROUS | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL3088066 | — | Ki | = | 3500.0 | nM | 5.46 |
| CHEMBL3088072 | — | Ki | = | 4400.0 | nM | 5.36 |
| CHEMBL3088062 | — | Ki | = | 5200.0 | nM | 5.28 |
| CHEMBL191249 | — | Ki | = | 6000.0 | nM | 5.22 |
| CHEMBL3088065 | — | Ki | = | 6200.0 | nM | 5.21 |
| CHEMBL3088058 | — | Ki | = | 6400.0 | nM | 5.19 |
| CHEMBL3085838 | — | Ki | = | 9600.0 | nM | 5.02 |
| CHEMBL3085837 | — | Ki | = | 9600.0 | nM | 5.02 |
| CHEMBL3088061 | — | Ki | = | 12000.0 | nM | 4.92 |
| CHEMBL3088074 | — | Ki | = | 12000.0 | nM | 4.92 |
| CHEMBL3088068 | — | Ki | = | 13000.0 | nM | 4.89 |
| CHEMBL3087684 | — | Ki | = | 13000.0 | nM | 4.89 |
| CHEMBL189985 | — | Ki | = | 16000.0 | nM | 4.80 |
| CHEMBL3085836 | — | Ki | = | 17000.0 | nM | 4.77 |
| CHEMBL3088073 | — | Ki | = | 20000.0 | nM | 4.70 |
| CHEMBL3087685 | — | Ki | = | 22000.0 | nM | 4.66 |
| CHEMBL3088054 | — | Ki | = | 30000.0 | nM | 4.52 |
| CHEMBL3088067 | — | Ki | = | 450000.0 | nM | - |
| CHEMBL3085835 | — | Ki | = | 335000.0 | nM | - |
| CHEMBL3088057 | — | Ki | = | 181000.0 | nM | - |
| CHEMBL3088056 | — | Ki | = | 128000.0 | nM | - |
| CHEMBL3088055 | — | Ki | = | 252000.0 | nM | - |
| CHEMBL2440697 | — | Ki | = | 553000.0 | nM | - |