Assay Detail
Binding
CHEMBL3089690
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]ATPA from human Gluk1 receptor
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 |
Target
Glutamate receptor ionotropic, kainate 1 (CHEMBL1918) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 6.01 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3088070 | — | — | 1 | 7.70 |
| CHEMBL3088072 | — | — | 1 | 7.05 |
| CHEMBL3088064 | — | — | 1 | 7.00 |
| CHEMBL3085837 | — | — | 1 | 6.80 |
| CHEMBL3085836 | — | — | 1 | 6.80 |
| CHEMBL3088058 | — | — | 1 | 6.70 |
| CHEMBL3088054 | — | — | 1 | 6.70 |
| CHEMBL3088060 | — | — | 1 | 6.40 |
| CHEMBL3087685 | — | — | 1 | 6.22 |
| CHEMBL3088069 | — | — | 1 | 6.16 |
| CHEMBL191249 | — | — | 1 | 6.10 |
| CHEMBL3088071 | — | — | 1 | 6.05 |
| CHEMBL3088074 | — | — | 1 | 6.05 |
| CHEMBL3088059 | — | — | 1 | 6.05 |
| CHEMBL3088068 | — | — | 1 | 6.00 |
| CHEMBL3088066 | — | — | 1 | 5.96 |
| CHEMBL3088062 | — | — | 1 | 5.96 |
| CHEMBL3088055 | — | — | 1 | 5.96 |
| CHEMBL189985 | — | — | 1 | 5.92 |
| CHEMBL3088063 | — | — | 1 | 5.85 |
| CHEMBL3085838 | — | — | 1 | 5.77 |
| CHEMBL3088065 | — | — | 1 | 5.54 |
| CHEMBL3087684 | — | — | 1 | 5.52 |
| CHEMBL3088056 | — | — | 1 | 5.50 |
| CHEMBL2440697 | — | — | 1 | 5.44 |
| CHEMBL14935 | TEZAMPANEL ANHYDROUS | 2.0 | 1 | 5.38 |
| CHEMBL3088073 | — | — | 1 | 5.00 |
| CHEMBL3088061 | — | — | 1 | 4.97 |
| CHEMBL3088057 | — | — | 1 | 4.89 |
| CHEMBL3085835 | — | — | 1 | 4.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3088070 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL3088072 | — | Ki | = | 90.0 | nM | 7.05 |
| CHEMBL3088064 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL3085837 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL3085836 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL3088058 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL3088054 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL3088060 | — | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL3087685 | — | Ki | = | 600.0 | nM | 6.22 |
| CHEMBL3088069 | — | Ki | = | 700.0 | nM | 6.16 |
| CHEMBL191249 | — | Ki | = | 800.0 | nM | 6.10 |
| CHEMBL3088071 | — | Ki | = | 900.0 | nM | 6.05 |
| CHEMBL3088074 | — | Ki | = | 900.0 | nM | 6.05 |
| CHEMBL3088059 | — | Ki | = | 900.0 | nM | 6.05 |
| CHEMBL3088068 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL3088066 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL3088062 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL3088055 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL189985 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL3088063 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL3085838 | — | Ki | = | 1700.0 | nM | 5.77 |
| CHEMBL3088065 | — | Ki | = | 2900.0 | nM | 5.54 |
| CHEMBL3087684 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL3088056 | — | Ki | = | 3200.0 | nM | 5.50 |
| CHEMBL2440697 | — | Ki | = | 3600.0 | nM | 5.44 |
| CHEMBL14935 | TEZAMPANEL ANHYDROUS | Ki | = | 4200.0 | nM | 5.38 |
| CHEMBL3088073 | — | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL3088061 | — | Ki | = | 10700.0 | nM | 4.97 |
| CHEMBL3088057 | — | Ki | = | 12800.0 | nM | 4.89 |
| CHEMBL3085835 | — | Ki | = | 17000.0 | nM | 4.77 |
| CHEMBL3088067 | — | Ki | = | 422000.0 | nM | - |