Assay Detail
Functional
CHEMBL2331015
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Agonist activity at human GABA-B B1/B2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 3 hrs by luciferase reporter gene assay
20
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Evaluation of difluoromethyl ketones as agonists of the γ-aminobutyric acid type B (GABAB) receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 20 | 4.89 | 6.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | 1.0 | 1 | 6.28 |
| CHEMBL301742 | ARBACLOFEN | 3.0 | 1 | 6.00 |
| CHEMBL701 | BACLOFEN | 4.0 | 1 | 5.77 |
| CHEMBL2322946 | — | — | 1 | 5.72 |
| CHEMBL2322934 | — | — | 3 | 4.80 |
| CHEMBL2322935 | — | — | 1 | 4.40 |
| CHEMBL2322942 | — | — | 1 | 4.27 |
| CHEMBL2322939 | — | — | 1 | 4.21 |
| CHEMBL2322940 | — | — | 1 | 4.17 |
| CHEMBL2322941 | — | — | 1 | 4.00 |
| CHEMBL2322943 | — | — | 1 | - |
| CHEMBL2322938 | — | — | 1 | - |
| CHEMBL2322944 | — | — | 1 | - |
| CHEMBL2322945 | — | — | 1 | - |
| CHEMBL2322932 | — | — | 1 | - |
| CHEMBL2322936 | — | — | 1 | - |
| CHEMBL2322933 | — | — | 1 | - |
| CHEMBL2322937 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | EC50 | = | 530.0 | nM | 6.28 |
| CHEMBL301742 | ARBACLOFEN | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL701 | BACLOFEN | EC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL2322946 | — | EC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL2322934 | — | EC50 | = | 15900.0 | nM | 4.80 |
| CHEMBL2322934 | — | EC50 | = | 24900.0 | nM | 4.60 |
| CHEMBL2322934 | — | EC50 | = | 37800.0 | nM | 4.42 |
| CHEMBL2322935 | — | EC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL2322942 | — | EC50 | = | 53500.0 | nM | 4.27 |
| CHEMBL2322939 | — | EC50 | = | 61800.0 | nM | 4.21 |
| CHEMBL2322940 | — | EC50 | = | 66900.0 | nM | 4.17 |
| CHEMBL2322941 | — | EC50 | = | 99300.0 | nM | 4.00 |
| CHEMBL2322943 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL2322938 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL2322944 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL2322945 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL2322932 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL2322936 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL2322933 | — | EC50 | - | — | - | |
| CHEMBL2322937 | — | EC50 | > | 100000.0 | nM | - |