Assay Detail
Binding
CHEMBL4033578
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Positive allosteric modulation of GluA2 (Q) flop isoform (unknown origin) expressed in HEK293 cells assessed as potentiation of glutamate-evoked calcium flux by fluo-4/AM dye-based fluorescence assay
38
Total Activities
19
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
7-Phenoxy-Substituted 3,4-Dihydro-2H-1,2,4-benzothiadiazine 1,1-Dioxides as Positive Allosteric Modulators of α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptors with Nanomolar Potency.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 38 | 5.77 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4091984 | — | — | 2 | 8.70 |
| CHEMBL4062524 | — | — | 2 | 7.34 |
| CHEMBL4060993 | — | — | 2 | 6.43 |
| CHEMBL4070694 | — | — | 2 | 6.41 |
| CHEMBL4066717 | — | — | 2 | 6.35 |
| CHEMBL4100668 | — | — | 2 | 6.15 |
| CHEMBL2441067 | — | — | 2 | 6.09 |
| CHEMBL4083809 | — | — | 2 | 6.02 |
| CHEMBL4081714 | — | — | 2 | 5.74 |
| CHEMBL4084231 | — | — | 2 | 5.50 |
| CHEMBL4089172 | — | — | 2 | 5.23 |
| CHEMBL4092527 | — | — | 2 | 5.12 |
| CHEMBL4091590 | — | — | 2 | 5.00 |
| CHEMBL4073898 | — | — | 2 | 4.81 |
| CHEMBL4071167 | — | — | 2 | 4.81 |
| CHEMBL4073431 | — | — | 2 | 4.73 |
| CHEMBL581906 | — | — | 2 | 4.69 |
| CHEMBL103741 | — | — | 2 | 4.30 |
| CHEMBL4062069 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4091984 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4091984 | — | EC50 | = | 1.995 | nM | 8.70 |
| CHEMBL4062524 | — | EC50 | = | 46.13 | nM | 7.34 |
| CHEMBL4062524 | — | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4060993 | — | EC50 | = | 370.0 | nM | 6.43 |
| CHEMBL4060993 | — | EC50 | = | 370.68 | nM | 6.43 |
| CHEMBL4070694 | — | EC50 | = | 390.84 | nM | 6.41 |
| CHEMBL4070694 | — | EC50 | = | 390.0 | nM | 6.41 |
| CHEMBL4066717 | — | EC50 | = | 450.0 | nM | 6.35 |
| CHEMBL4066717 | — | EC50 | = | 453.94 | nM | 6.34 |
| CHEMBL4100668 | — | EC50 | = | 712.85 | nM | 6.15 |
| CHEMBL4100668 | — | EC50 | = | 710.0 | nM | 6.15 |
| CHEMBL2441067 | — | EC50 | = | 810.0 | nM | 6.09 |
| CHEMBL2441067 | — | EC50 | = | 812.83 | nM | 6.09 |
| CHEMBL4083809 | — | EC50 | = | 950.0 | nM | 6.02 |
| CHEMBL4083809 | — | EC50 | = | 954.99 | nM | 6.02 |
| CHEMBL4081714 | — | EC50 | = | 1820.0 | nM | 5.74 |
| CHEMBL4081714 | — | EC50 | = | 1819.7 | nM | 5.74 |
| CHEMBL4084231 | — | EC50 | = | 3191.54 | nM | 5.50 |
| CHEMBL4084231 | — | EC50 | = | 3190.0 | nM | 5.50 |
| CHEMBL4089172 | — | EC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL4089172 | — | EC50 | = | 5902.01 | nM | 5.23 |
| CHEMBL4092527 | — | EC50 | = | 7620.79 | nM | 5.12 |
| CHEMBL4092527 | — | EC50 | = | 7620.0 | nM | 5.12 |
| CHEMBL4091590 | — | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4073898 | — | EC50 | = | 15595.53 | nM | 4.81 |
| CHEMBL4073898 | — | EC50 | = | 15600.0 | nM | 4.81 |
| CHEMBL4071167 | — | EC50 | = | 15600.0 | nM | 4.81 |
| CHEMBL4071167 | — | EC50 | = | 15595.53 | nM | 4.81 |
| CHEMBL4073431 | — | EC50 | = | 18706.82 | nM | 4.73 |
| CHEMBL4073431 | — | EC50 | = | 18700.0 | nM | 4.73 |
| CHEMBL581906 | — | EC50 | = | 20400.0 | nM | 4.69 |
| CHEMBL581906 | — | EC50 | = | 20417.38 | nM | 4.69 |
| CHEMBL103741 | — | EC50 | = | 50600.0 | nM | 4.30 |
| CHEMBL103741 | — | EC50 | = | 50582.47 | nM | 4.30 |
| CHEMBL4062069 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4062069 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4091590 | — | EC50 | > | 10000.0 | nM | - |