Assay Detail
Binding
CHEMBL3801516
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Positive allosteric modulation of human GluA2 AMPAR flip isomer expressed in Dox-inducible cells measured every 5 mins by BD calcium indicator dye based-fluorescence analysis in presence of glutamate
27
Total Activities
27
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
Discovery of GluN2A-Selective NMDA Receptor Positive Allosteric Modulators (PAMs): Tuning Deactivation Kinetics via Structure-Based Design.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 27 | 4.92 | 6.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3800556 | — | — | 1 | 6.82 |
| CHEMBL3799732 | — | — | 1 | 6.60 |
| CHEMBL3799878 | — | — | 1 | 6.15 |
| CHEMBL3799657 | — | — | 1 | 6.06 |
| CHEMBL3800605 | — | — | 1 | 5.77 |
| CHEMBL3800532 | — | — | 1 | 5.48 |
| CHEMBL3800265 | — | — | 1 | 5.27 |
| CHEMBL3797274 | — | — | 1 | 5.12 |
| CHEMBL3799213 | — | — | 1 | 5.04 |
| CHEMBL3797925 | — | — | 1 | 4.98 |
| CHEMBL3797378 | — | — | 1 | 4.91 |
| CHEMBL3797818 | — | — | 1 | 4.55 |
| CHEMBL3799832 | — | — | 1 | 4.49 |
| CHEMBL3799064 | — | — | 1 | 4.49 |
| CHEMBL3797313 | — | — | 1 | 4.48 |
| CHEMBL3799162 | — | — | 1 | 4.48 |
| CHEMBL3799325 | — | — | 1 | 4.47 |
| CHEMBL3799697 | — | — | 1 | 4.47 |
| CHEMBL3797797 | — | — | 1 | 4.46 |
| CHEMBL1555332 | — | — | 1 | 4.45 |
| CHEMBL3798166 | — | — | 1 | 4.45 |
| CHEMBL3799437 | — | — | 1 | 4.44 |
| CHEMBL3799694 | — | — | 1 | 4.43 |
| CHEMBL3797659 | — | — | 1 | 4.37 |
| CHEMBL3797994 | — | — | 1 | 4.18 |
| CHEMBL3799103 | — | — | 1 | 4.18 |
| CHEMBL3798907 | — | — | 1 | 4.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3800556 | — | EC50 | = | 150.0 | nM | 6.82 |
| CHEMBL3799732 | — | EC50 | = | 252.0 | nM | 6.60 |
| CHEMBL3799878 | — | EC50 | = | 702.0 | nM | 6.15 |
| CHEMBL3799657 | — | EC50 | = | 870.0 | nM | 6.06 |
| CHEMBL3800605 | — | EC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL3800532 | — | EC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL3800265 | — | EC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL3797274 | — | EC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL3799213 | — | EC50 | = | 9100.0 | nM | 5.04 |
| CHEMBL3797925 | — | EC50 | = | 10500.0 | nM | 4.98 |
| CHEMBL3797378 | — | EC50 | = | 12400.0 | nM | 4.91 |
| CHEMBL3797818 | — | EC50 | = | 28300.0 | nM | 4.55 |
| CHEMBL3799832 | — | EC50 | = | 32300.0 | nM | 4.49 |
| CHEMBL3799064 | — | EC50 | = | 32600.0 | nM | 4.49 |
| CHEMBL3797313 | — | EC50 | = | 33200.0 | nM | 4.48 |
| CHEMBL3799162 | — | EC50 | = | 32900.0 | nM | 4.48 |
| CHEMBL3799325 | — | EC50 | = | 34000.0 | nM | 4.47 |
| CHEMBL3799697 | — | EC50 | = | 33800.0 | nM | 4.47 |
| CHEMBL3797797 | — | EC50 | = | 34400.0 | nM | 4.46 |
| CHEMBL1555332 | — | EC50 | = | 35200.0 | nM | 4.45 |
| CHEMBL3798166 | — | EC50 | = | 35900.0 | nM | 4.45 |
| CHEMBL3799437 | — | EC50 | = | 36100.0 | nM | 4.44 |
| CHEMBL3799694 | — | EC50 | = | 37000.0 | nM | 4.43 |
| CHEMBL3797659 | — | EC50 | = | 43100.0 | nM | 4.37 |
| CHEMBL3797994 | — | EC50 | = | 66300.0 | nM | 4.18 |
| CHEMBL3799103 | — | EC50 | = | 66600.0 | nM | 4.18 |
| CHEMBL3798907 | — | EC50 | = | 75800.0 | nM | 4.12 |