Assay Detail
Binding
CHEMBL4012829
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Positive allosteric modulation of recombinant rat GluN1/GluN2C receptor expressed in xenopus laevis oocyte assessed as potentiation of glutamate and glycine-induced current response at holding potential -40mV by two electrode voltage clamp method
53
Total Activities
53
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Glutamate NMDA receptor; Grin1/Grin2c (CHEMBL2096911) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
The Structure-Activity Relationship of a Tetrahydroisoquinoline Class of N-Methyl-d-Aspartate Receptor Modulators that Potentiates GluN2B-Containing N-Methyl-d-Aspartate Receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 53 | 5.79 | 6.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4100452 | — | — | 1 | 6.47 |
| CHEMBL4070902 | — | — | 1 | 6.46 |
| CHEMBL4099510 | — | — | 1 | 6.46 |
| CHEMBL4083076 | — | — | 1 | 6.42 |
| CHEMBL4063861 | — | — | 1 | 6.38 |
| CHEMBL4091770 | — | — | 1 | 6.32 |
| CHEMBL4064008 | — | — | 1 | 6.32 |
| CHEMBL4064435 | — | — | 1 | 6.16 |
| CHEMBL4062279 | — | — | 1 | 6.16 |
| CHEMBL4091772 | — | — | 1 | 6.15 |
| CHEMBL4068612 | — | — | 1 | 6.05 |
| CHEMBL4083995 | — | — | 1 | 6.04 |
| CHEMBL4061206 | — | — | 1 | 6.03 |
| CHEMBL4091645 | — | — | 1 | 6.01 |
| CHEMBL4099073 | — | — | 1 | 6.00 |
| CHEMBL4096621 | — | — | 1 | 5.92 |
| CHEMBL4101706 | — | — | 1 | 5.89 |
| CHEMBL2397256 | — | — | 1 | 5.89 |
| CHEMBL4100185 | — | — | 1 | 5.89 |
| CHEMBL4081483 | — | — | 1 | 5.85 |
| CHEMBL4064895 | — | — | 1 | 5.82 |
| CHEMBL4069391 | — | — | 1 | 5.80 |
| CHEMBL4073018 | — | — | 1 | 5.77 |
| CHEMBL4101985 | — | — | 1 | 5.77 |
| CHEMBL4094134 | — | — | 1 | 5.77 |
| CHEMBL4066872 | — | — | 1 | 5.75 |
| CHEMBL4061988 | — | — | 1 | 5.75 |
| CHEMBL4063668 | — | — | 1 | 5.75 |
| CHEMBL4104348 | — | — | 1 | 5.75 |
| CHEMBL4095932 | — | — | 1 | 5.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4100452 | — | EC50 | = | 340.0 | nM | 6.47 |
| CHEMBL4070902 | — | EC50 | = | 350.0 | nM | 6.46 |
| CHEMBL4099510 | — | EC50 | = | 350.0 | nM | 6.46 |
| CHEMBL4083076 | — | EC50 | = | 380.0 | nM | 6.42 |
| CHEMBL4063861 | — | EC50 | = | 420.0 | nM | 6.38 |
| CHEMBL4091770 | — | EC50 | = | 480.0 | nM | 6.32 |
| CHEMBL4064008 | — | EC50 | = | 480.0 | nM | 6.32 |
| CHEMBL4064435 | — | EC50 | = | 690.0 | nM | 6.16 |
| CHEMBL4062279 | — | EC50 | = | 700.0 | nM | 6.16 |
| CHEMBL4091772 | — | EC50 | = | 710.0 | nM | 6.15 |
| CHEMBL4068612 | — | EC50 | = | 900.0 | nM | 6.05 |
| CHEMBL4083995 | — | EC50 | = | 920.0 | nM | 6.04 |
| CHEMBL4061206 | — | EC50 | = | 940.0 | nM | 6.03 |
| CHEMBL4091645 | — | EC50 | = | 970.0 | nM | 6.01 |
| CHEMBL4099073 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4096621 | — | EC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4101706 | — | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL2397256 | — | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4100185 | — | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4081483 | — | EC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL4064895 | — | EC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4069391 | — | EC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4073018 | — | EC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4101985 | — | EC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4094134 | — | EC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4066872 | — | EC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL4104348 | — | EC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL4061988 | — | EC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL4063668 | — | EC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL4095932 | — | EC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL4103457 | — | EC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL4073306 | — | EC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL4083829 | — | EC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL4088927 | — | EC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL4101865 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL4101301 | — | EC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL4093717 | — | EC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL4064718 | — | EC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL4073626 | — | EC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL4072003 | — | EC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL4083997 | — | EC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL4060709 | — | EC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL4081036 | — | EC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL4078507 | — | EC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL4093976 | — | EC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL4085532 | — | EC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL4089357 | — | EC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL4085970 | — | EC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL4102790 | — | EC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL4102354 | — | EC50 | = | 9500.0 | nM | 5.02 |