Assay Detail
Binding
CHEMBL4012828
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Positive allosteric modulation of recombinant rat GluN1/GluN2B 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
48
Total Activities
48
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/Grin2b (CHEMBL2096666) ↗| 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 | 48 | 5.64 | 6.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4100452 | — | — | 1 | 6.57 |
| CHEMBL4064008 | — | — | 1 | 6.50 |
| CHEMBL4061206 | — | — | 1 | 6.47 |
| CHEMBL4089357 | — | — | 1 | 6.40 |
| CHEMBL4083076 | — | — | 1 | 6.31 |
| CHEMBL4063861 | — | — | 1 | 6.31 |
| CHEMBL4081483 | — | — | 1 | 6.26 |
| CHEMBL4091770 | — | — | 1 | 6.26 |
| CHEMBL4062279 | — | — | 1 | 6.17 |
| CHEMBL4099510 | — | — | 1 | 6.14 |
| CHEMBL4070902 | — | — | 1 | 6.08 |
| CHEMBL4099073 | — | — | 1 | 6.00 |
| CHEMBL4064895 | — | — | 1 | 5.85 |
| CHEMBL4091645 | — | — | 1 | 5.85 |
| CHEMBL4083995 | — | — | 1 | 5.82 |
| CHEMBL4068612 | — | — | 1 | 5.82 |
| CHEMBL4064435 | — | — | 1 | 5.77 |
| CHEMBL4069391 | — | — | 1 | 5.75 |
| CHEMBL4100185 | — | — | 1 | 5.66 |
| CHEMBL4101706 | — | — | 1 | 5.62 |
| CHEMBL4072003 | — | — | 1 | 5.60 |
| CHEMBL4096621 | — | — | 1 | 5.57 |
| CHEMBL4073626 | — | — | 1 | 5.52 |
| CHEMBL4101865 | — | — | 1 | 5.50 |
| CHEMBL4063668 | — | — | 1 | 5.47 |
| CHEMBL4061988 | — | — | 1 | 5.43 |
| CHEMBL4094134 | — | — | 1 | 5.42 |
| CHEMBL4066872 | — | — | 1 | 5.41 |
| CHEMBL4081036 | — | — | 1 | 5.40 |
| CHEMBL4078507 | — | — | 1 | 5.36 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4100452 | — | EC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4064008 | — | EC50 | = | 320.0 | nM | 6.50 |
| CHEMBL4061206 | — | EC50 | = | 340.0 | nM | 6.47 |
| CHEMBL4089357 | — | EC50 | = | 400.0 | nM | 6.40 |
| CHEMBL4083076 | — | EC50 | = | 490.0 | nM | 6.31 |
| CHEMBL4063861 | — | EC50 | = | 490.0 | nM | 6.31 |
| CHEMBL4081483 | — | EC50 | = | 550.0 | nM | 6.26 |
| CHEMBL4091770 | — | EC50 | = | 550.0 | nM | 6.26 |
| CHEMBL4062279 | — | EC50 | = | 670.0 | nM | 6.17 |
| CHEMBL4099510 | — | EC50 | = | 720.0 | nM | 6.14 |
| CHEMBL4070902 | — | EC50 | = | 840.0 | nM | 6.08 |
| CHEMBL4099073 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4091645 | — | EC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL4064895 | — | EC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL4068612 | — | EC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4083995 | — | EC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4064435 | — | EC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4069391 | — | EC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL4100185 | — | EC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL4101706 | — | EC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL4072003 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL4096621 | — | EC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL4073626 | — | EC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL4101865 | — | EC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL4063668 | — | EC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL4061988 | — | EC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL4094134 | — | EC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL4066872 | — | EC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL4081036 | — | EC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL4078507 | — | EC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL4083997 | — | EC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL4064718 | — | EC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL4073306 | — | EC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL4095932 | — | EC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL4093717 | — | EC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL4104348 | — | EC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL4103457 | — | EC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL4073018 | — | EC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL4101301 | — | EC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL4100301 | — | EC50 | = | 7200.0 | nM | 5.14 |
| CHEMBL4083829 | — | EC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL4093976 | — | EC50 | = | 9300.0 | nM | 5.03 |
| CHEMBL4085532 | — | EC50 | = | 9300.0 | nM | 5.03 |
| CHEMBL4102354 | — | EC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL4085970 | — | EC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL4073331 | — | EC50 | - | — | - | |
| CHEMBL4060709 | — | EC50 | - | — | - | |
| CHEMBL4086214 | — | EC50 | - | — | - |