Assay Detail
Binding
CHEMBL748569
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Binding affinity towards NMDA receptor to displace [3H]-L-689,560 from rat cortical membranes
52
Total Activities
52
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Glutamate NMDA receptor (CHEMBL1907608) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
3-Acyl-4-hydroxyquinolin-2(1H)-ones. Systemically active anticonvulsants acting by antagonism at the glycine site of the N-methyl-D-aspartate receptor complex.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 52 | 5.38 | 6.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL113660 | — | — | 1 | 6.77 |
| CHEMBL114137 | — | — | 1 | 6.57 |
| CHEMBL115225 | — | — | 1 | 6.38 |
| CHEMBL116288 | — | — | 1 | 6.37 |
| CHEMBL115077 | — | — | 1 | 6.03 |
| CHEMBL115501 | — | — | 1 | 5.97 |
| CHEMBL324930 | — | — | 1 | 5.79 |
| CHEMBL115337 | — | — | 1 | 5.74 |
| CHEMBL325827 | — | — | 1 | 5.71 |
| CHEMBL115447 | — | — | 1 | 5.62 |
| CHEMBL114194 | — | — | 1 | 5.58 |
| CHEMBL112690 | — | — | 1 | 5.58 |
| CHEMBL439964 | — | — | 1 | 5.53 |
| CHEMBL324697 | — | — | 1 | 5.52 |
| CHEMBL114279 | — | — | 1 | 5.51 |
| CHEMBL114367 | — | — | 1 | 5.50 |
| CHEMBL113678 | — | — | 1 | 5.41 |
| CHEMBL114778 | — | — | 1 | 5.24 |
| CHEMBL114529 | — | — | 1 | 5.21 |
| CHEMBL114254 | — | — | 1 | 5.20 |
| CHEMBL104297 | — | — | 1 | 5.19 |
| CHEMBL114365 | — | — | 1 | 5.19 |
| CHEMBL114382 | — | — | 1 | 5.16 |
| CHEMBL111910 | — | — | 1 | 5.15 |
| CHEMBL113980 | — | — | 1 | 5.05 |
| CHEMBL117661 | — | — | 1 | 5.03 |
| CHEMBL114306 | — | — | 1 | 4.98 |
| CHEMBL117942 | — | — | 1 | 4.91 |
| CHEMBL114965 | — | — | 1 | 4.87 |
| CHEMBL432601 | — | — | 1 | 4.81 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL113660 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL114137 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL115225 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL116288 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL115077 | — | IC50 | = | 930.0 | nM | 6.03 |
| CHEMBL115501 | — | IC50 | = | 1070.0 | nM | 5.97 |
| CHEMBL324930 | — | IC50 | = | 1610.0 | nM | 5.79 |
| CHEMBL115337 | — | IC50 | = | 1820.0 | nM | 5.74 |
| CHEMBL325827 | — | IC50 | = | 1970.0 | nM | 5.71 |
| CHEMBL115447 | — | IC50 | = | 2390.0 | nM | 5.62 |
| CHEMBL114194 | — | IC50 | = | 2640.0 | nM | 5.58 |
| CHEMBL112690 | — | IC50 | = | 2620.0 | nM | 5.58 |
| CHEMBL439964 | — | IC50 | = | 2930.0 | nM | 5.53 |
| CHEMBL324697 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL114279 | — | IC50 | = | 3090.0 | nM | 5.51 |
| CHEMBL114367 | — | IC50 | = | 3160.0 | nM | 5.50 |
| CHEMBL113678 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL114778 | — | IC50 | = | 5820.0 | nM | 5.24 |
| CHEMBL114529 | — | IC50 | = | 6130.0 | nM | 5.21 |
| CHEMBL114254 | — | IC50 | = | 6320.0 | nM | 5.20 |
| CHEMBL104297 | — | IC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL114365 | — | IC50 | = | 6420.0 | nM | 5.19 |
| CHEMBL114382 | — | IC50 | = | 6850.0 | nM | 5.16 |
| CHEMBL111910 | — | IC50 | = | 7120.0 | nM | 5.15 |
| CHEMBL113980 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL117661 | — | IC50 | = | 9300.0 | nM | 5.03 |
| CHEMBL114306 | — | IC50 | = | 10500.0 | nM | 4.98 |
| CHEMBL117942 | — | IC50 | = | 12300.0 | nM | 4.91 |
| CHEMBL114965 | — | IC50 | = | 13600.0 | nM | 4.87 |
| CHEMBL432601 | — | IC50 | = | 15400.0 | nM | 4.81 |
| CHEMBL114089 | — | IC50 | = | 16700.0 | nM | 4.78 |
| CHEMBL112353 | — | IC50 | = | 25400.0 | nM | 4.59 |
| CHEMBL115058 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL322030 | — | IC50 | = | 27500.0 | nM | 4.56 |
| CHEMBL326277 | — | IC50 | = | 47100.0 | nM | 4.33 |
| CHEMBL112872 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL114095 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL112809 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL324517 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL113921 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL320554 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL117660 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL116214 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL115893 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL114714 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL114366 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL326853 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL115108 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL327148 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL114008 | — | IC50 | > | 100000.0 | nM | - |