Assay Detail
Binding
CHEMBL2317551
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of rat GluN1/2A receptor expressed in Xenopus laevis oocyte assessed as glutamate and glycine-induced current at holding potentials from -80 to -40 mV by two electrode voltage clamp analysis
24
Total Activities
24
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/Grin2a (CHEMBL2096680) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Structure-activity relationship studies of argiotoxins: selective and potent inhibitors of ionotropic glutamate receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 6.88 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2314718 | — | — | 1 | 8.30 |
| CHEMBL2311573 | — | — | 1 | 8.30 |
| CHEMBL2314938 | — | — | 1 | 8.10 |
| CHEMBL1098240 | — | — | 1 | 8.00 |
| CHEMBL2314939 | — | — | 1 | 7.85 |
| CHEMBL2314937 | — | — | 1 | 7.77 |
| CHEMBL2314935 | — | — | 1 | 7.68 |
| CHEMBL2314719 | — | — | 1 | 7.14 |
| CHEMBL2314929 | — | — | 1 | 7.09 |
| CHEMBL2314928 | — | — | 1 | 6.99 |
| CHEMBL2314931 | — | — | 1 | 6.91 |
| CHEMBL2314930 | — | — | 1 | 6.78 |
| CHEMBL2314933 | — | — | 1 | 6.64 |
| CHEMBL2314712 | — | — | 1 | 6.59 |
| CHEMBL2314936 | — | — | 1 | 6.08 |
| CHEMBL2314940 | — | — | 1 | 6.03 |
| CHEMBL2314934 | — | — | 1 | 5.69 |
| CHEMBL2314713 | — | — | 1 | 5.68 |
| CHEMBL2314927 | — | — | 1 | 5.65 |
| CHEMBL2314716 | — | — | 1 | 5.63 |
| CHEMBL2314717 | — | — | 1 | 5.54 |
| CHEMBL2314714 | — | — | 1 | - |
| CHEMBL2314932 | — | — | 1 | - |
| CHEMBL2314715 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2314718 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL2311573 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL2314938 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL1098240 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2314939 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2314937 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL2314935 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL2314719 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL2314929 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL2314928 | — | IC50 | = | 103.0 | nM | 6.99 |
| CHEMBL2314931 | — | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL2314930 | — | IC50 | = | 165.0 | nM | 6.78 |
| CHEMBL2314933 | — | IC50 | = | 231.0 | nM | 6.64 |
| CHEMBL2314712 | — | IC50 | = | 256.0 | nM | 6.59 |
| CHEMBL2314936 | — | IC50 | = | 842.0 | nM | 6.08 |
| CHEMBL2314940 | — | IC50 | = | 936.0 | nM | 6.03 |
| CHEMBL2314934 | — | IC50 | = | 2060.0 | nM | 5.69 |
| CHEMBL2314713 | — | IC50 | = | 2090.0 | nM | 5.68 |
| CHEMBL2314927 | — | IC50 | = | 2230.0 | nM | 5.65 |
| CHEMBL2314716 | — | IC50 | = | 2320.0 | nM | 5.63 |
| CHEMBL2314717 | — | IC50 | = | 2860.0 | nM | 5.54 |
| CHEMBL2314714 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL2314932 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL2314715 | — | IC50 | > | 3000.0 | nM | - |