Assay Detail
Binding
CHEMBL803933
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding assay for the sigma receptor sites is performed by utilizing [3H]N,N-di-o-tolylguanidine ([3H]DTG) and guinea pig brain membrane suspensions
70
Total Activities
70
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL287) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and pharmacological evaluation of N-(2,5-disubstituted phenyl)-N'-(3-substituted phenyl)-N'-methylguanidines as N-methyl-D-aspartate receptor ion-channel blockers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 70 | 7.12 | 8.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL542487 | — | — | 1 | 8.35 |
| CHEMBL553034 | — | — | 1 | 8.24 |
| CHEMBL552829 | — | — | 1 | 8.13 |
| CHEMBL552831 | — | — | 1 | 8.10 |
| CHEMBL544842 | — | — | 1 | 7.99 |
| CHEMBL556043 | — | — | 1 | 7.97 |
| CHEMBL553312 | — | — | 1 | 7.93 |
| CHEMBL542491 | — | — | 1 | 7.88 |
| CHEMBL543433 | — | — | 1 | 7.84 |
| CHEMBL545310 | — | — | 1 | 7.80 |
| CHEMBL543427 | — | — | 1 | 7.80 |
| CHEMBL542736 | — | — | 1 | 7.76 |
| CHEMBL542481 | — | — | 1 | 7.74 |
| CHEMBL538036 | — | — | 1 | 7.73 |
| CHEMBL553749 | — | — | 1 | 7.71 |
| CHEMBL543432 | — | — | 1 | 7.70 |
| CHEMBL541860 | — | — | 1 | 7.69 |
| CHEMBL540841 | — | — | 1 | 7.62 |
| CHEMBL554355 | — | — | 1 | 7.57 |
| CHEMBL543673 | — | — | 1 | 7.54 |
| CHEMBL543201 | — | — | 1 | 7.52 |
| CHEMBL542730 | — | — | 1 | 7.51 |
| CHEMBL543431 | — | — | 1 | 7.50 |
| CHEMBL539299 | — | — | 1 | 7.44 |
| CHEMBL542956 | — | — | 1 | 7.41 |
| CHEMBL545545 | — | — | 1 | 7.41 |
| CHEMBL545542 | — | — | 1 | 7.40 |
| CHEMBL538283 | — | — | 1 | 7.40 |
| CHEMBL542964 | — | — | 1 | 7.37 |
| CHEMBL555091 | — | — | 1 | 7.36 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL542487 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL553034 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL552829 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL552831 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL544842 | — | IC50 | = | 10.3 | nM | 7.99 |
| CHEMBL556043 | — | IC50 | = | 10.8 | nM | 7.97 |
| CHEMBL553312 | — | IC50 | = | 11.8 | nM | 7.93 |
| CHEMBL542491 | — | IC50 | = | 13.3 | nM | 7.88 |
| CHEMBL543433 | — | IC50 | = | 14.4 | nM | 7.84 |
| CHEMBL545310 | — | IC50 | = | 15.9 | nM | 7.80 |
| CHEMBL543427 | — | IC50 | = | 15.8 | nM | 7.80 |
| CHEMBL542736 | — | IC50 | = | 17.3 | nM | 7.76 |
| CHEMBL542481 | — | IC50 | = | 18.2 | nM | 7.74 |
| CHEMBL538036 | — | IC50 | = | 18.5 | nM | 7.73 |
| CHEMBL553749 | — | IC50 | = | 19.6 | nM | 7.71 |
| CHEMBL543432 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL541860 | — | IC50 | = | 20.6 | nM | 7.69 |
| CHEMBL540841 | — | IC50 | = | 23.9 | nM | 7.62 |
| CHEMBL554355 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL543673 | — | IC50 | = | 28.5 | nM | 7.54 |
| CHEMBL543201 | — | IC50 | = | 30.1 | nM | 7.52 |
| CHEMBL542730 | — | IC50 | = | 30.7 | nM | 7.51 |
| CHEMBL543431 | — | IC50 | = | 31.8 | nM | 7.50 |
| CHEMBL539299 | — | IC50 | = | 36.5 | nM | 7.44 |
| CHEMBL545545 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL542956 | — | IC50 | = | 39.3 | nM | 7.41 |
| CHEMBL545542 | — | IC50 | = | 40.2 | nM | 7.40 |
| CHEMBL538283 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL542964 | — | IC50 | = | 42.8 | nM | 7.37 |
| CHEMBL555091 | — | IC50 | = | 43.5 | nM | 7.36 |
| CHEMBL545544 | — | IC50 | = | 45.3 | nM | 7.34 |
| CHEMBL539549 | — | IC50 | = | 45.7 | nM | 7.34 |
| CHEMBL553167 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL542959 | — | IC50 | = | 69.9 | nM | 7.16 |
| CHEMBL554618 | — | IC50 | = | 71.8 | nM | 7.14 |
| CHEMBL540831 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL543434 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL555698 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL540326 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL543428 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL541848 | — | IC50 | = | 113.0 | nM | 6.95 |
| CHEMBL543196 | — | IC50 | = | 113.0 | nM | 6.95 |
| CHEMBL542238 | — | IC50 | = | 113.0 | nM | 6.95 |
| CHEMBL543436 | — | IC50 | = | 115.0 | nM | 6.94 |
| CHEMBL555099 | — | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL554868 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL542478 | — | IC50 | = | 156.0 | nM | 6.81 |
| CHEMBL545769 | — | IC50 | = | 164.0 | nM | 6.79 |
| CHEMBL540838 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL555606 | — | IC50 | = | 178.0 | nM | 6.75 |