Assay Detail
Binding
CHEMBL805220
Review assay metadata, readout intent, target linkage, and publication context from the same page.
The compound was evaluated for affinity at sigma-2 site by inhibition of [3H]1,3-di(2-tolyl)guanidine (DTG) binding in guinea pig brain
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Confidence | 3 — Cell-line / Tissue |
| Curated By | Expert |
Publication
Novel (4-phenylpiperidinyl)- and (4-phenylpiperazinyl)alkyl-spaced esters of 1-phenylcyclopentanecarboxylic acids as potent sigma-selective compounds.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 7.86 | 9.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL542630 | — | — | 1 | 9.16 |
| CHEMBL542131 | — | — | 1 | 9.06 |
| CHEMBL542380 | — | — | 1 | 8.98 |
| CHEMBL540013 | — | — | 1 | 8.93 |
| CHEMBL537464 | — | — | 1 | 8.77 |
| CHEMBL539252 | — | — | 1 | 8.73 |
| CHEMBL541284 | — | — | 1 | 8.41 |
| CHEMBL545216 | — | — | 1 | 8.36 |
| CHEMBL556409 | — | — | 1 | 8.19 |
| CHEMBL544041 | — | — | 1 | 7.62 |
| CHEMBL545678 | — | — | 1 | 7.57 |
| CHEMBL555580 | — | — | 1 | 7.52 |
| CHEMBL543808 | — | — | 1 | 7.50 |
| CHEMBL554628 | — | — | 1 | 7.28 |
| CHEMBL544516 | — | — | 1 | 7.28 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.16 |
| CHEMBL558028 | — | — | 1 | 6.53 |
| CHEMBL537989 | — | — | 1 | 6.16 |
| CHEMBL539245 | — | — | 1 | 6.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL542630 | — | Ki | = | 0.69 | nM | 9.16 |
| CHEMBL542131 | — | Ki | = | 0.88 | nM | 9.06 |
| CHEMBL542380 | — | Ki | = | 1.05 | nM | 8.98 |
| CHEMBL540013 | — | Ki | = | 1.17 | nM | 8.93 |
| CHEMBL537464 | — | Ki | = | 1.71 | nM | 8.77 |
| CHEMBL539252 | — | Ki | = | 1.88 | nM | 8.73 |
| CHEMBL541284 | — | Ki | = | 3.93 | nM | 8.41 |
| CHEMBL545216 | — | Ki | = | 4.41 | nM | 8.36 |
| CHEMBL556409 | — | Ki | = | 6.49 | nM | 8.19 |
| CHEMBL544041 | — | Ki | = | 23.9 | nM | 7.62 |
| CHEMBL545678 | — | Ki | = | 26.8 | nM | 7.57 |
| CHEMBL555580 | — | Ki | = | 30.3 | nM | 7.52 |
| CHEMBL543808 | — | Ki | = | 31.8 | nM | 7.50 |
| CHEMBL554628 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL544516 | — | Ki | = | 52.3 | nM | 7.28 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL558028 | — | Ki | = | 293.0 | nM | 6.53 |
| CHEMBL537989 | — | Ki | = | 696.0 | nM | 6.16 |
| CHEMBL539245 | — | Ki | = | 763.0 | nM | 6.12 |