Assay Detail
Binding
CHEMBL1909110
Review assay metadata, readout intent, target linkage, and publication context from the same page.
DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol)
1742
Total Activities
871
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | Jurkat |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL287) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
DrugMatrix in vitro pharmacology data
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 871 | 6.37 | 8.39 |
| Ki | 871 | 6.74 | 8.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1902981 | EPERISONE | 3.0 | 2 | 8.77 |
| CHEMBL1123 | DICYCLOMINE | 4.0 | 2 | 8.69 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 2 | 8.25 |
| CHEMBL1076211 | TOLPERISONE | 3.0 | 2 | 8.25 |
| CHEMBL726 | FLUPHENAZINE | 4.0 | 2 | 8.07 |
| CHEMBL83 | TAMOXIFEN | 4.0 | 2 | 8.06 |
| CHEMBL30008 | FLUNARIZINE | 2.0 | 2 | 8.00 |
| CHEMBL1231 | OXYBUTYNIN | 4.0 | 2 | 7.99 |
| CHEMBL954 | ENCLOMIPHENE | 3.0 | 2 | 7.92 |
| CHEMBL1626 | CLEMASTINE | 4.0 | 2 | 7.85 |
| CHEMBL43064 | CINNARIZINE | 2.0 | 2 | 7.77 |
| CHEMBL728 | PROCHLORPERAZINE | 4.0 | 2 | 7.64 |
| CHEMBL253376 | BROMHEXINE | 3.0 | 2 | 7.60 |
| CHEMBL809 | SERTRALINE | 4.0 | 2 | 7.53 |
| CHEMBL633 | AMIODARONE | 4.0 | 2 | 7.39 |
| CHEMBL1490 | TRIHEXYPHENIDYL | 4.0 | 2 | 7.35 |
| CHEMBL1909072 | PIPAMAZINE | 4.0 | 2 | 7.32 |
| CHEMBL404849 | SULOCTIDIL | 4.0 | 2 | 7.31 |
| CHEMBL1198 | PRAMOXINE | 4.0 | 2 | 7.29 |
| CHEMBL1201203 | BENZTROPINE | 4.0 | 2 | 7.23 |
| CHEMBL395110 | MEPAZINE | 4.0 | 2 | 7.12 |
| CHEMBL1196 | PROPARACAINE | 4.0 | 2 | 7.00 |
| CHEMBL936 | DIPHENIDOL | 4.0 | 2 | 6.97 |
| CHEMBL564 | PROMAZINE | 4.0 | 2 | 6.94 |
| CHEMBL643 | PROMETHAZINE | 4.0 | 2 | 6.92 |
| CHEMBL60889 | MOSAPRIDE | 3.0 | 2 | 6.89 |
| CHEMBL479 | THIORIDAZINE | 4.0 | 2 | 6.82 |
| CHEMBL549 | CITALOPRAM | 4.0 | 2 | 6.78 |
| CHEMBL833 | TICLOPIDINE | 4.0 | 2 | 6.75 |
| CHEMBL71 | CHLORPROMAZINE | 4.0 | 2 | 6.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1902981 | EPERISONE | Ki | = | 1.704 | nM | 8.77 |
| CHEMBL1123 | DICYCLOMINE | Ki | = | 2.055 | nM | 8.69 |
| CHEMBL1902981 | EPERISONE | IC50 | = | 4.055 | nM | 8.39 |
| CHEMBL1123 | DICYCLOMINE | IC50 | = | 4.89 | nM | 8.31 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 5.665 | nM | 8.25 |
| CHEMBL1076211 | TOLPERISONE | Ki | = | 5.587 | nM | 8.25 |
| CHEMBL726 | FLUPHENAZINE | Ki | = | 8.575 | nM | 8.07 |
| CHEMBL83 | TAMOXIFEN | Ki | = | 8.714 | nM | 8.06 |
| CHEMBL30008 | FLUNARIZINE | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL1231 | OXYBUTYNIN | Ki | = | 10.2 | nM | 7.99 |
| CHEMBL954 | ENCLOMIPHENE | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL54 | HALOPERIDOL | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1076211 | TOLPERISONE | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1626 | CLEMASTINE | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL43064 | CINNARIZINE | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL726 | FLUPHENAZINE | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL83 | TAMOXIFEN | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL728 | PROCHLORPERAZINE | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL1231 | OXYBUTYNIN | IC50 | = | 24.2 | nM | 7.62 |
| CHEMBL30008 | FLUNARIZINE | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL253376 | BROMHEXINE | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL954 | ENCLOMIPHENE | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL809 | SERTRALINE | Ki | = | 29.3 | nM | 7.53 |
| CHEMBL1626 | CLEMASTINE | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL43064 | CINNARIZINE | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL633 | AMIODARONE | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL1490 | TRIHEXYPHENIDYL | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL1909072 | PIPAMAZINE | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL404849 | SULOCTIDIL | Ki | = | 49.3 | nM | 7.31 |
| CHEMBL1198 | PRAMOXINE | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL728 | PROCHLORPERAZINE | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL1201203 | BENZTROPINE | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL253376 | BROMHEXINE | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL809 | SERTRALINE | IC50 | = | 69.7 | nM | 7.16 |
| CHEMBL395110 | MEPAZINE | Ki | = | 76.0 | nM | 7.12 |
| CHEMBL633 | AMIODARONE | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL1196 | PROPARACAINE | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL1490 | TRIHEXYPHENIDYL | IC50 | = | 108.0 | nM | 6.97 |
| CHEMBL936 | DIPHENIDOL | Ki | = | 108.0 | nM | 6.97 |
| CHEMBL1909072 | PIPAMAZINE | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL564 | PROMAZINE | Ki | = | 114.0 | nM | 6.94 |
| CHEMBL404849 | SULOCTIDIL | IC50 | = | 117.2 | nM | 6.93 |
| CHEMBL643 | PROMETHAZINE | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL1198 | PRAMOXINE | IC50 | = | 121.0 | nM | 6.92 |
| CHEMBL60889 | MOSAPRIDE | Ki | = | 128.4 | nM | 6.89 |
| CHEMBL1201203 | BENZTROPINE | IC50 | = | 139.0 | nM | 6.86 |
| CHEMBL479 | THIORIDAZINE | Ki | = | 153.0 | nM | 6.82 |
| CHEMBL549 | CITALOPRAM | Ki | = | 167.0 | nM | 6.78 |
| CHEMBL833 | TICLOPIDINE | Ki | = | 179.0 | nM | 6.75 |
| CHEMBL395110 | MEPAZINE | IC50 | = | 180.0 | nM | 6.75 |