Assay Detail
Binding
CHEMBL839610
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Affinity for sigma receptor type 1 of guinea pig using [3H]ifenprodil or (+)-[3H]pentazocine radioligand
48
Total Activities
48
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL287) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of high-affinity ligands of sigma1 receptor, ERG2, and emopamil binding protein by pharmacophore modeling and virtual screening.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 48 | 7.95 | 11.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL372700 | FENPROPIMORPH | — | 1 | 11.00 |
| CHEMBL365842 | — | — | 1 | 10.40 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 9.70 |
| CHEMBL370753 | OPIPRAMOL | 3.0 | 1 | 9.70 |
| CHEMBL17470 | — | — | 1 | 9.30 |
| CHEMBL361085 | — | — | 1 | 9.30 |
| CHEMBL62540 | — | — | 1 | 9.22 |
| CHEMBL15023 | TRIFLUPERIDOL | 2.0 | 1 | 9.08 |
| CHEMBL187615 | — | — | 1 | 9.00 |
| CHEMBL190883 | — | — | 1 | 9.00 |
| CHEMBL365141 | — | — | 1 | 9.00 |
| CHEMBL363884 | RONIPAMIL | 2.0 | 1 | 9.00 |
| CHEMBL633 | AMIODARONE | 4.0 | 1 | 9.00 |
| CHEMBL363765 | — | — | 1 | 8.89 |
| CHEMBL305593 | — | — | 1 | 8.77 |
| CHEMBL113830 | (S,R)-IFENPRODIL | — | 1 | 8.70 |
| CHEMBL187892 | — | — | 1 | 8.60 |
| CHEMBL190631 | — | — | 1 | 8.52 |
| CHEMBL188476 | — | — | 1 | 8.52 |
| CHEMBL187829 | LEVEMOPAMIL | 2.0 | 1 | 8.40 |
| CHEMBL167779 | ZUCLOMIPHENE | 2.0 | 1 | 8.30 |
| CHEMBL190422 | — | — | 1 | 8.30 |
| CHEMBL365722 | — | — | 1 | 8.22 |
| CHEMBL7393 | — | — | 1 | 8.22 |
| CHEMBL187709 | TRIPARANOL | 4.0 | 1 | 8.10 |
| CHEMBL954 | ENCLOMIPHENE | 3.0 | 1 | 8.10 |
| CHEMBL422 | TRIFLUOPERAZINE | 4.0 | 1 | 7.82 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.82 |
| CHEMBL61539 | — | — | 1 | 7.80 |
| CHEMBL28211 | NAFOXIDINE | 2.0 | 1 | 7.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL372700 | FENPROPIMORPH | Ki | = | 0.01 | nM | 11.00 |
| CHEMBL365842 | — | Ki | = | 0.04 | nM | 10.40 |
| CHEMBL370753 | OPIPRAMOL | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL17470 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL361085 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL62540 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL15023 | TRIFLUPERIDOL | Ki | = | 0.83 | nM | 9.08 |
| CHEMBL187615 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL190883 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL365141 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL363884 | RONIPAMIL | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL633 | AMIODARONE | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL363765 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL305593 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL113830 | (S,R)-IFENPRODIL | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL187892 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL190631 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL188476 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL187829 | LEVEMOPAMIL | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL167779 | ZUCLOMIPHENE | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL190422 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL365722 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL7393 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL187709 | TRIPARANOL | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL954 | ENCLOMIPHENE | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL422 | TRIFLUOPERAZINE | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL61539 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL28211 | NAFOXIDINE | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL83 | TAMOXIFEN | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL81 | RALOXIFENE | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL2368401 | (7S,8R)-6-ALLYLAMINO-7,8-DIMETHYL-8-PROPYL-5,6,7,8-TETRAHYDRO-NAPHTHALEN-2-OL | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL363703 | — | Ki | = | 74.0 | nM | 7.13 |
| CHEMBL365417 | — | Ki | = | 81.0 | nM | 7.09 |
| CHEMBL372484 | — | Ki | = | 207.0 | nM | 6.68 |
| CHEMBL188044 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL103 | PROGESTERONE | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL189871 | — | Ki | = | 680.0 | nM | 6.17 |
| CHEMBL626 | NAFTIFINE | Ki | = | 880.0 | nM | 6.06 |
| CHEMBL386630 | TESTOSTERONE | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL188921 | BUFLOMEDIL | Ki | = | 1290.0 | nM | 5.89 |
| CHEMBL607293 | — | Ki | = | 8554.0 | nM | 5.07 |
| CHEMBL345754 | — | Ki | = | 26700.0 | nM | 4.57 |
| CHEMBL110739 | CORTICOSTERONE | Ki | = | 35600.0 | nM | 4.45 |
| CHEMBL822 | TERBINAFINE | Ki | - | nM | - | |
| CHEMBL366154 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL186779 | JERVINE | Ki | > | 100000.0 | nM | - |