A sigma receptor modulator that activates the sigma-2 receptor.
ChEBI ID: 189684
| Member | Definition | Class |
|---|---|---|
| PB28 | A member of the class of tetralins that is tetralin that is substituted by 3-(4-cyclohexylpiperazin-1-yl)propyl and methoxy groups at positions 1 and 5, respectively. It is a sigma 2 (sigma2) receptor agonist (Ki = 0.68 nM) and exhibits antineoplastic and anti SARS-CoV-2 activities. | PB28 |
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 1 (2.86) | 18.2507 |
| 2000's | 8 (22.86) | 29.6817 |
| 2010's | 16 (45.71) | 24.3611 |
| 2020's | 10 (28.57) | 2.80 |
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 2 (5.71%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 33 (94.29%) | 84.16% |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASE | Homo sapiens (human) | Potency | 0.0028 | 1 | 1 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 2.1317 | 1 | 1 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 37.9083 | 1 | 1 |
| DNA polymerase kappa isoform 1 | Homo sapiens (human) | Potency | 3.3587 | 1 | 1 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 19.8548 | 4 | 4 |
| Fumarate hydratase | Homo sapiens (human) | Potency | 29.5659 | 1 | 1 |
| Interferon beta | Homo sapiens (human) | Potency | 14.7403 | 1 | 3 |
| polyprotein | Zika virus | Potency | 29.5659 | 1 | 1 |
| PPM1D protein | Homo sapiens (human) | Potency | 14.7403 | 1 | 2 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 5-hydroxytryptamine receptor 3A | Rattus norvegicus (Norway rat) | Ki | 0.7000 | 1 | 1 |
| 5-hydroxytryptamine receptor 3B | Rattus norvegicus (Norway rat) | Ki | 0.7000 | 1 | 1 |
| Alpha-1A adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 7.5000 | 1 | 2 |
| Alpha-1B adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 7.5000 | 1 | 2 |
| Alpha-1D adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 7.5000 | 1 | 2 |
| Alpha-2A adrenergic receptor | Homo sapiens (human) | Ki | 1.5136 | 1 | 1 |
| Alpha-2B adrenergic receptor | Homo sapiens (human) | Ki | 9.3325 | 1 | 1 |
| Alpha-2C adrenergic receptor | Homo sapiens (human) | Ki | 0.4786 | 1 | 1 |
| Glutamate receptor ionotropic, NMDA 2C | Rattus norvegicus (Norway rat) | Ki | 92.6000 | 1 | 1 |
| Mu-type opioid receptor | Cavia porcellus (domestic guinea pig) | Ki | 0.0004 | 1 | 1 |
| Muscarinic acetylcholine receptor M1 | Homo sapiens (human) | Ki | 23.4423 | 1 | 1 |
| Muscarinic acetylcholine receptor M2 | Homo sapiens (human) | Ki | 4.7863 | 1 | 1 |
| Muscarinic acetylcholine receptor M3 | Homo sapiens (human) | Ki | 19.4985 | 1 | 1 |
| Muscarinic acetylcholine receptor M4 | Homo sapiens (human) | Ki | 3.9811 | 1 | 1 |
| Muscarinic acetylcholine receptor M5 | Homo sapiens (human) | Ki | 3.5481 | 1 | 1 |
| Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| Sigma intracellular receptor 2 | Homo sapiens (human) | Ki | 0.0014 | 2 | 2 |
| Sigma intracellular receptor 2 | Rattus norvegicus (Norway rat) | Ki | 0.0136 | 1 | 1 |
| Sigma non-opioid intracellular receptor 1 | Cavia porcellus (domestic guinea pig) | Ki | 0.0004 | 4 | 4 |
| Sigma non-opioid intracellular receptor 1 | Homo sapiens (human) | Ki | 0.0094 | 5 | 5 |
| Sigma non-opioid intracellular receptor 1 | Rattus norvegicus (Norway rat) | Ki | 0.0710 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| ATP-dependent translocase ABCB1 | Homo sapiens (human) | EC50 | 0.5500 | 1 | 1 |