Any sphingosine-1-phosphate receptor (S1PR) antagonist that acts as an antagonist for the subtype 2 receptors (S1PR2).
ChEBI ID: 195542
| Member | Definition | Class |
|---|---|---|
| jte 013 | A semicarbazide derivative that is semicarbazide in which the amino group at position 2 is replaced by a [1,3-dimethyl-4-(propan-2-yl)-1H-pyrazolo[3,4-b]pyridin-6-yl]amino group and the amino group adjacent to the carbonyl is replaced by a (2,6-dichloropyridin-4-yl)amino group. It is a potent S1P2 antagonist (IC50 = 17.6 nM). | JTE-013 |
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 16 (19.05) | 29.6817 |
| 2010's | 53 (63.10) | 24.3611 |
| 2020's | 15 (17.86) | 2.80 |
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 4 (4.76%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 80 (95.24%) | 84.16% |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 19.9526 | 1 | 1 |
| nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 15.8489 | 1 | 1 |
| vitamin D3 receptor isoform VDRA | Homo sapiens (human) | Potency | 22.3872 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Sphingosine 1-phosphate receptor 1 | Homo sapiens (human) | IC50 | 1.0000 | 2 | 2 |
| Sphingosine 1-phosphate receptor 2 | Homo sapiens (human) | IC50 | 0.0401 | 6 | 6 |
| Sphingosine 1-phosphate receptor 2 | Rattus norvegicus (Norway rat) | IC50 | 0.0200 | 1 | 1 |
| Sphingosine 1-phosphate receptor 3 | Homo sapiens (human) | IC50 | 1.0000 | 2 | 2 |
| Sphingosine 1-phosphate receptor 4 | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
| Sphingosine 1-phosphate receptor 5 | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Sphingosine 1-phosphate receptor 2 | Homo sapiens (human) | Kd | 1.9600 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Sphingosine 1-phosphate receptor 2 | Homo sapiens (human) | Activity | 1.7500 | 1 | 1 |