Page last updated: 2024-08-05 15:50:23
PERK inhibitor
An EC 3.1.3.48 (protein-tyrosine-phosphatase) inhibitor that inhibits the expression of protein kinase RNA-like endoplasmic reticulum kinase.
ChEBI ID: 139055
Members (1)
| Member | Definition | Class |
|---|---|---|
| gsk2656157 | A pyrrolopyrimidine that is 7-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine which has been substituted at position 5 by a 4-fluoro-2,3-dihydro-1H-indol-5-yl group, the nitrogen of which has been acylated by a (6-methylpyridin-2-yl)acetyl group. An orally bioavailable PERK inhibitor. | GSK2656157 |
Research
Studies (29)
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 18 (62.07) | 24.3611 |
| 2020's | 11 (37.93) | 2.80 |
Study Types
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 2 (6.90%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 27 (93.10%) | 84.16% |
Protein Targets (12)
Potency Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 10.6840 | 1 | 1 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 8.4866 | 1 | 1 |
| G | Vesicular stomatitis virus | Potency | 10.6840 | 1 | 1 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 10.6840 | 1 | 1 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 10.6840 | 1 | 2 |
| Interferon beta | Homo sapiens (human) | Potency | 10.6840 | 1 | 1 |
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Cytochrome P450 3A4 | Homo sapiens (human) | IC50 | 0.2450 | 2 | 2 |
| eIF-2-alpha kinase GCN2 | Homo sapiens (human) | IC50 | 3.3880 | 1 | 1 |
| Eukaryotic translation initiation factor 2-alpha kinase 1 | Homo sapiens (human) | IC50 | 0.4600 | 1 | 1 |
| Eukaryotic translation initiation factor 2-alpha kinase 3 | Homo sapiens (human) | IC50 | 0.0154 | 2 | 2 |
| Interferon-induced, double-stranded RNA-activated protein kinase | Homo sapiens (human) | IC50 | 0.9050 | 1 | 1 |
| Receptor-interacting serine/threonine-protein kinase 1 | Homo sapiens (human) | IC50 | 0.0691 | 1 | 1 |