A hormone antagonist that blocks corticotropin-releasing factor receptors
ChEBI ID: 76977
| Member | Definition | Class |
|---|---|---|
| antalarmin | A pyrrolopyrimidine that is 7H-pyrrolo[2,3-d]pyrimidin-4-amine which is substituted by methyl groups at positions 2, 5, and 6, by a mesityl group at position 7, and in which the amino substituent at position 4 has been substituted by ethyl and butyl groups. It is an antagonist of corticotropin-releasing factor 1 (CRF-1) receptors (Ki = 1 nM). | antalarmin |
| astressin | A 30-membered homodetic cyclic peptide comprising the sequence D-Phe-His-Leu-Leu-Arg-Glu-Val-Leu-Glu-Nle-Ala-Arg-Ala-Glu-Gln-Leu-Ala-Gln-Glu-Ala-His-Lys-Asn-Arg-Lys-Leu-Nle-Glu-Ile-Ile-NH2 cyclised by an amide bridge, formed by condensation of the side-chain carboxy group of the Glu residue at position 19 and the side-chain amino group of the Lys residue at position 22. | astressin |
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 29 (8.66) | 18.2507 |
| 2000's | 180 (53.73) | 29.6817 |
| 2010's | 118 (35.22) | 24.3611 |
| 2020's | 8 (2.39) | 2.80 |
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 12 (3.42%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 339 (96.58%) | 84.16% |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Chain A, Ferritin light chain | Equus caballus (horse) | Potency | 39.8107 | 1 | 1 |
| Chain A, TYROSYL-DNA PHOSPHODIESTERASE | Homo sapiens (human) | Potency | 89.1251 | 1 | 1 |
| nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 15.2113 | 2 | 2 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Corticotropin-releasing factor receptor 1 | Homo sapiens (human) | IC50 | 0.0186 | 2 | 2 |
| Corticotropin-releasing factor receptor 1 | Homo sapiens (human) | Ki | 0.0083 | 5 | 5 |
| Corticotropin-releasing factor receptor 1 | Rattus norvegicus (Norway rat) | Ki | 0.0010 | 1 | 1 |
| Corticotropin-releasing factor receptor 2 | Rattus norvegicus (Norway rat) | Ki | 0.0010 | 1 | 1 |