Proteins > Corticotropin-releasing factor receptor 1
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Corticotropin-releasing factor receptor 1
A corticotropin-releasing factor receptor 1 that is encoded in the genome of rat. [OMA:P35353, PRO:DNx]
Synonyms
CRF-R-1;
CRF-R1;
CRFR-1;
Corticotropin-releasing hormone receptor 1;
CRH-R-1;
CRH-R1
Research
Bioassay Publications (6)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 5 (83.33) | 29.6817 |
| 2010's | 1 (16.67) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (7)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| nbi 27914 | Rattus norvegicus (Norway rat) | Ki | 5.0010 | 2 | 2 |
| antalarmin | Rattus norvegicus (Norway rat) | Ki | 0.0010 | 1 | 1 |
| cp 154526 | Rattus norvegicus (Norway rat) | Ki | 0.0027 | 1 | 1 |
| r 121919 | Rattus norvegicus (Norway rat) | Ki | 0.0044 | 2 | 2 |
| pexacerfont | Rattus norvegicus (Norway rat) | IC50 | 0.0368 | 4 | 4 |
| dmp 696 | Rattus norvegicus (Norway rat) | IC50 | 0.0042 | 1 | 1 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| nbi 27914 | Rattus norvegicus (Norway rat) | EC50 | 0.1500 | 1 | 1 |
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| norbinaltorphimine | Rattus norvegicus (Norway rat) | Ke | 0.0000 | 1 | 1 |
Synthesis and in vitro opioid receptor functional antagonism of methyl-substituted analogues of (3R)-7-hydroxy-N-[(1S)-1-{[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl}-2-methylpropyl]-1,2,3,4-tetrahydro-3-isoquinolinecarboxamide (JDTic).Journal of medicinal chemistry, , Dec-10, Volume: 52, Issue:23, 2009
Discovery of N-(1-ethylpropyl)-[3-methoxy-5-(2-methoxy-4-trifluoromethoxyphenyl)-6-methyl-pyrazin-2-yl]amine 59 (NGD 98-2): an orally active corticotropin releasing factor-1 (CRF-1) receptor antagonist.Journal of medicinal chemistry, , Jun-23, Volume: 54, Issue:12, 2011
3-Aryl pyrazolo[4,3-d]pyrimidine derivatives: Nonpeptide CRF-1 antagonists.Bioorganic & medicinal chemistry letters, , Aug-19, Volume: 12, Issue:16, 2002
Discovery of N-(1-ethylpropyl)-[3-methoxy-5-(2-methoxy-4-trifluoromethoxyphenyl)-6-methyl-pyrazin-2-yl]amine 59 (NGD 98-2): an orally active corticotropin releasing factor-1 (CRF-1) receptor antagonist.Journal of medicinal chemistry, , Jun-23, Volume: 54, Issue:12, 2011
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.Journal of medicinal chemistry, , May-14, Volume: 52, Issue:9, 2009