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 human. [PRO:DNx, UniProtKB:P34998]
Synonyms
CRF-R-1;
CRF-R1;
CRFR-1;
Corticotropin-releasing hormone receptor 1;
CRH-R-1;
CRH-R1
Research
Bioassay Publications (44)
Timeframe | Studies on this Protein(%) | All Drugs % |
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 7 (15.91) | 18.2507 |
2000's | 20 (45.45) | 29.6817 |
2010's | 17 (38.64) | 24.3611 |
2020's | 0 (0.00) | 2.80 |
Compounds (15)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
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, structure-activity relationships, and anxiolytic activity of 7-aryl-6,7-dihydroimidazoimidazole corticotropin-releasing factor 1 receptor antagonists.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 15, Issue:17, 2005
Rational design, synthesis, and structure-activity relationships of aryltriazoles as novel corticotropin-releasing factor-1 receptor antagonists.Journal of medicinal chemistry, , Mar-10, Volume: 48, Issue:5, 2005
Synthesis of benzoylpyrimidines as antagonists of the corticotropin-releasing factor-1 receptor.Bioorganic & medicinal chemistry letters, , Aug-02, Volume: 14, Issue:15, 2004
2-arylaminothiazoles as high-affinity corticotropin-releasing factor 1 receptor (CRF1R) antagonists: synthesis, binding studies and behavioral efficacy.Bioorganic & medicinal chemistry letters, , Nov-17, Volume: 13, Issue:22, 2003
Pharmacophore development for corticotropin-releasing hormone: new insights into inhibitor activity.Journal of medicinal chemistry, , Jul-01, Volume: 42, Issue:13, 1999
Design and synthesis of a series of non-peptide high-affinity human corticotropin-releasing factor1 receptor antagonists.Journal of medicinal chemistry, , Oct-25, Volume: 39, Issue:22, 1996
Synthesis of 2-imino and 2-hydrazono thiazolo[4,5-d]pyrimidines as corticotropin releasing factor (CRF) antagonists.European journal of medicinal chemistry, , Sep-29, Volume: 138, 2017
Synthesis of substituted pyrimidines as corticotropin releasing factor (CRF) receptor ligands.European journal of medicinal chemistry, , May-06, Volume: 78, 2014
Lead diversification. Application to existing drug molecules: mifepristone 1 and antalarmin 8.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 22, Issue:1, 2012
Potent, orally active corticotropin-releasing factor receptor-1 antagonists containing a tricyclic pyrrolopyridine or pyrazolopyridine core.Journal of medicinal chemistry, , Jun-16, Volume: 48, Issue:12, 2005
Design and synthesis of tricyclic corticotropin-releasing factor-1 antagonists.Journal of medicinal chemistry, , Sep-08, Volume: 48, Issue:18, 2005
Design and synthesis of tricyclic imidazo[4,5-b]pyridin-2-ones as corticotropin-releasing factor-1 antagonists.Journal of medicinal chemistry, , Aug-11, Volume: 48, Issue:16, 2005
Synthesis, corticotropin-releasing factor receptor binding affinity, and pharmacokinetic properties of triazolo-, imidazo-, and pyrrolopyrimidines and -pyridines.Journal of medicinal chemistry, , Mar-11, Volume: 42, Issue:5, 1999
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
Discovery of pyrrolo[2,3-d]pyrimidin-4-ones as corticotropin-releasing factor 1 receptor antagonists with a carbonyl-based hydrogen bonding acceptor.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 21, Issue:8, 2011
2-Arylpyrimidines: novel CRF-1 receptor antagonists.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 18, Issue:16, 2008
The design, synthesis and structure-activity relationships of 1-aryl-4-aminoalkylisoquinolines: a novel series of CRF-1 receptor antagonists.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 18, Issue:3, 2008
Novel substituted tetrahydrotriazaacenaphthylene derivatives as potent CRF1 receptor antagonists.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 17, Issue:18, 2007
Synthesis, structure-activity relationships, and anxiolytic activity of 7-aryl-6,7-dihydroimidazoimidazole corticotropin-releasing factor 1 receptor antagonists.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 15, Issue:17, 2005
2-arylaminothiazoles as high-affinity corticotropin-releasing factor 1 receptor (CRF1R) antagonists: synthesis, binding studies and behavioral efficacy.Bioorganic & medicinal chemistry letters, , Nov-17, Volume: 13, Issue:22, 2003
3-Aryl pyrazolo[4,3-d]pyrimidine derivatives: Nonpeptide CRF-1 antagonists.Bioorganic & medicinal chemistry letters, , Aug-19, Volume: 12, Issue:16, 2002
Synthesis, corticotropin-releasing factor receptor binding affinity, and pharmacokinetic properties of triazolo-, imidazo-, and pyrrolopyrimidines and -pyridines.Journal of medicinal chemistry, , Mar-11, Volume: 42, Issue:5, 1999
4-Aryl-2-anilinopyrimidines as corticotropin-releasing hormone (CRH) antagonists.Bioorganic & medicinal chemistry letters, , Apr-05, Volume: 9, Issue:7, 1999
Use of the Suzuki reaction for the synthesis of aryl-substituted heterocycles as corticotropin-releasing hormone (CRH) antagonists.Bioorganic & medicinal chemistry letters, , Apr-05, Volume: 9, Issue:7, 1999
Pyrazolo[1,5-a]pyrimidine CRF-1 receptor antagonists.Bioorganic & medicinal chemistry letters, , Aug-18, Volume: 8, Issue:16, 1998
Synthesis and oral efficacy of a 4-(butylethylamino)pyrrolo[2,3-d]pyrimidine: a centrally active corticotropin-releasing factor1 receptor antagonist.Journal of medicinal chemistry, , May-23, Volume: 40, Issue:11, 1997
[no title available]Bioorganic & medicinal chemistry, , 03-01, Volume: 25, Issue:5, 2017
Design and Synthesis of Benzimidazoles As Novel Corticotropin-Releasing Factor 1 Receptor Antagonists.Journal of medicinal chemistry, , Mar-24, Volume: 59, Issue:6, 2016
Synthesis, binding affinity, radiolabeling, and microPET evaluation of 4-(2-substituted-4-substituted)-8-(dialkylamino)-6-methyl-1-substituted-3,4-dihydropyrido[2,3-b]pyrazin-2(1H)-ones as ligands for brain corticotropin-releasing factor type-1 (CRF1) recBioorganic & medicinal chemistry letters, , Nov-15, Volume: 25, Issue:22, 2015
Synthesis and structure-activity relationships of pyrazolo[1,5-a]pyridine derivatives: potent and orally active antagonists of corticotropin-releasing factor 1 receptor.Journal of medicinal chemistry, , Jun-14, Volume: 55, Issue:11, 2012
Design, synthesis, and structure-activity relationships of novel pyrazolo[5,1-b]thiazole derivatives as potent and orally active corticotropin-releasing factor 1 receptor antagonists.Journal of medicinal chemistry, , Oct-11, Volume: 55, Issue:19, 2012
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
Discovery of potent, metabolically stable purine CRF-1 antagonists with differentiated binding kinetic profiles.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 21, Issue:20, 2011
Discovery of NBI-77860/GSK561679, a potent corticotropin-releasing factor (CRF1) receptor antagonist with improved pharmacokinetic properties.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 20, Issue:24, 2010
2-Arylpyrimidines: novel CRF-1 receptor antagonists.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 18, Issue:16, 2008
Synthesis and pharmacological characterization of novel druglike corticotropin-releasing factor 1 antagonists.Journal of medicinal chemistry, , Dec-11, Volume: 51, Issue:23, 2008
Design and synthesis of tricyclic imidazo[4,5-b]pyridin-2-ones as corticotropin-releasing factor-1 antagonists.Journal of medicinal chemistry, , Aug-11, Volume: 48, Issue:16, 2005
Potent, orally active corticotropin-releasing factor receptor-1 antagonists containing a tricyclic pyrrolopyridine or pyrazolopyridine core.Journal of medicinal chemistry, , Jun-16, Volume: 48, Issue:12, 2005
Design of 2,5-dimethyl-3-(6-dimethyl-4-methylpyridin-3-yl)-7-dipropylaminopyrazolo[1,5-a]pyrimidine (NBI 30775/R121919) and structure--activity relationships of a series of potent and orally active corticotropin-releasing factor receptor antagonists.Journal of medicinal chemistry, , Sep-09, Volume: 47, Issue:19, 2004
3-Aryl pyrazolo[4,3-d]pyrimidine derivatives: Nonpeptide CRF-1 antagonists.Bioorganic & medicinal chemistry letters, , Aug-19, Volume: 12, Issue:16, 2002
[no title available]Bioorganic & medicinal chemistry, , 03-01, Volume: 25, Issue:5, 2017
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.Drug metabolism and disposition: the biological fate of chemicals, , Volume: 40, Issue:6, 2012
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
An insight on synthetic and medicinal aspects of pyrazolo[1,5-a]pyrimidine scaffold.European journal of medicinal chemistry, , Jan-27, Volume: 126, 2017
6,7-Dihydro-5H-cyclopenta[d]pyrazolo[1,5-a]pyrimidines and their derivatives as novel corticotropin-releasing factor 1 receptor antagonists.Bioorganic & medicinal chemistry, , Sep-15, Volume: 19, Issue:18, 2011
Discovery of potent, metabolically stable purine CRF-1 antagonists with differentiated binding kinetic profiles.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 21, Issue:20, 2011
Corticotropin releasing factor (CRF) receptor modulators: progress and opportunities for new therapeutic agents.Journal of medicinal chemistry, , May-04, Volume: 43, Issue:9, 2000
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
Design and synthesis of tricyclic imidazo[4,5-b]pyridin-2-ones as corticotropin-releasing factor-1 antagonists.Journal of medicinal chemistry, , Aug-11, Volume: 48, Issue:16, 2005
Design and synthesis of tricyclic corticotropin-releasing factor-1 antagonists.Journal of medicinal chemistry, , Sep-08, Volume: 48, Issue:18, 2005
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
Dihydropyrrole[2,3-d]pyridine derivatives as novel corticotropin-releasing factor-1 antagonists: mapping of the receptor binding pocket by in silico docking studies.Journal of medicinal chemistry, , Nov-27, Volume: 51, Issue:22, 2008
Synthesis and pharmacological characterization of novel druglike corticotropin-releasing factor 1 antagonists.Journal of medicinal chemistry, , Dec-11, Volume: 51, Issue:23, 2008
Novel substituted tetrahydrotriazaacenaphthylene derivatives as potent CRF1 receptor antagonists.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 17, Issue:18, 2007
4-(1,3-Dimethoxyprop-2-ylamino)-2,7-dimethyl-8-(2, 4-dichlorophenyl)pyrazolo[1,5-a]-1,3,5-triazine: a potent, orally bioavailable CRF(1) receptor antagonist.Journal of medicinal chemistry, , Feb-10, Volume: 43, Issue:3, 2000
Corticotropin releasing factor (CRF) receptor modulators: progress and opportunities for new therapeutic agents.Journal of medicinal chemistry, , May-04, Volume: 43, Issue:9, 2000
Corticotropin releasing factor (CRF) receptor modulators: progress and opportunities for new therapeutic agents.Journal of medicinal chemistry, , May-04, Volume: 43, Issue:9, 2000
4-(1,3-Dimethoxyprop-2-ylamino)-2,7-dimethyl-8-(2, 4-dichlorophenyl)pyrazolo[1,5-a]-1,3,5-triazine: a potent, orally bioavailable CRF(1) receptor antagonist.Journal of medicinal chemistry, , Feb-10, Volume: 43, Issue:3, 2000
Enables
This protein enables 5 target(s):
Target | Category | Definition |
protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
corticotrophin-releasing factor receptor activity | molecular function | Combining with the corticotrophin-releasing factor family of ligands, including the urocortins, to initiate a change in cell activity. [PMID:12032352] |
G protein-coupled peptide receptor activity | molecular function | Combining with a peptide and transmitting the signal across the membrane by activating an associated G-protein; promotes the exchange of GDP for GTP on the alpha subunit of a heterotrimeric G-protein complex. [GOC:dph, GOC:tb] |
corticotropin-releasing hormone binding | molecular function | Binding to corticotropin-releasing hormone, a polypeptide hormone involved in the stress response. It is released by the hypothalamus and stimulates the release of corticotropin by the anterior pituitary gland. [PMID:7556876] |
corticotropin-releasing hormone receptor activity | molecular function | Combining with corticotropin-releasing hormone and transmitting the signal to initiate a change in cell activity. [GOC:signaling, ISBN:0838577016, PMID:11027914, PMID:15134857] |
Located In
This protein is located in 3 target(s):
Target | Category | Definition |
endosome | cellular component | A vacuole to which materials ingested by endocytosis are delivered. [ISBN:0198506732, PMID:19696797] |
plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
membrane | cellular component | A lipid bilayer along with all the proteins and protein complexes embedded in it and attached to it. [GOC:dos, GOC:mah, ISBN:0815316194] |
Active In
This protein is active in 2 target(s):
Target | Category | Definition |
plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
neuron projection | cellular component | A prolongation or process extending from a nerve cell, e.g. an axon or dendrite. [GOC:jl, http://www.cogsci.princeton.edu/~wn/] |
Involved In
This protein is involved in 16 target(s):
Target | Category | Definition |
immune response | biological process | Any immune system process that functions in the calibrated response of an organism to a potential internal or invasive threat. [GO_REF:0000022, GOC:add] |
cell surface receptor signaling pathway | biological process | The series of molecular signals initiated by an extracellular ligand binding to a receptor located on the cell surface. The pathway ends with regulation of a downstream cellular process, e.g. transcription. [GOC:signaling] |
adenylate cyclase-activating G protein-coupled receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation of adenylyl cyclase activity which results in an increase in the intracellular concentration of cyclic AMP (cAMP). This pathway is negatively regulated by phosphodiesterase, which cleaves cAMP and terminates the signaling. [GOC:dph, GOC:mah, GOC:signaling, GOC:tb, ISBN:0815316194] |
activation of adenylate cyclase activity | biological process | Any process that initiates the activity of the inactive enzyme adenylate cyclase. [GOC:ai] |
female pregnancy | biological process | The set of physiological processes that allow an embryo or foetus to develop within the body of a female animal. It covers the time from fertilization of a female ovum by a male spermatozoon until birth. [ISBN:0192800825] |
parturition | biological process | The reproductive process in which the parent is separated from its offspring either by giving birth to live young or by laying eggs. [ISBN:0198506732] |
regulation of adenylate cyclase activity involved in G protein-coupled receptor signaling pathway | biological process | Any process that modulates the frequency, rate or extent of adenylate cyclase (AC) activity that is an integral part of a G protein-coupled receptor signaling pathway. [GOC:dph, GOC:signaling, GOC:tb] |
adrenal gland development | biological process | The process whose specific outcome is the progression of the adrenal gland over time, from its formation to the mature structure. This gland can either be a discrete structure located bilaterally above each kidney, or a cluster of cells in the head kidney that perform the functions of the adrenal gland. In either case, this organ consists of two cells types, aminergic chromaffin cells and steroidogenic cortical cells. [GOC:dgh] |
exploration behavior | biological process | The specific behavior of an organism in response to a novel environment or stimulus. [GOC:BHF, GOC:pr, PMID:11682103, PMID:9767169] |
fear response | biological process | The response of an organism to a perceived external threat. [GOC:go_curators] |
behavioral response to ethanol | biological process | Any process that results in a change in the behavior of an organism as a result of an ethanol stimulus. [GOC:jid] |
corticotropin secretion | biological process | The regulated release of corticotropin by a cell. Corticotropin hormone is a polypeptide hormone synthesized and secreted from corticotropes in the anterior lobe of the pituitary gland in response to corticotropin-releasing hormone (CRH) released by the hypothalamus. [GOC:cjm, PMID:11027914] |
general adaptation syndrome, behavioral process | biological process | The set of behavioral processes that occur as part of the general adaptation syndrome, the response of the body to a strong, stressful stimulus. [GOC:ai] |
cellular response to corticotropin-releasing hormone stimulus | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a corticotropin-releasing hormone stimulus. Corticotropin-releasing hormone is a peptide hormone involved in the stress response. [GOC:mah] |
negative regulation of voltage-gated calcium channel activity | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of voltage-gated calcium channel activity. [GOC:BHF, GOC:TermGenie] |
regulation of corticosterone secretion | biological process | Any process that modulates the frequency, rate or extent of corticosterone secretion. [GOC:sl] |