Compounds > gsk 561679
Page last updated: 2024-11-12

gsk 561679

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth

Description

NBI 77860: a CRF1 receptor antagonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID11596613
CHEMBL ID1287935
SCHEMBL ID205309
MeSH IDM0555518

Synonyms (39)

Synonym
885220-61-1
D09695
verucerfont (usan/inn)
unii-x60608b091
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x60608b091 ,
nbi 77860
3-(4-methoxy-2-methylphenyl)-2,5-dimethyl-n-((1s)-1-(3-methyl-1,2,4-oxadiazol-5- yl)propyl)pyrazolo(1,5-a)pyrimidin-7-amine
pyrazolo(1,5-a)pyrimidin-7-amine, 3-(4-methoxy-2-methylphenyl)-2,5-dimethyl-n-((1s)- 1-(3-methyl-1,2,4-oxadiazol-5-yl)propyl)-
gsk 561679
verucerfont
CHEMBL1287935
gsk561679a
gsk-561,679
nbi-77860
gsk-561679
gsk-561679a
gsk561679
bdbm50417503
verucerfont [usan]
verucerfont [who-dd]
pyrazolo(1,5-a)pyrimidin-7-amine, 3-(4-methoxy-2-methylphenyl)-2,5-dimethyl-n-((1s)-1-(3-methyl-1,2,4-oxadiazol-5-yl)propyl)-
3-(4-methoxy-2-methylphenyl)-2,5-dimethyl-n-[(1s)-1-(3-methyl-1,2,4-oxadiazol-5-yl)propyl]pyrazolo[1,5-a]pyrimidin-7-amine
verucerfont [inn]
SCHEMBL205309
AC-30339
gsk 561679a
EX-A1718
3-(4-methoxy-2-methylphenyl)-2,5-dimethyl-n-((s)-1-(3-methyl-1,2,4-oxadiazol-5-yl)propyl)pyrazolo[1,5-a]pyrimidin-7-amine
gsk561679;3-(4-methoxy-2-methylphenyl)-2,5-dimethyl-n-[(1s)-1-(3-methyl-1,2,4-oxadiazol-5-yl)propyl]pyrazolo[1,5-a]pyrimidin-7-amine
DB12512
CS-8099
(s)-3-(4-methoxy-2-methylphenyl)-2,5-dimethyl-n-(1-(3-methyl-1,2,4-oxadiazol-5-yl)propyl)pyrazolo[1,5-a]pyrimidin-7-amine
HY-14875
Q21098847
MS-26970
gtpl10378
compound (s)-8d [pmid: 21074436]
DTXSID501032013

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
"The meaningful reductions in ACTH and 17OHP following NBI-77860 dosing in 21OHD patients demonstrate target engagement and proof of principle in this disorder."( Single-Dose Study of a Corticotropin-Releasing Factor Receptor-1 Antagonist in Women With 21-Hydroxylase Deficiency.
Auchus, RJ; Farber, RH; Grigoriadis, DE; Luo, R; Madrigal, D; Muth, T; O'Brien, CF; Ramm, CA; Spencer-Segal, JL; Turcu, AF, 2016)		0.43
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Corticotropin-releasing factor receptor 1Homo sapiens (human)IC50 (µMol)0.10000.00070.06490.3400AID538004
Corticotropin-releasing factor receptor 1Homo sapiens (human)Ki0.00630.00080.01020.2400AID538004
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (16)

Processvia Protein(s)Taxonomy
immune responseCorticotropin-releasing factor receptor 1Homo sapiens (human)
cell surface receptor signaling pathwayCorticotropin-releasing factor receptor 1Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayCorticotropin-releasing factor receptor 1Homo sapiens (human)
activation of adenylate cyclase activityCorticotropin-releasing factor receptor 1Homo sapiens (human)
female pregnancyCorticotropin-releasing factor receptor 1Homo sapiens (human)
parturitionCorticotropin-releasing factor receptor 1Homo sapiens (human)
regulation of adenylate cyclase activity involved in G protein-coupled receptor signaling pathwayCorticotropin-releasing factor receptor 1Homo sapiens (human)
adrenal gland developmentCorticotropin-releasing factor receptor 1Homo sapiens (human)
exploration behaviorCorticotropin-releasing factor receptor 1Homo sapiens (human)
fear responseCorticotropin-releasing factor receptor 1Homo sapiens (human)
behavioral response to ethanolCorticotropin-releasing factor receptor 1Homo sapiens (human)
corticotropin secretionCorticotropin-releasing factor receptor 1Homo sapiens (human)
general adaptation syndrome, behavioral processCorticotropin-releasing factor receptor 1Homo sapiens (human)
cellular response to corticotropin-releasing hormone stimulusCorticotropin-releasing factor receptor 1Homo sapiens (human)
negative regulation of voltage-gated calcium channel activityCorticotropin-releasing factor receptor 1Homo sapiens (human)
regulation of corticosterone secretionCorticotropin-releasing factor receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (5)

Processvia Protein(s)Taxonomy
protein bindingCorticotropin-releasing factor receptor 1Homo sapiens (human)
corticotrophin-releasing factor receptor activityCorticotropin-releasing factor receptor 1Homo sapiens (human)
G protein-coupled peptide receptor activityCorticotropin-releasing factor receptor 1Homo sapiens (human)
corticotropin-releasing hormone bindingCorticotropin-releasing factor receptor 1Homo sapiens (human)
corticotropin-releasing hormone receptor activityCorticotropin-releasing factor receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (4)

Processvia Protein(s)Taxonomy
endosomeCorticotropin-releasing factor receptor 1Homo sapiens (human)
plasma membraneCorticotropin-releasing factor receptor 1Homo sapiens (human)
membraneCorticotropin-releasing factor receptor 1Homo sapiens (human)
plasma membraneCorticotropin-releasing factor receptor 1Homo sapiens (human)
neuron projectionCorticotropin-releasing factor receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (8)

Assay IDTitleYearJournalArticle
AID538011Plasma protein binding in rat at 5 mg/kg, iv after 72 hrs2010Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
Discovery of NBI-77860/GSK561679, a potent corticotropin-releasing factor (CRF1) receptor antagonist with improved pharmacokinetic properties.
AID538007AUC (0 to 24 hrs) in rat at 10 mg/kg, po2010Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
Discovery of NBI-77860/GSK561679, a potent corticotropin-releasing factor (CRF1) receptor antagonist with improved pharmacokinetic properties.
AID538008Ratio of drug uptake in brain to plasma in rat at 10 mg/kg, po2010Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
Discovery of NBI-77860/GSK561679, a potent corticotropin-releasing factor (CRF1) receptor antagonist with improved pharmacokinetic properties.
AID538004Antagonist activity at human recombinant CRF1 receptor2010Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
Discovery of NBI-77860/GSK561679, a potent corticotropin-releasing factor (CRF1) receptor antagonist with improved pharmacokinetic properties.
AID538005Metabolic stability in human liver microsome assessed as maximum bioavailability2010Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
Discovery of NBI-77860/GSK561679, a potent corticotropin-releasing factor (CRF1) receptor antagonist with improved pharmacokinetic properties.
AID538010Volume of distribution in rat at 5 mg/kg, iv after 72 hrs2010Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
Discovery of NBI-77860/GSK561679, a potent corticotropin-releasing factor (CRF1) receptor antagonist with improved pharmacokinetic properties.
AID538006Oral bioavailability in rat at 10 mg/kg after 24 hrs2010Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
Discovery of NBI-77860/GSK561679, a potent corticotropin-releasing factor (CRF1) receptor antagonist with improved pharmacokinetic properties.
AID538009Clearance in rat at 5 mg/kg, iv after 72 hrs2010Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
Discovery of NBI-77860/GSK561679, a potent corticotropin-releasing factor (CRF1) receptor antagonist with improved pharmacokinetic properties.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (10)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's8 (80.00)24.3611
2020's2 (20.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials9 (90.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other1 (10.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
alprazolam
Alprazolam: A triazolobenzodiazepine compound with antianxiety and sedative-hypnotic actions, that is efficacious in the treatment of PANIC DISORDERS, with or without AGORAPHOBIA, and in generalized ANXIETY DISORDERS. (From AMA Drug Evaluations Annual, 1994, p238). alprazolam : A member of the class of triazolobenzodiazepines that is 4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine carrying methyl, phenyl and chloro substituents at positions 1, 6 and 8 respectively. Alprazolam is only found in individuals that have taken this drug.		3.511organochlorine compound;
triazolobenzodiazepine		anticonvulsant;
anxiolytic drug;
GABA agonist;
muscle relaxant;
sedative;
xenobiotic
androstenedione
Androstenedione: A delta-4 C19 steroid that is produced not only in the TESTIS, but also in the OVARY and the ADRENAL CORTEX. Depending on the tissue type, androstenedione can serve as a precursor to TESTOSTERONE as well as ESTRONE and ESTRADIOL.. androst-4-ene-3,17-dione : A 3-oxo Delta(4)-steroid that is androst-4-ene substituted by oxo groups at positions 3 and 17. It is a steroid hormone synthesized in the adrenal glands and gonads.		4.721117-oxo steroid;
3-oxo-Delta(4) steroid;
androstanoid		androgen;
Daphnia magna metabolite;
human metabolite;
mouse metabolite
17-alpha-hydroxyprogesterone
17alpha-hydroxyprogesterone : A 17alpha-hydroxy steroid that is the 17alpha-hydroxy derivative of progesterone.		5.472217alpha-hydroxy-C21-steroid;
17alpha-hydroxy steroid;
tertiary alpha-hydroxy ketone		human metabolite;
metabolite;
mouse metabolite;
progestin
ssr 125543a
SSR125543: a CRF1 receptor antagonist with antidepressant-like effects		4.7211amine
r 121919
[no description available]		2.0510
oxadiazoles
Oxadiazoles: Compounds containing five-membered heteroaromatic rings containing two carbons, two nitrogens, and one oxygen atom which exist in various regioisomeric forms.		9.12109
pyrazolopyridine
pyrazolopyridine: act as competitive antagonists of brain adenosine A1 receptors		2.0510
ConditionIndicatedRelationship StrengthStudiesTrials
Congenital Adrenal Hyperplasia
[description not available]		05.4722
Adrenal Hyperplasia, Congenital
A group of inherited disorders of the ADRENAL GLANDS, caused by enzyme defects in the synthesis of cortisol (HYDROCORTISONE) and/or ALDOSTERONE leading to accumulation of precursors for ANDROGENS. Depending on the hormone imbalance, congenital adrenal hyperplasia can be classified as salt-wasting, hypertensive, virilizing, or feminizing. Defects in STEROID 21-HYDROXYLASE; STEROID 11-BETA-HYDROXYLASE; STEROID 17-ALPHA-HYDROXYLASE; 3-beta-hydroxysteroid dehydrogenase (3-HYDROXYSTEROID DEHYDROGENASES); TESTOSTERONE 5-ALPHA-REDUCTASE; or steroidogenic acute regulatory protein; among others, underlie these disorders.		17.4722
Genetic Predisposition
[description not available]		03.5311
Acute Post-Traumatic Stress Disorder
[description not available]		07.7355
Stress Disorders, Post-Traumatic
A class of traumatic stress disorders with symptoms that last more than one month.		19.7355
Anxiety
Feelings or emotions of dread, apprehension, and impending disaster but not disabling as with ANXIETY DISORDERS.		04.4722
Alcohol Abuse
[description not available]		03.5111
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		03.5111
Alcoholism
A primary, chronic disease with genetic, psychosocial, and environmental factors influencing its development and manifestations. The disease is often progressive and fatal. It is characterized by impaired control over drinking, preoccupation with the drug alcohol, use of alcohol despite adverse consequences, and distortions in thinking, most notably denial. Each of these symptoms may be continuous or periodic. (Morse & Flavin for the Joint Commission of the National Council on Alcoholism and Drug Dependence and the American Society of Addiction Medicine to Study the Definition and Criteria for the Diagnosis of Alcoholism: in JAMA 1992;268:1012-4)		15.5111