pexacerfont profile

ID Source	ID
PubMed CID	9884366
CHEMBL ID	482950
CHEBI ID	177416
SCHEMBL ID	5235999
MeSH ID	M0537739

Synonym
n-[(2r)-butan-2-yl]-8-(6-methoxy-2-methylpyridin-3-yl)-2,7-dimethylpyrazolo[1,5-a][1,3,5]triazin-4-amine
pexacerfont
459856-18-9
CHEBI:177416
pyrazolo[1,5-a]-1,3,5-triazine, 13-15
bdbm29490
crf1 antagonist
bms562086
bms-562086
dpc-a69448
CHEMBL482950
8-(6-methoxy-2-methylpyridin-3-yl)-2,7-dimethyl-n-((1r)-1-methylpropyl)pyrazolo(1,5-a)-1,3,5-triazin-4-amine
unii-lf1vbg4zuk
pyrazolo(1,5-a)-1,3,5-triazin-4-amine, 8-(6-methoxy-2-methyl-3-pyridinyl)-2,7-dimethyl-n-((1r)-1-methylpropyl)-
pexacerfont [usan:inn]
lf1vbg4zuk ,
bms 562086
D10022
pexacerfont (usan/inn)
8-(6-methoxy-2-methylpyridin-3-yl)-2,7-dimethyl-n-[(1r)-1-methylpropyl]pyrazolo[1,5-a]-1,3,5-triazin-4-amine
pexacerfont [inn]
pexacerfont [usan]
n-((2r)-butan-2-yl)-8-(6-methoxy-2-methylpyridin-3-yl)-2,7-dimethylpyrazolo(1,5-a)(1,3,5)triazin-4-amine
SCHEMBL5235999
AC-32621
DTXSID60196675
CS-6630
HY-12127
(r)-n-(sec-butyl)-8-(6-methoxy-2-methylpyridin-3-yl)-2,7-dimethyl pyrazolo[1,5-a][1,3,5]triazin-4-amine
DB12572
ZB1563
Q7179563
EX-A3079
8-(6-methoxy-2-methyl-3-pyridinyl)-2,7-dimethyl-n-[(1r)-1-methylpropyl]pyrazolo[1,5-a]-1,3,5-triazin-4-amine
D70085
n-((r)-sec-butyl)-8-(6-methoxy-2-methylpyridin-3-yl)-2,7-dimethylpyrazolo[1,5-a][1,3,5]triazin-4-amine
MS-25202
gtpl10379
AKOS040742389

Excerpt	Reference	Relevance
"Pexacerfont is a corticotrophin-releasing factor subtype 1 receptor (CRF-1) antagonist developed for potential treatment of anxiety and stress-related disorders. "	( T4-mediated rescue of aortic malformations in hypothyroid rats indicates maternal thyroid status can affect great vessel development. Augustine-Rauch, K; Graziano, M; Liaw, JJ, 2021)	2.06
"Pexacerfont is a corticotropin-releasing factor subtype 1 receptor antagonist that was developed for the treatment of anxiety- and stress-related disorders. "	( Toxicity of Pexacerfont, a Corticotropin-Releasing Factor Type 1 Receptor Antagonist, in Rats and Dogs. Graziano, MJ; Sanderson, TP; White, MR, )	1.95

Excerpt	Reference	Relevance
"Pexacerfont treatment had no effect on alcohol craving, emotional responses, or anxiety."	( The corticotropin releasing hormone-1 (CRH1) receptor antagonist pexacerfont in alcohol dependence: a randomized controlled experimental medicine study. Anizan, S; Concheiro, M; George, DT; Heilig, M; Huestis, M; Kwako, LE; Momenan, R; Rio, DE; Schwandt, ML; Sinha, R; Spagnolo, PA; Thorsell, A, 2015)	1.38

Excerpt	Reference	Relevance
"The absorption, distribution, metabolism, and excretion (ADME) and the pharmacokinetic characteristics of BMS-562086 [pexacerfont; 8-(6-methoxy-2-methyl-3-pyridinyl)-2,7-dimethyl-N-[(1R)-1-methylpropyl]pyrazolo(1,5-a)-1,3,5-triazin-4-amine (DPC-A69448)] were investigated in vitro and in animals to support its clinical development."	( In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist. Dockens, RC; Grossman, SJ; Iyer, RA; Liu-Kreyche, P; Zhou, L, 2012)	0.59

Excerpt	Reference	Relevance
" BMS-562086 was orally bioavailable in rats, dogs, and chimpanzees, with an absolute oral bioavailability of 40."	( In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist. Dockens, RC; Grossman, SJ; Iyer, RA; Liu-Kreyche, P; Zhou, L, 2012)	0.38

Excerpt	Relevance	Reference
" A separate group of 10 patients received open-label pexacerfont following the same dosing regimen and had cerebrospinal fluid sampled to estimate central nervous system exposure."	( The corticotropin releasing hormone-1 (CRH1) receptor antagonist pexacerfont in alcohol dependence: a randomized controlled experimental medicine study. Anizan, S; Concheiro, M; George, DT; Heilig, M; Huestis, M; Kwako, LE; Momenan, R; Rio, DE; Schwandt, ML; Sinha, R; Spagnolo, PA; Thorsell, A, 2015)	0.9
" To better understand this relationship, pregnant rats were implanted with a subcutaneous L-thyroxine pellet designed to provide a sustained release of T4 throughout organogenesis in rat embryos (GD 6 to 15; the dosing period of pexacerfont)."	( T4-mediated rescue of aortic malformations in hypothyroid rats indicates maternal thyroid status can affect great vessel development. Augustine-Rauch, K; Graziano, M; Liaw, JJ, 2021)	0.81

Class	Description
pyrazolopyridine
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Substance-K receptor	Homo sapiens (human)	IC50 (µMol)	4.9000	0.0001	3.1210	9.5530	AID353816
Adenosine receptor A1	Rattus norvegicus (Norway rat)	Ki	2.6600	0.0001	1.2092	9.9700	AID353815
Corticotropin-releasing factor receptor 1	Homo sapiens (human)	IC50 (µMol)	2.5877	0.0007	0.0649	0.3400	AID1218590; AID1435127; AID1435128; AID353813
Corticotropin-releasing factor receptor 1	Rattus norvegicus (Norway rat)	IC50 (µMol)	0.0368	0.0042	0.0303	0.1290	AID1799009; AID353808; AID353812; AID609183
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
muscle contraction	Substance-K receptor	Homo sapiens (human)
tachykinin receptor signaling pathway	Substance-K receptor	Homo sapiens (human)
positive regulation of acetylcholine secretion, neurotransmission	Substance-K receptor	Homo sapiens (human)
intestine smooth muscle contraction	Substance-K receptor	Homo sapiens (human)
negative regulation of luteinizing hormone secretion	Substance-K receptor	Homo sapiens (human)
operant conditioning	Substance-K receptor	Homo sapiens (human)
positive regulation of vascular permeability	Substance-K receptor	Homo sapiens (human)
positive regulation of monoatomic ion transport	Substance-K receptor	Homo sapiens (human)
positive regulation of smooth muscle contraction	Substance-K receptor	Homo sapiens (human)
response to electrical stimulus	Substance-K receptor	Homo sapiens (human)
prolactin secretion	Substance-K receptor	Homo sapiens (human)
positive regulation of uterine smooth muscle contraction	Substance-K receptor	Homo sapiens (human)
positive regulation of flagellated sperm motility	Substance-K receptor	Homo sapiens (human)
synaptic transmission, dopaminergic	Corticotropin-releasing factor-binding protein	Homo sapiens (human)
inflammatory response	Corticotropin-releasing factor-binding protein	Homo sapiens (human)
signal transduction	Corticotropin-releasing factor-binding protein	Homo sapiens (human)
female pregnancy	Corticotropin-releasing factor-binding protein	Homo sapiens (human)
learning or memory	Corticotropin-releasing factor-binding protein	Homo sapiens (human)
hormone-mediated signaling pathway	Corticotropin-releasing factor-binding protein	Homo sapiens (human)
cellular response to potassium ion	Corticotropin-releasing factor-binding protein	Homo sapiens (human)
regulated exocytosis	Corticotropin-releasing factor-binding protein	Homo sapiens (human)
behavioral response to ethanol	Corticotropin-releasing factor-binding protein	Homo sapiens (human)
regulation of corticotropin secretion	Corticotropin-releasing factor-binding protein	Homo sapiens (human)
negative regulation of corticotropin secretion	Corticotropin-releasing factor-binding protein	Homo sapiens (human)
cellular response to calcium ion	Corticotropin-releasing factor-binding protein	Homo sapiens (human)
cellular response to cocaine	Corticotropin-releasing factor-binding protein	Homo sapiens (human)
cellular response to cAMP	Corticotropin-releasing factor-binding protein	Homo sapiens (human)
cellular response to tumor necrosis factor	Corticotropin-releasing factor-binding protein	Homo sapiens (human)
cellular response to estrogen stimulus	Corticotropin-releasing factor-binding protein	Homo sapiens (human)
cellular response to estradiol stimulus	Corticotropin-releasing factor-binding protein	Homo sapiens (human)
cellular response to xenobiotic stimulus	Corticotropin-releasing factor-binding protein	Homo sapiens (human)
regulation of cellular response to stress	Corticotropin-releasing factor-binding protein	Homo sapiens (human)
cellular response to gonadotropin-releasing hormone	Corticotropin-releasing factor-binding protein	Homo sapiens (human)
negative regulation of corticotropin-releasing hormone receptor activity	Corticotropin-releasing factor-binding protein	Homo sapiens (human)
regulation of NMDA receptor activity	Corticotropin-releasing factor-binding protein	Homo sapiens (human)
immune response	Corticotropin-releasing factor receptor 1	Homo sapiens (human)
cell surface receptor signaling pathway	Corticotropin-releasing factor receptor 1	Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathway	Corticotropin-releasing factor receptor 1	Homo sapiens (human)
activation of adenylate cyclase activity	Corticotropin-releasing factor receptor 1	Homo sapiens (human)
female pregnancy	Corticotropin-releasing factor receptor 1	Homo sapiens (human)
parturition	Corticotropin-releasing factor receptor 1	Homo sapiens (human)
regulation of adenylate cyclase activity involved in G protein-coupled receptor signaling pathway	Corticotropin-releasing factor receptor 1	Homo sapiens (human)
adrenal gland development	Corticotropin-releasing factor receptor 1	Homo sapiens (human)
exploration behavior	Corticotropin-releasing factor receptor 1	Homo sapiens (human)
fear response	Corticotropin-releasing factor receptor 1	Homo sapiens (human)
behavioral response to ethanol	Corticotropin-releasing factor receptor 1	Homo sapiens (human)
corticotropin secretion	Corticotropin-releasing factor receptor 1	Homo sapiens (human)
general adaptation syndrome, behavioral process	Corticotropin-releasing factor receptor 1	Homo sapiens (human)
cellular response to corticotropin-releasing hormone stimulus	Corticotropin-releasing factor receptor 1	Homo sapiens (human)
negative regulation of voltage-gated calcium channel activity	Corticotropin-releasing factor receptor 1	Homo sapiens (human)
regulation of corticosterone secretion	Corticotropin-releasing factor receptor 1	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
tachykinin receptor activity	Substance-K receptor	Homo sapiens (human)
protein binding	Substance-K receptor	Homo sapiens (human)
substance K receptor activity	Substance-K receptor	Homo sapiens (human)
protein binding	Corticotropin-releasing factor-binding protein	Homo sapiens (human)
peptide binding	Corticotropin-releasing factor-binding protein	Homo sapiens (human)
corticotropin-releasing hormone binding	Corticotropin-releasing factor-binding protein	Homo sapiens (human)
protein binding	Corticotropin-releasing factor receptor 1	Homo sapiens (human)
corticotrophin-releasing factor receptor activity	Corticotropin-releasing factor receptor 1	Homo sapiens (human)
G protein-coupled peptide receptor activity	Corticotropin-releasing factor receptor 1	Homo sapiens (human)
corticotropin-releasing hormone binding	Corticotropin-releasing factor receptor 1	Homo sapiens (human)
corticotropin-releasing hormone receptor activity	Corticotropin-releasing factor receptor 1	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
plasma membrane	Substance-K receptor	Homo sapiens (human)
sperm flagellum	Substance-K receptor	Homo sapiens (human)
sperm head	Substance-K receptor	Homo sapiens (human)
sperm midpiece	Substance-K receptor	Homo sapiens (human)
sperm midpiece	Substance-K receptor	Homo sapiens (human)
plasma membrane	Substance-K receptor	Homo sapiens (human)
endoplasmic reticulum	Corticotropin-releasing factor-binding protein	Homo sapiens (human)
Golgi apparatus	Corticotropin-releasing factor-binding protein	Homo sapiens (human)
extracellular region	Corticotropin-releasing factor-binding protein	Homo sapiens (human)
extracellular space	Corticotropin-releasing factor-binding protein	Homo sapiens (human)
nucleus	Corticotropin-releasing factor-binding protein	Homo sapiens (human)
secondary lysosome	Corticotropin-releasing factor-binding protein	Homo sapiens (human)
multivesicular body	Corticotropin-releasing factor-binding protein	Homo sapiens (human)
microtubule	Corticotropin-releasing factor-binding protein	Homo sapiens (human)
secretory granule	Corticotropin-releasing factor-binding protein	Homo sapiens (human)
dendrite	Corticotropin-releasing factor-binding protein	Homo sapiens (human)
dense core granule	Corticotropin-releasing factor-binding protein	Homo sapiens (human)
varicosity	Corticotropin-releasing factor-binding protein	Homo sapiens (human)
perikaryon	Corticotropin-releasing factor-binding protein	Homo sapiens (human)
axon terminus	Corticotropin-releasing factor-binding protein	Homo sapiens (human)
extracellular space	Corticotropin-releasing factor-binding protein	Homo sapiens (human)
endosome	Corticotropin-releasing factor receptor 1	Homo sapiens (human)
plasma membrane	Corticotropin-releasing factor receptor 1	Homo sapiens (human)
membrane	Corticotropin-releasing factor receptor 1	Homo sapiens (human)
plasma membrane	Corticotropin-releasing factor receptor 1	Homo sapiens (human)
neuron projection	Corticotropin-releasing factor receptor 1	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (228)

Assay ID	Title	Year	Journal	Article
AID354074	Inhibition of ligand binding in neurokinin 2 receptor	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID353851	Clearance in chimpanzee at 0.5 mg/kg, iv	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1218681	AUC (infinity) in Sprague-Dawley rat at 5 mg/kg, po	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID353829	Ex vivo receptor occupancy of CRF receptor in rat brain at 10 mg/kg, po by [125I]sauvagine binding and autoradiography relative to control	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID354084	Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in intrapleural pressure at 5 mg/kg after intravenous infusion for 30 mins (RVb= -90.8+/-103 %)	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1218679	Cmax in Sprague-Dawley rat at 5 mg/kg, po	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID354104	Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in airway resistance at 5 mg/kg after intravenous infusion for 30 mins (RVb= 20.2+/-12.3 %)	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID353832	Toxicity in rat assessed as total distance traveled at 3 mg/kg, po after 1 hr by spontaneous locomotor test	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID353810	Cmax in Beagle dog at 1 mg/kg, po by cassette dosing	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID353828	Ex vivo receptor occupancy of CRF receptor in rat brain at 3 mg/kg, po by [125I]sauvagine binding and autoradiography relative to control	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID354329	Effect on acute renal function in rat assessed as change in urine potassium level per 100 gm body weight at 30 mg/kg, po (RVb= 60.3+/-11.1 mg/dl)	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID353854	Elimination half life in chimpanzee at 1 mg/kg, po	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID354080	Plasma concentration in dog at 5 mg/kg after intravenous infusion for 30 mins	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1218706	Drug metabolism in dog liver microsomes assessed as BMS-572273 metabolite level at 100 uM after 1 hr in presence of NADPH	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID353844	Cmax in rat at 5 mg/kg, po	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1435128	Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes preincubated for 1 hr followed by compound washout for 2 hrs and subsequent addition of [125I]-CRF measured after 1 hr by liquid scintillation counting method
AID354334	Effect on acute renal function in rat assessed as change in urine urea level per 100 gm body weight at 30 mg/kg, po (RVb= 321+/-62 mg/dl)	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID353838	Toxicity in rat assessed as time spent on rotarod at 10 mg/kg, po after 1 hr by rotarod test	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID354094	Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in tidal volume at 5 mg/kg after intravenous infusion for 6 mins (RVb= 5.8+/-3.8 %)	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID353817	Aqueous solubility at pH 7.4	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1218701	Drug metabolism in dog liver microsomes assessed as DPH-124921 metabolite level at 100 uM after 1 hr in presence of NADPH	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218695	Drug metabolism in rat liver microsomes assessed as DPH-123554 metabolite level at 100 uM after 1 hr in presence of NADPH	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID353822	Anxiolytic activity in rat assessed as increase in time spent on open arm at 18 mg/kg, po by elevated plus-maze test	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1218618	Drug metabolism in cynomolgus monkey cryopreserved hepatocytes assessed as decrease of compound level at 25 uM after 3 hrs by HPLC analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID354090	Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in respiration rate at 5 mg/kg after intravenous infusion for 6 mins (RVb= -8.3+/-8.3 %)	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1218694	Drug metabolism in mouse liver microsomes assessed as DPH-123554 metabolite level at 100 uM after 1 hr in presence of NADPH	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218620	Drug metabolism in mouse hepatocytes at 25 uM after 3 hrs by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID353853	Elimination half life in chimpanzee at 0.5 mg/kg, iv	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID353858	Cardiovascular activity in mongrel dog assessed as change in QRS intervals	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID354335	Effect on acute renal function in rat assessed as change in glucose level in urine per 100 gm body weight at 30 mg/kg, po (RVb= 9.9+/-1.9 mg/dl)	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1218700	Drug metabolism in rat liver microsomes assessed as DPH-124921 metabolite level at 100 uM after 1 hr in presence of NADPH	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID354333	Effect on acute renal function in rat assessed as change in urine creatinine level per 100 gm body weight at 30 mg/kg, po (RVb= 16.2+/-3.3 mg/dl)	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1218626	Drug metabolism in rat hepatocytes assessed as DPH-123554 metabolite level at 25 uM after 3 hrs by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID354088	Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in peak expiratory flow at 5 mg/kg after intravenous infusion for 30 mins (RVb= -3.3+/-6.4 %)	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1218715	Detection of compound level in rat hepatocytes treated with 25 uM of BMS-562086 after 3 hrs by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218705	Drug metabolism in rat liver microsomes assessed as BMS-572273 metabolite level at 100 uM after 1 hr in presence of NADPH	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218606	Drug metabolism in rat hepatocytes assessed as 7-hydroxycoumarin formation at 25 uM after 3 hrs by HPLC analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218684	AUC (infinity) in beagle dog at 1 mg/kg, iv	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218707	Drug metabolism in cynomolgus monkey liver microsomes assessed as BMS-572273 metabolite level at 100 uM after 1 hr in presence of NADPH	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID354102	Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in airway resistance at 5 mg/kg after intravenous infusion for 6 mins (RVb= 3.9+/-4.7 %)	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1218673	Drug metabolism in rat hepatocytes assessed as BMS-572273 metabolite level at 25 uM after 3 hrs by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID353818	Solubility in 0.01 N HCl at pH 2.5	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID354113	Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in mean arterial pressure at 5 mg/kg after intravenous infusion for 60 mins (RVb= 5.1+/-3.5 %)	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID354331	Effect on acute renal function in rat assessed as change in urine protein level per 100 gm body weight at 30 mg/kg, po (RVb= 12.0+/-2.4 mg/dl)	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID353848	AUC (0 to infinity) in chimpanzee at 0.5 mg/kg, iv	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1218688	Drug metabolism in human cryopreserved hepatocytes assessed as BMS-572273 metabolite level at 25 uM after 3 hrs by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218639	Terminal half life in chimpanzee at 0.5 mg/kg, iv	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218696	Drug metabolism in beagle dog liver microsomes assessed as DPH-123554 metabolite level at 100 uM after 1 hr in presence of NADPH	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218668	Drug metabolism in rat hepatocytes assessed as DPH-124921 metabolite level at 25 uM after 3 hrs by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218664	Detection of compound level in cynomolgus monkey liver microsomes treated with 25 uM of BMS-562086 after 3 hrs by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID353834	Toxicity in rat assessed as total distance traveled at 30 mg/kg, po after 1 hr by spontaneous locomotor test	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID353846	AUC in rat at 1 mg/kg, iv and 5 mg/kg, po	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID354097	Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in tidal volume at 5 mg/kg after intravenous infusion for 60 mins (RVb= 13.0+/-10.3 %)	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID354121	Plasma concentration in spontaneously breathing dog at 5 mg/kg, iv after 60 mins	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID353850	Cmax in chimpanzee at 1 mg/kg, po	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1218717	Detection of compound level in cynomolgus monkey cryopreserved hepatocytes treated with 25 uM of BMS-562086 after 3 hrs by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218704	Drug metabolism in mouse liver microsomes assessed as BMS-572273 metabolite level at 100 uM after 1 hr in presence of NADPH	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID354089	Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in peak expiratory flow at 5 mg/kg after intravenous infusion for 60 mins (RVb= 0.4+/-6.7 %)	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID353820	Solubility in acetone	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1218634	Tmax in beagle dog at 5 mg/kg, po	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218602	Drug metabolism in beagle dog hepatocytes assessed as 7-ethoxycoumarin formation at 25 uM after 3 hrs by HPLC analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218644	AUC (infinity) in chimpanzee at 1 mg/kg, po	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218685	Terminal half life in beagle dog at 1 mg/kg, iv	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218609	Drug metabolism in human cryopreserved hepatocytes assessed as 7-hydroxycoumarin formation at 25 uM after 3 hrs by HPLC analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID353827	Ex vivo receptor occupancy of CRF receptor in rat brain at 1 mg/kg, po by [125I]sauvagine binding and autoradiography relative to control	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID353806	Lipophilicity log P of the compound	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1218646	Oral bioavailability in chimpanzee at 5 mg/kg	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID354118	Plasma concentration in spontaneously breathing dog at 5 mg/kg, iv after 6 mins	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1218636	Terminal half life in beagle dog at 5 mg/kg, po	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218674	Drug metabolism in human liver microsomes assessed as BMS-572273 metabolite formation at 100 uM after 1 hr in presence of NADPH and ketoconazole	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218689	Drug metabolism in mouse liver microsomes at 100 uM after 1 hr in presence of NADPH	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218680	Tmax in Sprague-Dawley rat at 5 mg/kg, po	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218594	Protein binding in rat serum after 3 hrs by equilibrium dialysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218699	Drug metabolism in mouse liver microsomes assessed as DPH-124921 metabolite level at 100 uM after 1 hr in presence of NADPH	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218633	Cmax in beagle dog at 5 mg/kg, po	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218692	Drug metabolism in cynomolgus monkey liver microsomes at 100 uM after 1 hr in presence of NADPH	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218598	Metabolic stability in dog serum after 3 hrs by equilibrium dialysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218714	Detection of compound level in mouse hepatocytes treated with 25 uM of BMS-562086 after 3 hrs by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID353830	Ex vivo receptor occupancy of CRF receptor in rat brain at 30 mg/kg, po by [125I]sauvagine binding and autoradiography relative to control	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1218690	Drug metabolism in rat liver microsomes at 100 uM after 1 hr in presence of NADPH	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218686	Drug metabolism in beagle dog hepatocytes assessed as BMS-572273 metabolite level at 25 uM after 3 hrs by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID354105	Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in airway resistance at 5 mg/kg after intravenous infusion for 60 mins (RVb= 17.3+/-15.1 %)	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID354338	Plasma concentration in rat at 30 mg/kg, po after 1 hr	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1218617	Drug metabolism in beagle dog hepatocytes assessed as decrease of compound level at 25 uM after 3 hrs by HPLC analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218625	Drug metabolism in mouse hepatocytes assessed as DPH-123554 metabolite level at 25 uM after 3 hrs by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID353811	Half life in Beagle dog at 1 mg/kg, po by cassette dosing	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1218678	Terminal volume of distribution in Sprague-Dawley rat at 1 mg/kg, iv	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID354101	Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in minute volume at 5 mg/kg after intravenous infusion for 60 mins (RVb= -13.4+/-10.7 %)	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1218631	Plasma clearance in beagle dog at 1 mg/kg, iv	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218628	Drug metabolism in cynomolgus monkey cryopreserved hepatocytes assessed as DPH-123554 metabolite level at 25 uM after 3 hrs by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1435127	Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes preincubated for 1 hr followed by [125I]-CRF addition measured after 1 hr by liquid scintillation counting method
AID1218622	Drug metabolism in beagle dog hepatocytes at 25 uM after 3 hrs by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218691	Drug metabolism in dog liver microsomes at 100 uM after 1 hr in presence of NADPH	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID353809	AUC in Beagle dog at 1 mg/kg, po by cassette dosing	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID353845	Tmax in rat at 5 mg/kg, po	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID354107	Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in pulmonary compliance at 5 mg/kg after intravenous infusion for 15 mins (RVb= 0.8+/-2.0 %)	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1218675	AUC (infinity) in Sprague-Dawley rat at 1 mg/kg, iv	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID354079	Plasma concentration in dog at 3 mg/kg after intravenous infusion for 30 mins	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID353826	Ex vivo receptor occupancy of CRF receptor in rat brain at 0.3 mg/kg, po by [125I]sauvagine binding and autoradiography relative to control	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID354108	Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in pulmonary compliance at 5 mg/kg after intravenous infusion for 30 mins (RVb= -2.8+/-4.0 %)	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1218599	Metabolic stability in human serum after 3 hrs by equilibrium dialysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218716	Detection of compound level in beagle dog hepatocytes treated with 25 uM of BMS-562086 after 3 hrs by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID354116	Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in heart rate at 5 mg/kg after intravenous infusion for 30 mins (RVb= -0.9+/-3.8 %)	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1218682	Terminal half life in Sprague-Dawley rat at 5 mg/kg, po	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID354075	Cardiovascular activity in spontaneously breathing mongrel dog at assessed as increase in contractility at 3 mg/kg to 5 mg/kg, iv by dose escalation study	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID353833	Toxicity in rat assessed as total distance traveled at 10 mg/kg, po after 1 hr by spontaneous locomotor test	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID354078	Plasma concentration in dog at 1 mg/kg after intravenous infusion for 30 mins	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID354081	Cardiovascular activity in mongrel dog assessed as change in heart rate	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1218697	Drug metabolism in cynomolgus monkey liver microsomes assessed as DPH-123554 metabolite level at 100 uM after 1 hr in presence of NADPH	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID354109	Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in pulmonary compliance at 5 mg/kg after intravenous infusion for 60 mins (RVb= -4.8+/-4.5 %)	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1218615	Drug metabolism in mouse hepatocytes assessed as decrease of compound level at 25 uM after 3 hrs by HPLC analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID353814	Displacement of [125I]Tyr0-sauvagine from CRF2beta receptor expressed in pig choroid plexus membrane	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1218595	Protein binding in dog serum after 3 hrs by equilibrium dialysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218623	Drug metabolism in cynomolgus monkey cryopreserved hepatocytes at 25 uM after 3 hrs by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218593	Apparent permeability from apical to basolateral side in human Caco2 cells	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID354339	Plasma concentration in rat at 30 mg/kg, po after 5 hrs	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID353843	Elimination half life in rat at 1 mg/kg, iv and 5 mg/kg, po	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID353808	Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID354087	Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in peak expiratory flow at 5 mg/kg after intravenous infusion for 15 mins (RVb= -8.4+/-6.6 %)	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID354092	Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in respiration rate at 5 mg/kg after intravenous infusion for 30 mins (RVb= -4.5+/-8.2 %)	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID354131	Effect on acute renal function in rat assessed as change in urine chloride level per 100 gm body weight at 30 mg/kg, po (RVb= 95.3+/-11.6 mg/dl)	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID353859	Cardiovascular activity in mongrel dog assessed as change in PR intervals	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1218676	Terminal half life in Sprague-Dawley rat at 1 mg/kg, iv	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID353841	Clearance in rat at 1 mg/kg, iv and 5 mg/kg, po	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID353839	Toxicity in rat assessed as time spent on rotarod at 30 mg/kg, po after 1 hr by rotarod test	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID353812	Antagonist activity at CRF1 receptor in rat pituitary cells assessed as inhibition of CRF-mediated ACTH production	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID354120	Plasma concentration in spontaneously breathing dog at 5 mg/kg, iv after 30 mins	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID354093	Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in respiration rate at 5 mg/kg after intravenous infusion for 60 mins (RVb= -19.5+/-16.3 %)	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID353816	Binding affinity to human neurokinin 2 receptor	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1218601	Drug metabolism in rat hepatocytes assessed as 7-ethoxycoumarin formation at 25 uM after 3 hrs by HPLC analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218672	Drug metabolism in mouse hepatocytes assessed as BMS-572273 metabolite level at 25 uM after 3 hrs by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID354115	Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in heart rate at 5 mg/kg after intravenous infusion for 15 mins (RVb= -2.3+/-1.7 %)	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID354112	Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in mean arterial pressure at 5 mg/kg after intravenous infusion for 30 mins (RVb= 4.0+/-3.0 %)	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1218698	Drug metabolism in human liver microsomes assessed as DPH-123554 metabolite level at 100 uM after 1 hr in presence of NADPH	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID354091	Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in respiration rate at 5 mg/kg after intravenous infusion for 15 mins (RVb= -6.4+/-4.0 %)	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1218632	Terminal volume of distribution in beagle dog at 1 mg/kg, iv	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218667	Drug metabolism in human liver microsomes assessed as DPH-124921 metabolite formation at 100 uM after 1 hr in presence of NADPH and ketoconazole	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218643	Tmax in chimpanzee at 1 mg/kg, po	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218640	Plasma clearance in chimpanzee at 0.5 mg/kg, iv	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID353823	Anxiolytic activity in rat assessed as increase in time spent on open arm at 30 mg/kg, po by elevated plus-maze test	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID354085	Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in intrapleural pressure at 5 mg/kg after intravenous infusion for 60 mins (RVb= 18.5+/-19.9 %)	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1218619	Drug metabolism in human cryopreserved hepatocytes assessed as decrease of compound level at 25 uM after 3 hrs by HPLC analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218708	Drug metabolism in human liver microsomes assessed as BMS-572273 metabolite level at 100 uM after 1 hr in presence of NADPH	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID354077	Plasma concentration in dog at 0.3 mg/kg after intravenous infusion for 30 mins	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1435129	Ratio of IC50 for displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes with compound washout to IC50 for displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes without compound wash
AID354119	Plasma concentration in spontaneously breathing dog at 5 mg/kg, iv after 15 mins	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID354336	Effect on acute renal function in rat assessed as change in osmolality in urine per 100 gm body weight at 30 mg/kg, po (RVb= 325+/-1.9 mg/dl)	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID353847	Oral bioavailability in rat at 5 mg/kg	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID354083	Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in intrapleural pressure at 5 mg/kg after intravenous infusion for 15 mins (RVb= 12.6+/-17.1 %)	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID354114	Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in heart rate at 5 mg/kg after intravenous infusion for 6 mins (RVb= -0.4+/-0.7 %)	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID353824	Anxiolytic activity in rat assessed as decrease in latency to exit dark chamber at 10 mg/kg, po by defensive withdrawal test relative to untreated control	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID354332	Effect on acute renal function in rat assessed as change in urine phosphate level per 100 gm body weight at 30 mg/kg, po (RVb= 8.7+/-2.3 mg/dl)	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1218660	Detection of compound level in human cryopreserved hepatocytes treated with 25 uM of BMS-562086 after 3 hrs by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID353835	Toxicity in rat assessed as total distance traveled at 100 mg/kg, po after 1 hr by spontaneous locomotor test	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1218663	Detection of compound level in beagle dog liver microsomes treated with 25 uM of BMS-562086 after 3 hrs by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID353855	Oral bioavailability in chimpanzee at 1 mg/kg	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1218605	Drug metabolism in mouse hepatocytes assessed as 7-hydroxycoumarin formation at 25 uM after 3 hrs by HPLC analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218597	Metabolic stability in rat serum after 3 hrs by equilibrium dialysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218591	Binding affinity to CRF-binding protein (unknown origin)	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID354096	Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in tidal volume at 5 mg/kg after intravenous infusion for 30 mins (RVb= 6.1+/-5.6 %)	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1218647	Retention time of the compound by HPLC method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID353861	Cardiovascular activity in dog assessed as increase in mean atrial pressure at 3 mg to 5 mg/kg, iv by dose escalation study	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID353837	Toxicity in rat assessed as time spent on rotarod at 3 mg/kg, po after 1 hr by rotarod test	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID354086	Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in peak expiratory flow at 5 mg/kg after intravenous infusion for 6 mins (RVb= 3.6+/-3.7 %)	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1218661	Detection of compound level in mouse liver microsomes treated with 25 uM of BMS-562086 after 3 hrs by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID354344	Agonist activity at CRF1 receptor in rat pituitary cells	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1218608	Drug metabolism in cynomolgus monkey cryopreserved hepatocytes assessed as 7-hydroxycoumarin formation at 25 uM after 3 hrs by HPLC analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218637	Oral bioavailability in beagle dog at 5 mg/kg	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID354082	Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in intrapleural pressure at 5 mg/kg after intravenous infusion for 6 mins (RVb= -21.2+/-26.5 %)	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID353849	AUC (0 to infinity) in chimpanzee at 1 mg/kg, po	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1218702	Drug metabolism in cynomolgus monkey liver microsomes assessed as DPH-124921 metabolite level at 100 uM after 1 hr in presence of NADPH	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218693	Drug metabolism in human liver microsomes at 100 uM after 1 hr in presence of NADPH	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID354103	Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in airway resistance at 5 mg/kg after intravenous infusion for 15 mins (RVb= 27.8+/-17.9 %)	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1218592	Selectivity ratio of IC50 for CRF-binding protein (unknown origin) to IC50 for human CRF1 receptor	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID353825	Anxiolytic activity in rat assessed as decrease in latency to exit dark chamber at 3 mg/kg, po by defensive withdrawal test relative to untreated control	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID354110	Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in mean arterial pressure at 5 mg/kg after intravenous infusion for 6 mins (RVb= 1.5+/-0.9 %)	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1218645	Terminal half life in chimpanzee at 1 mg/kg, po	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID354098	Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in minute volume at 5 mg/kg after intravenous infusion for 6 mins (RVb= -3.6+/-7.5 %)	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1218642	Cmax in chimpanzee at 1 mg/kg, po	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218666	Drug metabolism in human liver microsomes assessed as DPH-123554 metabolite formation at 100 uM after 1 hr in presence of NADPH and ketoconazole	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID353836	Toxicity in rat assessed as time spent on rotarod at 1 mg/kg, po after 1 hr by rotarod test	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1218596	Protein binding in human serum after 3 hrs by equilibrium dialysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218669	Drug metabolism in beagle dog hepatocytes assessed as DPH-124921 metabolite level at 25 uM after 3 hrs by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218662	Detection of compound level in rat liver microsomes treated with 25 uM of BMS-562086 after 3 hrs by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID353840	Toxicity in rat assessed as time spent on rotarod at 100 mg/kg, po after 1 hr by rotarod test	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1218630	Drug metabolism in mouse hepatocytes assessed as DPH-124921 metabolite level at 25 uM after 3 hrs by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID353819	Solubility in ethanol	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID609183	Displacement of [125I]-sauvagine from rat CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting	2011	Journal of medicinal chemistry, Jun-23, Volume: 54, Issue:12	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.
AID1218635	AUC (infinity) in beagle dog at 5 mg/kg, po	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID354337	Effect on acute renal function in rat assessed as change in urine volume per 100 gm body weight at 30 mg/kg, po (RVb= 1.7+/-0.2 ml/100g)	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID354076	Binding affinity to human recombinant CRF binding protein	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1218703	Drug metabolism in human liver microsomes assessed as DPH-124921 metabolite level at 100 uM after 1 hr in presence of NADPH	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218600	Drug metabolism in mouse hepatocytes assessed as 7-ethoxycoumarin formation at 25 uM after 3 hrs by HPLC analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID353842	Volume of distribution at steady state in rat at 1 mg/kg, iv and 5 mg/kg, po	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1218590	Antagonist activity at human CRF1 receptor	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID354111	Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in mean arterial pressure at 5 mg/kg after intravenous infusion for 15 mins (RVb= 2.1+/-1.5 %)	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID354330	Effect on acute renal function in rat assessed as change in urine sodium level per 100 gm body weight at 30 mg/kg, po (RVb= 49.9+/-3.1 mg/dl)	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID354099	Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in minute volume at 5 mg/kg after intravenous infusion for 15 mins (RVb= -4.7+/-3.4 %)	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1218629	Drug metabolism in human cryopreserved hepatocytes assessed as DPH-123554 metabolite level at 25 uM after 3 hrs by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218616	Drug metabolism in rat hepatocytes assessed as decrease of compound level at 25 uM after 3 hrs by HPLC analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218687	Drug metabolism in cynomolgus monkey cryopreserved hepatocytes assessed as BMS-572273 metabolite level at 25 uM after 3 hrs by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218683	Oral bioavailability in Sprague-Dawley rat at 5 mg/kg	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID354095	Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in tidal volume at 5 mg/kg after intravenous infusion for 15 mins (RVb= 2.2+/-4.3 %)	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID354100	Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in minute volume at 5 mg/kg after intravenous infusion for 30 mins (RVb= 1.0+/-9.7 %)	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1218627	Drug metabolism in beagle dog hepatocytes assessed as DPH-123554 metabolite level at 25 uM after 3 hrs by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID354130	Effect on acute renal function in rat assessed as change in urine pH per 100 gm body weight at 30 mg/kg, po (RVb= 7.74+/-0.07 mg/dl)	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1218677	Plasma clearance in Sprague-Dawley rat at 1 mg/kg, iv	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218638	AUC (infinity) in chimpanzee at 0.5 mg/kg, iv	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218665	Detection of compound level in human liver microsomes treated with 25 uM of BMS-562086 after 3 hrs by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218621	Drug metabolism in rat hepatocytes at 25 uM after 3 hrs by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218604	Drug metabolism in human cryopreserved hepatocytes assessed as 7-ethoxycoumarin formation at 25 uM after 3 hrs by HPLC analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID353815	Binding affinity to rat adenosine A1 receptor expressed in CHO cells	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1218641	Terminal volume of distribution in chimpanzee at 0.5 mg/kg, iv	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218670	Drug metabolism in cynomolgus monkey cryopreserved hepatocytes assessed as DPH-124921 metabolite level at 25 uM after 3 hrs by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID353860	Cardiovascular activity in dog assessed as increase in mean atrial pressure at 5 mg/kg, iv	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID354343	Inhibition of ligand binding in adenosine A1 receptor	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID353857	Cardiovascular activity in mongrel dog assessed as change in QT intervals	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1218603	Drug metabolism in cynomolgus monkey cryopreserved hepatocytes assessed as 7-ethoxycoumarin formation at 25 uM after 3 hrs by HPLC analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID353852	Volume of distribution at steady state in chimpanzee at 0.5 mg/kg, iv	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1218671	Drug metabolism in human cryopreserved hepatocytes assessed as DPH-124921 metabolite level at 25 uM after 3 hrs by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID354117	Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in heart rate at 5 mg/kg after intravenous infusion for 60 mins (RVb= -0.9+/-5.8 %)	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1218624	Drug metabolism in human cryopreserved hepatocytes at 25 uM after 3 hrs by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID353813	Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in human IMR32 cells	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID354106	Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in pulmonary compliance at 5 mg/kg after intravenous infusion for 6 mins (RVb= 6.0+/-4.2 %)	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1218607	Drug metabolism in beagle dog hepatocytes assessed as 7-hydroxycoumarin formation at 25 uM after 3 hrs by HPLC analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6	In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID353831	Toxicity in rat assessed as total distance traveled at 1 mg/kg, po after 1 hr by spontaneous locomotor test	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID353856	Cardiovascular activity in mongrel dog assessed as change in QTc intervals	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
AID1799009	In Vitro Binding Autoradiography from Article 10.1021/jm900025h: \\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.\\	2009	Journal of medicinal chemistry, May-14, Volume: 52, Issue:9	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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	2 (16.67)	29.6817
2010's	9 (75.00)	24.3611
2020's	1 (8.33)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	5 (38.46%)	5.53%
Reviews	0 (0.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	8 (61.54%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Trials	Classes	Roles
chlordiazepoxide Chlordiazepoxide: An anxiolytic benzodiazepine derivative with anticonvulsant, sedative, and amnesic properties. It has also been used in the symptomatic treatment of alcohol withdrawal.. chlordiazepoxide : A benzodiazepine that is 3H-1,4-benzodiazepine 4-oxide substituted by a chloro group at position 7, a phenyl group at position 5 and a methylamino group at position 2.	2.05	1	0	benzodiazepine
citalopram Citalopram: A furancarbonitrile that is one of the serotonin uptake inhibitors used as an antidepressant. The drug is also effective in reducing ethanol uptake in alcoholics and is used in depressed patients who also suffer from TARDIVE DYSKINESIA in preference to tricyclic antidepressants, which aggravate dyskinesia.. citalopram : A racemate comprising equimolar amounts of (R)-citalopram and its enantiomer, escitalopram. It is used as an antidepressant, although only escitalopram is active.. 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-2-benzofuran-5-carbonitrile : A nitrile that is 1,3-dihydro-2-benzofuran-5-carbonitrile in which one of the hydrogens at position 1 is replaced by a p-fluorophenyl group, while the other is replaced by a 3-(dimethylamino)propyl group.	4.36	1	1	2-benzofurans; cyclic ether; nitrile; organofluorine compound; tertiary amino compound
furosemide Furosemide: A benzoic-sulfonamide-furan. It is a diuretic with fast onset and short duration that is used for EDEMA and chronic RENAL INSUFFICIENCY.. furosemide : A chlorobenzoic acid that is 4-chlorobenzoic acid substituted by a (furan-2-ylmethyl)amino and a sulfamoyl group at position 2 and 5 respectively. It is a diuretic used in the treatment of congestive heart failure.	2.05	1	0	chlorobenzoic acid; furans; sulfonamide	environmental contaminant; loop diuretic; xenobiotic
thyroxine Thyroxine: The major hormone derived from the thyroid gland. Thyroxine is synthesized via the iodination of tyrosines (MONOIODOTYROSINE) and the coupling of iodotyrosines (DIIODOTYROSINE) in the THYROGLOBULIN. Thyroxine is released from thyroglobulin by proteolysis and secreted into the blood. Thyroxine is peripherally deiodinated to form TRIIODOTHYRONINE which exerts a broad spectrum of stimulatory effects on cell metabolism.. thyroxine : An iodothyronine compound having iodo substituents at the 3-, 3'-, 5- and 5'-positions.	2.31	1	0	2-halophenol; iodophenol; L-phenylalanine derivative; non-proteinogenic L-alpha-amino acid; thyroxine zwitterion; thyroxine	antithyroid drug; human metabolite; mouse metabolite; thyroid hormone
carbachol Carbachol: A slowly hydrolyzed CHOLINERGIC AGONIST that acts at both MUSCARINIC RECEPTORS and NICOTINIC RECEPTORS.	2.05	1	0	ammonium salt; carbamate ester	cardiotonic drug; miotic; muscarinic agonist; nicotinic acetylcholine receptor agonist; non-narcotic analgesic
alanine Alanine: A non-essential amino acid that occurs in high levels in its free state in plasma. It is produced from pyruvate by transamination. It is involved in sugar and acid metabolism, increases IMMUNITY, and provides energy for muscle tissue, BRAIN, and the CENTRAL NERVOUS SYSTEM.. alanine : An alpha-amino acid that consists of propionic acid bearing an amino substituent at position 2.	2.07	1	0	alanine zwitterion; alanine; L-alpha-amino acid; proteinogenic amino acid; pyruvate family amino acid	EC 4.3.1.15 (diaminopropionate ammonia-lyase) inhibitor; fundamental metabolite
mannitol [no description available]	2.07	1	0	mannitol	allergen; antiglaucoma drug; compatible osmolytes; Escherichia coli metabolite; food anticaking agent; food bulking agent; food humectant; food stabiliser; food thickening agent; hapten; metabolite; osmotic diuretic; sweetening agent
indazoles Indazoles: A group of heterocyclic aromatic organic compounds consisting of the fusion of BENZENE and PYRAZOLES.	2.08	1	0	indazole
isoxazoles Isoxazoles: Azoles with an OXYGEN and a NITROGEN next to each other at the 1,2 positions, in contrast to OXAZOLES that have nitrogens at the 1,3 positions.. isoxazole : A monocyclic heteroarene with a structure consisting of a 5-membered ring containing three carbon atoms and an oxygen and nitrogen atom adjacent to each other. It is the parent of the class of isoxazoles.. isoxazoles : Oxazoles in which the N and O atoms are adjacent.	2.07	1	0	isoxazoles; mancude organic heteromonocyclic parent; monocyclic heteroarene
methamphetamine Methamphetamine: A central nervous system stimulant and sympathomimetic with actions and uses similar to DEXTROAMPHETAMINE. The smokable form is a drug of abuse and is referred to as crank, crystal, crystal meth, ice, and speed.. methamphetamine : A member of the class of amphetamines in which the amino group of (S)-amphetamine carries a methyl substituent.	8.56	1	1	amphetamines; secondary amine	central nervous system stimulant; environmental contaminant; neurotoxin; psychotropic drug; xenobiotic
7-ethoxycoumarin 7-ethoxycoumarin : A member of the class of coumarins that is umbelliferone in which the hydroxy group at position 7 is replaced by an ethoxy group.	2.07	1	0	aromatic ether; coumarins
atropine tropan-3alpha-yl 3-hydroxy-2-phenylpropanoate : A tropane alkaloid that is (1R,5)-8-methyl-8-azabicyclo[3.2.1]octane substituted by a (3-hydroxy-2-phenylpropanoyl)oxy group at position 3.	2.05	1	0
nbi 27914 [no description available]	2.06	1	0	dialkylarylamine; tertiary amino compound
razaxaban razaxaban: structure in first source	2.07	1	0
7-hydroxycoumarin 7-oxycoumarin: derivatives have anti-oxidant properties. umbelliferone : A hydroxycoumarin that is coumarin substituted by a hydroxy group ay position 7.	2.07	1	0	hydroxycoumarin	fluorescent probe; food component; plant metabolite
cp 154526 [no description available]	2.06	1	0
heroin Heroin: A narcotic analgesic that may be habit-forming. It is a controlled substance (opium derivative) listed in the U.S. Code of Federal Regulations, Title 21 Parts 329.1, 1308.11 (1987). Sale is forbidden in the United States by Federal statute. (Merck Index, 11th ed). heroin : A morphinane alkaloid that is morphine bearing two acetyl substituents on the O-3 and O-6 positions. As with other opioids, heroin is used as both an analgesic and a recreational drug. Frequent and regular administration is associated with tolerance and physical dependence, which may develop into addiction. Its use includes treatment for acute pain, such as in severe physical trauma, myocardial infarction, post-surgical pain, and chronic pain, including end-stage cancer and other terminal illnesses.	8.56	1	1	morphinane alkaloid	mu-opioid receptor agonist; opioid analgesic; prodrug
r 121919 [no description available]	2.06	1	0
nbi-34041 NBI-34041: high-affinity CRF1 (corticotropin-releasing factor receptor 1) receptor antagonist for attenuating elevated stress response	2.06	1	0
dmp 696 DMP 696: a CRF(1) receptor antagonist; structure in first source	2.46	2	0
brivanib [no description available]	2.07	1	0	aromatic ether; diether; fluoroindole; pyrrolotriazine; secondary alcohol	angiogenesis inhibitor; antineoplastic agent; apoptosis inducer; drug metabolite; EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor; fibroblast growth factor receptor antagonist
cp 154526 CP 154526: structure in first source	2.05	1	0

Condition	Indicated	Relationship Strength	Studies	Trials
Central Hypothyroidism [description not available]	0	2.31	1	0
Complications, Pregnancy [description not available]	0	2.31	1	0
Hypothyroidism A syndrome that results from abnormally low secretion of THYROID HORMONES from the THYROID GLAND, leading to a decrease in BASAL METABOLIC RATE. In its most severe form, there is accumulation of MUCOPOLYSACCHARIDES in the SKIN and EDEMA, known as MYXEDEMA. It may be primary or secondary due to other pituitary disease, or hypothalamic dysfunction.	0	2.31	1	0
Pregnancy The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH.	0	2.31	1	0
Vascular Malformations A spectrum of congenital, inherited, or acquired abnormalities in BLOOD VESSELS that can adversely affect the normal blood flow in ARTERIES or VEINS. Most are congenital defects such as abnormal communications between blood vessels (fistula), shunting of arterial blood directly into veins bypassing the CAPILLARIES (arteriovenous malformations), formation of large dilated blood blood-filled vessels (cavernous angioma), and swollen capillaries (capillary telangiectases). In rare cases, vascular malformations can result from trauma or diseases.	0	2.31	1	0
Chemical Dependence [description not available]	0	3.56	1	1
Drug Withdrawal Symptoms [description not available]	0	3.56	1	1
Substance Withdrawal Syndrome Physiological and psychological symptoms associated with withdrawal from the use of a drug after prolonged administration or habituation. The concept includes withdrawal from smoking or drinking, as well as withdrawal from an administered drug.	0	3.56	1	1
Substance-Related Disorders Disorders related to substance use or abuse.	0	3.56	1	1
Sensitivity and Specificity Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed)	0	2.08	1	0
Alcohol Abuse [description not available]	0	4.41	1	1
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)	0	4.41	1	1
Colitis, Mucous [description not available]	0	3.43	1	1
Anxiety Feelings or emotions of dread, apprehension, and impending disaster but not disabling as with ANXIETY DISORDERS.	0	3.43	1	1
Depression Depressive states usually of moderate intensity in contrast with MAJOR DEPRESSIVE DISORDER present in neurotic and psychotic disorders.	0	3.43	1	1
Irritable Bowel Syndrome A disorder with chronic or recurrent colonic symptoms without a clearcut etiology. This condition is characterized by chronic or recurrent ABDOMINAL PAIN, bloating, MUCUS in FECES, and an erratic disturbance of DEFECATION.	1	5.43	1	1
Anxiety Neuroses [description not available]	0	4.36	1	1
Anxiety Disorders Persistent and disabling ANXIETY.	1	6.36	1	1

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Cross-References

Synonyms (39)

Research Excerpts

Overview

Treatment

Pharmacokinetics

Bioavailability

Dosage Studied

Drug Classes (1)

Protein Targets (5)

Inhibition Measurements

Biological Processes (49)

Molecular Functions (8)

Ceullar Components (21)

Bioassays (228)

Research

Studies (12)

Market Indicators

Research Demand Index: 27.68

Study Types

pexacerfont

Cross-References

Synonyms (39)

Research Excerpts

Overview

Treatment

Pharmacokinetics

Bioavailability

Dosage Studied

Drug Classes (1)

Protein Targets (5)

Inhibition Measurements

Biological Processes (49)

Molecular Functions (8)

Ceullar Components (21)

Bioassays (228)

Research

Studies (12)

Market Indicators

Research Demand Index: 27.68

Study Types

Related Drugs (22)

Related Conditions (18)