amg 853 profile

vidupiprant: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ID Source	ID
PubMed CID	42641863
CHEMBL ID	1951575
SCHEMBL ID	4344221
MeSH ID	M0575690

Synonym
SCHEMBL4344221
bdbm50363928
D09990
1169483-24-2
vidupiprant (usan/inn)
vidupiprant [usan:inn]
61otz32xnc ,
vidupiprant
benzeneacetic acid, 5-chloro-4-(2-(((2-chloro-4-cyclopropylphenyl)sulfonyl)amino)-4- (((1,1-dimethylethyl)amino)carbonyl)phenoxy)-2-fluoro-
unii-61otz32xnc
AM806705
benzeneacetic acid, 5-chloro-4-[2-[[(2-chloro-4-cyclopropylphenyl)sulfonyl]amino]-4-[[(1,1-dimethylethyl)amino]carbonyl]phenoxy]-2-fluoro-
amg 853
CHEMBL1951575 ,
amg-853
vidupiprant [inn]
amg853
vidupiprant [who-dd]
2-(4-(4-(tert-butylcarbamoyl)-2-(2-chloro-4-cyclopropylbenzenesulfonamido)phenoxy)-5-chloro-2-fluorophenyl)acetic acid
vidupiprant [usan]
(4-(4-(tert-butylcarbamoyl)-2-(2-chloro-4-cyclopropylbenzenesulfonamido)phenoxy)-5-chloro-2-fluorophenyl)acetic acid
2-(4-(4-(tert-butylcarbamoyl)-2-(2-chloro-4-cyclopropylphenylsulfonamido)phenoxy)-5-chloro-2-fluorophenyl)acetic acid
DTXSID40151606
AKOS027422769
5-chloro-4-[2-[[(2-chloro-4-cyclopropylphenyl)sulfonyl]amino]-4-[[(1,1-dimethylethyl)amino]carbonyl]phenoxy]-2-fluorobenzeneacetic acid
amg 853(amg853;vidupiprant)
DB12272
2-(4-(4-(tert-butylcarbamoyl)-2-((2-chloro-4-cyclopropylphenyl)sulfonamido)phenoxy)-5-chloro-2-fluorophenyl)acetic acid
HY-14973
gtpl10169
compound 2 [pmid: 24900313]
2-[4-[4-(tert-butylcarbamoyl)-2-[(2-chloro-4-cyclopropylphenyl)sulfonylamino]phenoxy]-5-chloro-2-fluorophenyl]acetic acid
amg853; amg 853; amg-853
BCP28132
Q27263366
CS-0003670
MS-30687
EX-A6356

Excerpt	Reference	Relevance
"AMG 853 is a potent, selective, orally bioavailable, small-molecule dual antagonist of human D-prostanoid and CRTH2."	( Safety and efficacy of the prostaglandin D2 receptor antagonist AMG 853 in asthmatic patients. Budelsky, AL; Busse, WW; Chon, Y; Kerwin, EM; Lin, J; Lin, SL; Liu, MC; Meltzer, EO; Wenzel, SE; Zhang, N, 2013)	1.35

Excerpt	Reference	Relevance
" The most commonly reported adverse events were asthma, upper respiratory tract infection, and headache; 9 patients experienced serious adverse events, all of which were deemed unrelated to study treatment by the investigator."	( Safety and efficacy of the prostaglandin D2 receptor antagonist AMG 853 in asthmatic patients. Budelsky, AL; Busse, WW; Chon, Y; Kerwin, EM; Lin, J; Lin, SL; Liu, MC; Meltzer, EO; Wenzel, SE; Zhang, N, 2013)	0.63

Excerpt	Reference	Relevance
"2-(4-(4-(tert-Butylcarbamoyl)-2-(2-chloro-4-cyclopropylphenylsulfonamido)phenoxy)-5-chloro-2-fluorophenyl)acetic acid (AMG 853) is an orally bioavailable and potent dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors."	( Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors. Amore, BM; Banfield, C; Boudreaux, MD; Davis, JA; Emery, MG; Foti, RS; Pearson, JT; Prokop, SP; Rock, DA; Wahlstrom, JL; Wienkers, LC; Wong, SL; Zalikowski, JA, 2012)	0.85

Excerpt	Relevance	Reference
" Of these, 19k and 19s were tested in two different pharmacological models (acute FITC-mediated contact hypersensitivity and ovalbumin-induced eosinophilia models) and found to be active after oral dosing (10 and 30 mg/kg)."	( Discovery of potent, selective, and orally bioavailable alkynylphenoxyacetic acid CRTH2 (DP2) receptor antagonists for the treatment of allergic inflammatory diseases. Abla, N; Arrighi, JF; Augustine, JK; Burgat-Charvillon, F; Cleva, C; Crosignani, S; Daff, H; Fraboulet, G; Gaudet, M; Hamernig, I; Humbert, Y; Johnson, Z; Jorand-Lebrun, C; Juillard, P; Missotten, M; Prêtre, A; Rivron, D; Schneider, M; Schott, O; Seenisamy, J; Zimmerli, SC, 2011)	0.37

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Prostaglandin G/H synthase 2	Homo sapiens (human)	IC50 (µMol)	0.0040	0.0001	0.9950	10.0000	AID648029
Calpain-1 catalytic subunit	Sus scrofa (pig)	IC50 (µMol)	53.7500	0.0075	1.5285	7.5000	AID1417239; AID1417240
Prostaglandin D2 receptor	Homo sapiens (human)	IC50 (µMol)	0.0035	0.0001	1.1583	7.3000	AID648027; AID648029
Prostaglandin D2 receptor 2	Homo sapiens (human)	IC50 (µMol)	0.0035	0.0004	0.1009	0.9600	AID648027; AID648029
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Prostaglandin D2 receptor 2	Homo sapiens (human)	Kb	0.0002	0.0000	0.0003	0.0010	AID648031
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
prostaglandin biosynthetic process	Prostaglandin G/H synthase 2	Homo sapiens (human)
angiogenesis	Prostaglandin G/H synthase 2	Homo sapiens (human)
response to oxidative stress	Prostaglandin G/H synthase 2	Homo sapiens (human)
embryo implantation	Prostaglandin G/H synthase 2	Homo sapiens (human)
learning	Prostaglandin G/H synthase 2	Homo sapiens (human)
memory	Prostaglandin G/H synthase 2	Homo sapiens (human)
regulation of blood pressure	Prostaglandin G/H synthase 2	Homo sapiens (human)
negative regulation of cell population proliferation	Prostaglandin G/H synthase 2	Homo sapiens (human)
response to xenobiotic stimulus	Prostaglandin G/H synthase 2	Homo sapiens (human)
response to nematode	Prostaglandin G/H synthase 2	Homo sapiens (human)
response to fructose	Prostaglandin G/H synthase 2	Homo sapiens (human)
response to manganese ion	Prostaglandin G/H synthase 2	Homo sapiens (human)
positive regulation of vascular endothelial growth factor production	Prostaglandin G/H synthase 2	Homo sapiens (human)
cyclooxygenase pathway	Prostaglandin G/H synthase 2	Homo sapiens (human)
bone mineralization	Prostaglandin G/H synthase 2	Homo sapiens (human)
positive regulation of prostaglandin biosynthetic process	Prostaglandin G/H synthase 2	Homo sapiens (human)
positive regulation of fever generation	Prostaglandin G/H synthase 2	Homo sapiens (human)
positive regulation of synaptic plasticity	Prostaglandin G/H synthase 2	Homo sapiens (human)
negative regulation of synaptic transmission, dopaminergic	Prostaglandin G/H synthase 2	Homo sapiens (human)
prostaglandin secretion	Prostaglandin G/H synthase 2	Homo sapiens (human)
response to estradiol	Prostaglandin G/H synthase 2	Homo sapiens (human)
response to lipopolysaccharide	Prostaglandin G/H synthase 2	Homo sapiens (human)
positive regulation of peptidyl-serine phosphorylation	Prostaglandin G/H synthase 2	Homo sapiens (human)
response to vitamin D	Prostaglandin G/H synthase 2	Homo sapiens (human)
cellular response to heat	Prostaglandin G/H synthase 2	Homo sapiens (human)
response to tumor necrosis factor	Prostaglandin G/H synthase 2	Homo sapiens (human)
maintenance of blood-brain barrier	Prostaglandin G/H synthase 2	Homo sapiens (human)
positive regulation of protein import into nucleus	Prostaglandin G/H synthase 2	Homo sapiens (human)
hair cycle	Prostaglandin G/H synthase 2	Homo sapiens (human)
positive regulation of apoptotic process	Prostaglandin G/H synthase 2	Homo sapiens (human)
positive regulation of nitric oxide biosynthetic process	Prostaglandin G/H synthase 2	Homo sapiens (human)
negative regulation of cell cycle	Prostaglandin G/H synthase 2	Homo sapiens (human)
positive regulation of vasoconstriction	Prostaglandin G/H synthase 2	Homo sapiens (human)
negative regulation of smooth muscle contraction	Prostaglandin G/H synthase 2	Homo sapiens (human)
positive regulation of smooth muscle contraction	Prostaglandin G/H synthase 2	Homo sapiens (human)
decidualization	Prostaglandin G/H synthase 2	Homo sapiens (human)
positive regulation of smooth muscle cell proliferation	Prostaglandin G/H synthase 2	Homo sapiens (human)
regulation of inflammatory response	Prostaglandin G/H synthase 2	Homo sapiens (human)
brown fat cell differentiation	Prostaglandin G/H synthase 2	Homo sapiens (human)
response to glucocorticoid	Prostaglandin G/H synthase 2	Homo sapiens (human)
negative regulation of calcium ion transport	Prostaglandin G/H synthase 2	Homo sapiens (human)
positive regulation of synaptic transmission, glutamatergic	Prostaglandin G/H synthase 2	Homo sapiens (human)
response to fatty acid	Prostaglandin G/H synthase 2	Homo sapiens (human)
cellular response to mechanical stimulus	Prostaglandin G/H synthase 2	Homo sapiens (human)
cellular response to lead ion	Prostaglandin G/H synthase 2	Homo sapiens (human)
cellular response to ATP	Prostaglandin G/H synthase 2	Homo sapiens (human)
cellular response to hypoxia	Prostaglandin G/H synthase 2	Homo sapiens (human)
cellular response to non-ionic osmotic stress	Prostaglandin G/H synthase 2	Homo sapiens (human)
cellular response to fluid shear stress	Prostaglandin G/H synthase 2	Homo sapiens (human)
positive regulation of transforming growth factor beta production	Prostaglandin G/H synthase 2	Homo sapiens (human)
positive regulation of cell migration involved in sprouting angiogenesis	Prostaglandin G/H synthase 2	Homo sapiens (human)
positive regulation of fibroblast growth factor production	Prostaglandin G/H synthase 2	Homo sapiens (human)
positive regulation of brown fat cell differentiation	Prostaglandin G/H synthase 2	Homo sapiens (human)
positive regulation of platelet-derived growth factor production	Prostaglandin G/H synthase 2	Homo sapiens (human)
cellular oxidant detoxification	Prostaglandin G/H synthase 2	Homo sapiens (human)
regulation of neuroinflammatory response	Prostaglandin G/H synthase 2	Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to osmotic stress	Prostaglandin G/H synthase 2	Homo sapiens (human)
cellular response to homocysteine	Prostaglandin G/H synthase 2	Homo sapiens (human)
response to angiotensin	Prostaglandin G/H synthase 2	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Prostaglandin D2 receptor	Homo sapiens (human)
male sex determination	Prostaglandin D2 receptor	Homo sapiens (human)
sleep	Prostaglandin D2 receptor	Homo sapiens (human)
mast cell degranulation	Prostaglandin D2 receptor	Homo sapiens (human)
adenosine metabolic process	Prostaglandin D2 receptor	Homo sapiens (human)
cellular response to prostaglandin D stimulus	Prostaglandin D2 receptor	Homo sapiens (human)
positive regulation of cytosolic calcium ion concentration	Prostaglandin D2 receptor	Homo sapiens (human)
inflammatory response	Prostaglandin D2 receptor	Homo sapiens (human)
chemotaxis	Prostaglandin D2 receptor 2	Homo sapiens (human)
immune response	Prostaglandin D2 receptor 2	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Prostaglandin D2 receptor 2	Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway	Prostaglandin D2 receptor 2	Homo sapiens (human)
calcium-mediated signaling	Prostaglandin D2 receptor 2	Homo sapiens (human)
positive regulation of G protein-coupled receptor signaling pathway	Prostaglandin D2 receptor 2	Homo sapiens (human)
negative regulation of male germ cell proliferation	Prostaglandin D2 receptor 2	Homo sapiens (human)
neuropeptide signaling pathway	Prostaglandin D2 receptor 2	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
peroxidase activity	Prostaglandin G/H synthase 2	Homo sapiens (human)
prostaglandin-endoperoxide synthase activity	Prostaglandin G/H synthase 2	Homo sapiens (human)
protein binding	Prostaglandin G/H synthase 2	Homo sapiens (human)
enzyme binding	Prostaglandin G/H synthase 2	Homo sapiens (human)
heme binding	Prostaglandin G/H synthase 2	Homo sapiens (human)
protein homodimerization activity	Prostaglandin G/H synthase 2	Homo sapiens (human)
metal ion binding	Prostaglandin G/H synthase 2	Homo sapiens (human)
oxidoreductase activity, acting on single donors with incorporation of molecular oxygen, incorporation of two atoms of oxygen	Prostaglandin G/H synthase 2	Homo sapiens (human)
prostaglandin J receptor activity	Prostaglandin D2 receptor	Homo sapiens (human)
prostaglandin D receptor activity	Prostaglandin D2 receptor	Homo sapiens (human)
protein binding	Prostaglandin D2 receptor	Homo sapiens (human)
prostaglandin J receptor activity	Prostaglandin D2 receptor 2	Homo sapiens (human)
G protein-coupled receptor activity	Prostaglandin D2 receptor 2	Homo sapiens (human)
prostaglandin D receptor activity	Prostaglandin D2 receptor 2	Homo sapiens (human)
prostaglandin F receptor activity	Prostaglandin D2 receptor 2	Homo sapiens (human)
neuropeptide binding	Prostaglandin D2 receptor 2	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
nuclear inner membrane	Prostaglandin G/H synthase 2	Homo sapiens (human)
nuclear outer membrane	Prostaglandin G/H synthase 2	Homo sapiens (human)
cytoplasm	Prostaglandin G/H synthase 2	Homo sapiens (human)
endoplasmic reticulum	Prostaglandin G/H synthase 2	Homo sapiens (human)
endoplasmic reticulum lumen	Prostaglandin G/H synthase 2	Homo sapiens (human)
endoplasmic reticulum membrane	Prostaglandin G/H synthase 2	Homo sapiens (human)
caveola	Prostaglandin G/H synthase 2	Homo sapiens (human)
neuron projection	Prostaglandin G/H synthase 2	Homo sapiens (human)
protein-containing complex	Prostaglandin G/H synthase 2	Homo sapiens (human)
neuron projection	Prostaglandin G/H synthase 2	Homo sapiens (human)
cytoplasm	Prostaglandin G/H synthase 2	Homo sapiens (human)
plasma membrane	Prostaglandin D2 receptor	Homo sapiens (human)
membrane	Prostaglandin D2 receptor	Homo sapiens (human)
plasma membrane	Prostaglandin D2 receptor	Homo sapiens (human)
plasma membrane	Prostaglandin D2 receptor 2	Homo sapiens (human)
plasma membrane	Prostaglandin D2 receptor 2	Homo sapiens (human)
neuron projection	Prostaglandin D2 receptor 2	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (95)

Assay ID	Title	Year	Journal	Article
AID645055	Plasma concentration in guinea pig at 0.1 mg/kg, sc after 4 hrs	2011	ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5	Discovery of AMG 853, a CRTH2 and DP Dual Antagonist.
AID1213916	Drug metabolism in human liver microsomes assessed as 2-(4-(4-(tert-butylcarbamoyl)-2-(2-chloro-4-(1-hydroxycyclopropyl)phenylsulfonamido)phenoxy)-5-chloro-2-fluorophenyl)acetic acid formation at 2 uM after 60 mins by LC-MS/MS analysis in presence of mont	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID645058	Clearance in rat at 0.5 mg/kg, iv	2011	ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5	Discovery of AMG 853, a CRTH2 and DP Dual Antagonist.
AID1213945	Inhibition of CYP2C8 in human liver microsomes assessed as paclitaxel 6-hydroxylation after 5 to 30 mins by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID1213950	Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate after 5 to 30 mins by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID1213962	Time dependent inhibition of CYP2C19 in human liver microsomes using (S)-Mephenytoin as substrate at 10 uM by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID1213898	Drug metabolism assessed as recombinant CYP2J2 (unknown origin)-mediated 2-(5-chloro-4-(2-(2-chloro-4-cyclopropylphenylsulfonamido)-4-(1-hydroxy-2-methylpropan-2-ylcarbamoyl)phenoxy)-2-fluorophenyl)acetic acid formation at 10 uM after 30 mins by LC-MS/MS	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID1213964	Time dependent inhibition of CYP2E1 in human liver microsomes using chlorzoxazone as substrate at 10 uM by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID1213958	Time dependent inhibition of CYP1A2 in human liver microsomes using phenacetin as substrate at 10 uM by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID645052	Plasma concentration in guinea pig at 3 mg/kg, sc after 4 hrs	2011	ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5	Discovery of AMG 853, a CRTH2 and DP Dual Antagonist.
AID645053	Plasma concentration in guinea pig at 1 mg/kg, sc after 4 hrs	2011	ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5	Discovery of AMG 853, a CRTH2 and DP Dual Antagonist.
AID1213977	Drug metabolism assessed as human recombinant UGT2B7-mediated (2S,3S,4S,5R,6S)-6-(2-(4-(4-(tert-butylcarbamoyl)-2-(2-chloro-4-cyclopropylphenylsulfonamido)phenoxy)-5-chloro-2-fluorophenyl)acetoxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxylic acid form	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID1213956	Biphasic inhibition of CYP2C8 in human liver microsomes assessed as montelukast 36-hydroxylation after 20 mins by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID1213917	Drug metabolism in human liver microsomes assessed as 2-(5-chloro-4-(2-(2-chloro-4-cyclopropylphenylsulfonamido)-4-(1-hydroxy-2-methylpropan-2-ylcarbamoyl)phenoxy)-2-fluorophenyl)acetic acid formation at 2 uM after 60 mins by LC-MS/MS analysis in presence	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID1213966	Induction of CYP1A2 in human hepatocytes using phenacetin as substrate at 0.3 to 30 uM treated every 24 hrs for 2 days measured on day 5 by LC-MS/MS analysis relative to control	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID1417241	Binding affinity to human Calpain-1 PEF(S) domain at 0.5 to 500 uM expressed in Escherichia coli BL21-CodonPlus (DE3) RP cells incubated for 5 mins by TNS displacement assay	2018	European journal of medicinal chemistry, Sep-05, Volume: 157	Structure-based design of allosteric calpain-1 inhibitors populating a novel bioactivity space.
AID1213891	Drug metabolism assessed as human recombinant UGT2B15-mediated (2S,3S,4S,5R,6S)-6-(2-(4-(4-(tert-butylcarbamoyl)-2-(2-chloro-4-cyclopropylphenylsulfonamido)phenoxy)-5-chloro-2-fluorophenyl)acetoxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxylic acid for	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID645062	Mean residence time in dog	2011	ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5	Discovery of AMG 853, a CRTH2 and DP Dual Antagonist.
AID1213944	Inhibition of CYP2B6 in human liver microsomes using bupropion as substrate after 5 to 30 mins by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID645057	Inhibition of CYP450	2011	ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5	Discovery of AMG 853, a CRTH2 and DP Dual Antagonist.
AID645051	Plasma concentration in guinea pig at 10 mg/kg, sc after 4 hrs	2011	ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5	Discovery of AMG 853, a CRTH2 and DP Dual Antagonist.
AID1213925	Drug metabolism assessed as human recombinant UGT1A1-mediated (2S,3S,4S,5R,6S)-6-(2-(4-(4-(tert-butylcarbamoyl)-2-(2-chloro-4-cyclopropylphenylsulfonamido)phenoxy)-5-chloro-2-fluorophenyl)acetoxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxylic acid form	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID1213890	Drug metabolism assessed as human recombinant UGT2B4-mediated (2S,3S,4S,5R,6S)-6-(2-(4-(4-(tert-butylcarbamoyl)-2-(2-chloro-4-cyclopropylphenylsulfonamido)phenoxy)-5-chloro-2-fluorophenyl)acetoxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxylic acid form	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID1213915	Drug metabolism in human liver microsomes assessed as 2-(5-chloro-4-(2-(2-chloro-4-cyclopropylphenylsulfonamido)-4-(1-hydroxy-2-methylpropan-2-ylcarbamoyl)phenoxy)-2-fluorophenyl)acetic acid formation at 2 uM after 60 mins by LC-MS/MS analysis in presence	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID645061	Mean residence time in rat	2011	ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5	Discovery of AMG 853, a CRTH2 and DP Dual Antagonist.
AID1213937	Drug metabolism in human liver microsomes assessed as CYP3A51/1-mediated (2S,3S,4S,5R,6S)-6-(2-(4-(4-(tert-butylcarbamoyl)-2-(2-chloro-4-cyclopropylphenylsulfonamido)phenoxy)-5-chloro-2-fluorophenyl)acetoxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxy	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID1213980	Drug metabolism assessed as human recombinant UGT1A6-mediated (2S,3S,4S,5R,6S)-6-(2-(4-(4-(tert-butylcarbamoyl)-2-(2-chloro-4-cyclopropylphenylsulfonamido)phenoxy)-5-chloro-2-fluorophenyl)acetoxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxylic acid form	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID1213972	Upregulation of CYP3A4 mRNA expression in human hepatocytes at 0.3 to 30 uM treated every 24 hrs for 2 days measured on day 5 relative to control	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID1213948	Inhibition of CYP2D6 in human liver microsomes using dextromethorphan as substrate after 5 to 30 mins by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID648028	Displacement of [3H]-PGD2 from human CRTH2 receptor expressed in human HEK293 cells by scintillation counter in presence of 50% human plasma	2011	ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5	Discovery of AMG 853, a CRTH2 and DP Dual Antagonist.
AID645063	Mean residence time in cynomolgus monkey	2011	ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5	Discovery of AMG 853, a CRTH2 and DP Dual Antagonist.
AID1213974	Cmax in healthy human at 50 mg, po in presence of ketoconazole	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID1213957	Induction of CYP3A4 in human hepatocytes using midazolam as substrate at 0.3 to 30 uM treated every 24 hrs for 2 days measured on day 5 by LC-MS/MS analysis relative to control	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID1213970	Upregulation of CYP2B6 mRNA expression in human hepatocytes at 0.3 to 30 uM treated every 24 hrs for 2 days measured on day 5 relative to control	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID1213975	AUC (0 to infinity) in healthy human at 50 mg, po	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID1213965	Time dependent inhibition of CYP3A4 in human liver microsomes using midazolam as substrate at 10 uM by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID645054	Plasma concentration in guinea pig at 0.3 mg/kg, sc after 4 hrs	2011	ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5	Discovery of AMG 853, a CRTH2 and DP Dual Antagonist.
AID648027	Displacement of [3H]-PGD2 from human CRTH2 receptor expressed in human HEK293 cells by scintillation counter in presence of 0.5% bovine serum albumin	2011	ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5	Discovery of AMG 853, a CRTH2 and DP Dual Antagonist.
AID1213960	Time dependent inhibition of CYP2C8 in human liver microsomes using paclitaxel as substrate at 10 uM by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID648033	Antagonist activity at CRTH2 receptor expressed in human HEK293 cells assessed as eosinophil shape change assay by aequorin assay	2011	ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5	Discovery of AMG 853, a CRTH2 and DP Dual Antagonist.
AID1213979	Drug metabolism assessed as human recombinant UGT1A8-mediated (2S,3S,4S,5R,6S)-6-(2-(4-(4-(tert-butylcarbamoyl)-2-(2-chloro-4-cyclopropylphenylsulfonamido)phenoxy)-5-chloro-2-fluorophenyl)acetoxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxylic acid form	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID1213940	Drug metabolism in human liver microsomes assessed as CYP3A53/3-mediated (2S,3S,4S,5R,6S)-6-(2-(4-(4-(tert-butylcarbamoyl)-2-(2-chloro-4-cyclopropylphenylsulfonamido)phenoxy)-5-chloro-2-fluorophenyl)acetoxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxy	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID1213959	Time dependent inhibition of CYP2B6 in human liver microsomes using bupropion as substrate at 10 uM by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID1213971	Upregulation of CYP2C9 mRNA expression in human hepatocytes at 0.3 to 30 uM treated every 24 hrs for 2 days measured on day 5 relative to control	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID1213910	Drug metabolism assessed as recombinant CYP3A4 (unknown origin)-mediated 2-(4-(4-(tert-butylcarbamoyl)-2-(2-chloro-4-(1-hydroxycyclopropyl)phenylsulfonamido)phenoxy)-5-chloro-2-fluorophenyl)acetic acid formation at 10 uM after 30 mins by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID1213951	Inhibition of CYP3A4 in human liver microsomes using testosterone as substrate after 5 to 30 mins by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID1213908	Drug metabolism assessed as recombinant CYP2C8 (unknown origin)-mediated 2-(4-(4-(tert-butylcarbamoyl)-2-(2-chloro-4-(1-hydroxycyclopropyl)phenylsulfonamido)phenoxy)-5-chloro-2-fluorophenyl)acetic acid formation at 10 uM after 30 mins by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID1213926	Drug metabolism assessed as human recombinant UGT1A3-mediated (2S,3S,4S,5R,6S)-6-(2-(4-(4-(tert-butylcarbamoyl)-2-(2-chloro-4-cyclopropylphenylsulfonamido)phenoxy)-5-chloro-2-fluorophenyl)acetoxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxylic acid form	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID1213967	Induction of CYP2B6 in human hepatocytes using bupropion as substrate at 0.3 to 30 uM treated every 24 hrs for 2 days measured on day 5 by LC-MS/MS analysis relative to control	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID1213952	Competitive inhibition of CYP2C8 in human liver microsomes assessed as paclitaxel 6-hydroxylation after 20 mins by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID645060	Clearance in cynomolgus monkey at 0.5 mg/kg, iv	2011	ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5	Discovery of AMG 853, a CRTH2 and DP Dual Antagonist.
AID1213978	Drug metabolism assessed as human recombinant UGT1A4-mediated (2S,3S,4S,5R,6S)-6-(2-(4-(4-(tert-butylcarbamoyl)-2-(2-chloro-4-cyclopropylphenylsulfonamido)phenoxy)-5-chloro-2-fluorophenyl)acetoxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxylic acid form	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID1213889	Drug metabolism assessed as human recombinant UGT1A10-mediated (2S,3S,4S,5R,6S)-6-(2-(4-(4-(tert-butylcarbamoyl)-2-(2-chloro-4-cyclopropylphenylsulfonamido)phenoxy)-5-chloro-2-fluorophenyl)acetoxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxylic acid for	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID1213973	Cmax in healthy human at 50 mg, po	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID1213911	Drug metabolism assessed as recombinant CYP3A5 (unknown origin)-mediated 2-(4-(4-(tert-butylcarbamoyl)-2-(2-chloro-4-(1-hydroxycyclopropyl)phenylsulfonamido)phenoxy)-5-chloro-2-fluorophenyl)acetic acid formation at 10 uM after 30 mins by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID645069	Oral bioavailability in cynomolgus monkey at 2 mg/kg	2011	ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5	Discovery of AMG 853, a CRTH2 and DP Dual Antagonist.
AID1213924	Fraction unbound in plasma (unknown origin)	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID645049	Inhibition of PGD2-induced airway constriction in guinea pig model at 0.1 to 10 mg/kg, sc administered 4 hrs prior to aerosolized PGD2 challenge	2011	ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5	Discovery of AMG 853, a CRTH2 and DP Dual Antagonist.
AID1213949	Inhibition of CYP2E1 in human liver microsomes using chlorzoxazone as substrate after 5 to 30 mins by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID1213976	AUC (0 to infinity) in healthy human at 50 mg, po in presence of ketoconazole	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID1417240	Inhibition of porcine Calpain-1 active site domain using (H2NeK(-FAM)-EVYGMMK(DABCYL)eOH) substrate by FRET assay	2018	European journal of medicinal chemistry, Sep-05, Volume: 157	Structure-based design of allosteric calpain-1 inhibitors populating a novel bioactivity space.
AID1213961	Time dependent inhibition of CYP2C9 in human liver microsomes using diclofenac as substrate at 10 uM by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID1213982	Drug metabolism assessed as human recombinant UGT1A9-mediated (2S,3S,4S,5R,6S)-6-(2-(4-(4-(tert-butylcarbamoyl)-2-(2-chloro-4-cyclopropylphenylsulfonamido)phenoxy)-5-chloro-2-fluorophenyl)acetoxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxylic acid form	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID1213912	Drug metabolism assessed as recombinant CYP3A7 (unknown origin)-mediated 2-(4-(4-(tert-butylcarbamoyl)-2-(2-chloro-4-(1-hydroxycyclopropyl)phenylsulfonamido)phenoxy)-5-chloro-2-fluorophenyl)acetic acid formation at 10 uM after 30 mins by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID1213938	Drug metabolism in human liver microsomes assessed as CYP3A53/3-mediated (2S,3S,4S,5R,6S)-6-(2-(4-(4-(tert-butylcarbamoyl)-2-(2-chloro-4-cyclopropylphenylsulfonamido)phenoxy)-5-chloro-2-fluorophenyl)acetoxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxy	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID1213963	Time dependent inhibition of CYP2D6 in human liver microsomes using dextromethorphan as substrate at 10 uM by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID1213969	Upregulation of CYP1A2 mRNA expression in human hepatocytes at 0.3 to 30 uM treated every 24 hrs for 2 days measured on day 5 relative to control	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID645059	Clearance in dog at 0.5 mg/kg, iv	2011	ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5	Discovery of AMG 853, a CRTH2 and DP Dual Antagonist.
AID648031	Inhibition of PGD2-induced CRTH2 internalization in human CD16 negative granulocytes by flow cytometry	2011	ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5	Discovery of AMG 853, a CRTH2 and DP Dual Antagonist.
AID1213946	Inhibition of CYP2C9 in human liver microsomes using diclofenac as substrate after 5 to 30 mins by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID648030	Displacement of [3H]-PGD2 from human Prostanoid DP receptor expressed in human HEK293 cells by scintillation counter in presence of 50% human plasma	2011	ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5	Discovery of AMG 853, a CRTH2 and DP Dual Antagonist.
AID645056	Antagonist activity at guinea pig Prostanoid DP receptor in whole blood by cAMP assay	2011	ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5	Discovery of AMG 853, a CRTH2 and DP Dual Antagonist.
AID1417239	Inhibition of full length porcine Calpain-1 complex using (H2NeK(-FAM)-EVYGMMK(DABCYL)eOH) substrate by FRET assay	2018	European journal of medicinal chemistry, Sep-05, Volume: 157	Structure-based design of allosteric calpain-1 inhibitors populating a novel bioactivity space.
AID1213939	Drug metabolism in human liver microsomes assessed as CYP3A51/1-mediated (2S,3S,4S,5R,6S)-6-(2-(4-(4-(tert-butylcarbamoyl)-2-(2-chloro-4-cyclopropylphenylsulfonamido)phenoxy)-5-chloro-2-fluorophenyl)acetoxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxy	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID1213899	Drug metabolism assessed as recombinant CYP3A5 (unknown origin)-mediated 2-(5-chloro-4-(2-(2-chloro-4-cyclopropylphenylsulfonamido)-4-(1-hydroxy-2-methylpropan-2-ylcarbamoyl)phenoxy)-2-fluorophenyl)acetic acid formation at 10 uM after 30 mins by LC-MS/MS	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID1213943	Inhibition of CYP1A2 in human liver microsomes using phenacetin as substrate after 5 to 30 mins by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID1213954	Competitive inhibition of CYP2C8 in human liver microsomes assessed as rosiglitazone demethylation after 20 mins by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID1213901	Drug metabolism assessed as recombinant CYP3A4 (unknown origin)-mediated 2-(5-chloro-4-(2-(2-chloro-4-cyclopropylphenylsulfonamido)-4-(1-hydroxy-2-methylpropan-2-ylcarbamoyl)phenoxy)-2-fluorophenyl)acetic acid formation at 10 uM after 30 mins by LC-MS/MS	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID645064	Volume of distribution at steady state in rat	2011	ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5	Discovery of AMG 853, a CRTH2 and DP Dual Antagonist.
AID1213947	Inhibition of CYP2C19 in human liver microsomes using (S)-Mephenytoin as substrate after 5 to 30 mins by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID645067	Oral bioavailability in rat at 2 mg/kg	2011	ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5	Discovery of AMG 853, a CRTH2 and DP Dual Antagonist.
AID1213909	Drug metabolism assessed as recombinant CYP2J2 (unknown origin)-mediated 2-(4-(4-(tert-butylcarbamoyl)-2-(2-chloro-4-(1-hydroxycyclopropyl)phenylsulfonamido)phenoxy)-5-chloro-2-fluorophenyl)acetic acid formation at 10 uM after 30 mins by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID648032	Antagonist activity at human CRTH2 receptor in human whole blood cells assessed as inhibition of PGD2-induced cAMP formation by ELISA	2011	ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5	Discovery of AMG 853, a CRTH2 and DP Dual Antagonist.
AID1213913	Drug metabolism assessed as recombinant CYP2C19 (unknown origin)-mediated 2-(4-(4-(tert-butylcarbamoyl)-2-(2-chloro-4-(1-hydroxycyclopropyl)phenylsulfonamido)phenoxy)-5-chloro-2-fluorophenyl)acetic acid formation at 10 uM after 30 mins by LC-MS/MS analysi	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID645065	Volume of distribution at steady state in dog	2011	ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5	Discovery of AMG 853, a CRTH2 and DP Dual Antagonist.
AID1213981	Drug metabolism assessed as human recombinant UGT1A7-mediated (2S,3S,4S,5R,6S)-6-(2-(4-(4-(tert-butylcarbamoyl)-2-(2-chloro-4-cyclopropylphenylsulfonamido)phenoxy)-5-chloro-2-fluorophenyl)acetoxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxylic acid form	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID1213918	Drug metabolism in human liver microsomes assessed as 2-(4-(4-(tert-butylcarbamoyl)-2-(2-chloro-4-(1-hydroxycyclopropyl)phenylsulfonamido)phenoxy)-5-chloro-2-fluorophenyl)acetic acid formation at 2 uM after 60 mins by LC-MS/MS analysis in presence of keto	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID1213968	Induction of CYP2C9 in human hepatocytes using diclofenac as substrate at 0.3 to 30 uM treated every 24 hrs for 2 days measured on day 5 by LC-MS/MS analysis relative to control	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID645066	Volume of distribution at steady state in cynomolgus monkey	2011	ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5	Discovery of AMG 853, a CRTH2 and DP Dual Antagonist.
AID628374	Inverse agonist activity at human CRTH2 expressed in chinese hamster CHO cells by [35S]GTPgamma binding assay relative to control	2011	Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20	Discovery of potent, selective, and orally bioavailable alkynylphenoxyacetic acid CRTH2 (DP2) receptor antagonists for the treatment of allergic inflammatory diseases.
AID648029	Displacement of [3H]-PGD2 from human Prostanoid DP receptor expressed in human HEK293 cells by scintillation counter in presence of 0.5% bovine serum albumin	2011	ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5	Discovery of AMG 853, a CRTH2 and DP Dual Antagonist.
AID645068	Oral bioavailability in dog at 2 mg/kg	2011	ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5	Discovery of AMG 853, a CRTH2 and DP Dual Antagonist.
AID1213892	Drug metabolism assessed as human recombinant UGT2B17-mediated (2S,3S,4S,5R,6S)-6-(2-(4-(4-(tert-butylcarbamoyl)-2-(2-chloro-4-cyclopropylphenylsulfonamido)phenoxy)-5-chloro-2-fluorophenyl)acetoxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxylic acid for	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID1213900	Drug metabolism assessed as recombinant CYP2C8 (unknown origin)-mediated 2-(5-chloro-4-(2-(2-chloro-4-cyclopropylphenylsulfonamido)-4-(1-hydroxy-2-methylpropan-2-ylcarbamoyl)phenoxy)-2-fluorophenyl)acetic acid formation at 10 uM after 30 mins by LC-MS/MS	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID1213902	Drug metabolism assessed as recombinant CYP3A7 (unknown origin)-mediated 2-(5-chloro-4-(2-(2-chloro-4-cyclopropylphenylsulfonamido)-4-(1-hydroxy-2-methylpropan-2-ylcarbamoyl)phenoxy)-2-fluorophenyl)acetic acid formation at 10 uM after 30 mins by LC-MS/MS	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
[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	0 (0.00)	29.6817
2010's	7 (100.00)	24.3611
2020's	0 (0.00)	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	1 (14.29%)	5.53%
Reviews	0 (0.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	6 (85.71%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
phenylacetic acid phenylacetic acid : A monocarboxylic acid that is toluene in which one of the hydrogens of the methyl group has been replaced by a carboxy group.	2.07	1	benzenes; monocarboxylic acid; phenylacetic acids	allergen; Aspergillus metabolite; auxin; EC 6.4.1.1 (pyruvate carboxylase) inhibitor; Escherichia coli metabolite; human metabolite; plant growth retardant; plant metabolite; Saccharomyces cerevisiae metabolite; toxin
ketoconazole 1-acetyl-4-(4-{[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazine : A dioxolane that is 1,3-dioxolane which is substituted at positions 2, 2, and 4 by imidazol-1-ylmethyl, 2,4-dichlorophenyl, and [para-(4-acetylpiperazin-1-yl)phenoxy]methyl groups, respectively.	2.07	1	dichlorobenzene; dioxolane; ether; imidazoles; N-acylpiperazine; N-arylpiperazine
omeprazole Omeprazole: A 4-methoxy-3,5-dimethylpyridyl, 5-methoxybenzimidazole derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits an H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS.. omeprazole : A racemate comprising equimolar amounts of (R)- and (S)-omeprazole.. 5-methoxy-2-{[(4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulfinyl}-1H-benzimidazole : A member of the class of benzimidazoles that is 1H-benzimidazole which is substituted by a [4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulfinyl group at position 2 and a methoxy group at position 5.	2.07	1	aromatic ether; benzimidazoles; pyridines; sulfoxide
phenobarbital Phenobarbital: A barbituric acid derivative that acts as a nonselective central nervous system depressant. It potentiates GAMMA-AMINOBUTYRIC ACID action on GABA-A RECEPTORS, and modulates chloride currents through receptor channels. It also inhibits glutamate induced depolarizations.. phenobarbital : A member of the class of barbiturates, the structure of which is that of barbituric acid substituted at C-5 by ethyl and phenyl groups.	2.07	1	barbiturates	anticonvulsant; drug allergen; excitatory amino acid antagonist; sedative
prostaglandin d2 Prostaglandin D2: The principal cyclooxygenase metabolite of arachidonic acid. It is released upon activation of mast cells and is also synthesized by alveolar macrophages. Among its many biological actions, the most important are its bronchoconstrictor, platelet-activating-factor-inhibitory, and cytotoxic effects.. prostaglandin D2 : A member of the class of prostaglandins D that is prosta-5,13-dien-1-oic acid substituted by hydroxy groups at positions 9 and 15 and an oxo group at position 11 (the 5Z,9alpha,13E,15S- stereoisomer).	2.07	1	prostaglandins D	human metabolite; mouse metabolite
pd 150606 PD 150606: a calpain inhibitor; structure given in first source. (Z)-3-(4-iodophenyl)-2-mercaptoacrylic acid : An organoiodine compound that is acrylic acid in which the vinylic hydrogens at positions 2 and 3 are replaced by mercapto and 4-iodophenyl groups respectively (the Z geoisomer).	2.17	1	cinnamic acids; organoiodine compound; thioenol	apoptosis inhibitor; calpain inhibitor
amg 009 AMG 009: an anti-inflammatory agent; structure in first source	2.47	2
mk-7246 [no description available]	2.06	1
rifampin Rifampin: A semisynthetic antibiotic produced from Streptomyces mediterranei. It has a broad antibacterial spectrum, including activity against several forms of Mycobacterium. In susceptible organisms it inhibits DNA-dependent RNA polymerase activity by forming a stable complex with the enzyme. It thus suppresses the initiation of RNA synthesis. Rifampin is bactericidal, and acts on both intracellular and extracellular organisms. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1160)	2.07	1	cyclic ketal; hydrazone; N-iminopiperazine; N-methylpiperazine; rifamycins; semisynthetic derivative; zwitterion	angiogenesis inhibitor; antiamoebic agent; antineoplastic agent; antitubercular agent; DNA synthesis inhibitor; EC 2.7.7.6 (RNA polymerase) inhibitor; Escherichia coli metabolite; geroprotector; leprostatic drug; neuroprotective agent; pregnane X receptor agonist; protein synthesis inhibitor

Condition	Indicated	Relationship Strength	Studies	Trials
Contact Dermatitis [description not available]	0	2.06	1	0
Eosinophilia, Pulmonary [description not available]	0	2.06	1	0
Dermatitis, Contact A type of acute or chronic skin reaction in which sensitivity is manifested by reactivity to materials or substances coming in contact with the skin. It may involve allergic or non-allergic mechanisms.	0	2.06	1	0
Pulmonary Eosinophilia A condition characterized by infiltration of the lung with EOSINOPHILS due to inflammation or other disease processes. Major eosinophilic lung diseases are the eosinophilic pneumonias caused by infections, allergens, or toxic agents.	0	2.06	1	0
Asthma, Bronchial [description not available]	0	4.79	2	1
Allergic Reaction [description not available]	0	2.07	1	0
Asthma A form of bronchial disorder with three distinct components: airway hyper-responsiveness (RESPIRATORY HYPERSENSITIVITY), airway INFLAMMATION, and intermittent AIRWAY OBSTRUCTION. It is characterized by spasmodic contraction of airway smooth muscle, WHEEZING, and dyspnea (DYSPNEA, PAROXYSMAL).	1	11.79	2	1
Hypersensitivity Altered reactivity to an antigen, which can result in pathologic reactions upon subsequent exposure to that particular antigen.	0	2.07	1	0

amg 853

Description

Cross-References

Synonyms (38)

Research Excerpts

Overview

Toxicity

Bioavailability

Dosage Studied

Protein Targets (4)

Inhibition Measurements

Other Measurements

Biological Processes (74)

Molecular Functions (13)

Ceullar Components (11)

Bioassays (95)

Research

Studies (7)

Market Indicators

Research Demand Index: 15.77

Study Types

amg 853

Description

Cross-References

Synonyms (38)

Research Excerpts

Overview

Toxicity

Bioavailability

Dosage Studied

Protein Targets (4)

Inhibition Measurements

Other Measurements

Biological Processes (74)

Molecular Functions (13)

Ceullar Components (11)

Bioassays (95)

Research

Studies (7)

Market Indicators

Research Demand Index: 15.77

Study Types

Related Drugs (9)

Related Conditions (8)