cj-023,423 profile

grapiprant: a potent and selective prostaglandin EP4 receptor antagonist with antihyperalgesic properties; cyclooxygenase inhibitors [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID Source	ID
PubMed CID	11677589
CHEMBL ID	3039498
SCHEMBL ID	120428
MeSH ID	M0513562

Synonyms (61)

Synonym
415903-37-6
cj-023
cj-023423
cj-023,423
j9f5zph7nb ,
mr-10a7
mr10a7
rq-00000007
unii-j9f5zph7nb
grapiprant [usan:inn]
1-(2-(4-(2-ethyl-4,6-dimethylimidazo(4,5-c)pyridin-1-yl)phenyl)ethyl)-3-(4-methylphenyl)sulfonylurea
benzenesulfonamide, n-(((2-(4-(2-ethyl-4,6-dimethyl-1h-imidazo(4,5-c)pyridin-1-yl)phenyl)ethyl)amino)carbonyl)-4-methyl-
rq-7
aat-007
grapiprant
cj 023423
S6694
CHEMBL3039498
1-[2-[4-(2-ethyl-4,6-dimethylimidazo[4,5-c]pyridin-1-yl)phenyl]ethyl]-3-(4-methylphenyl)sulfonylurea
gtpl5858
grapiprant [who-dd]
grapiprant [inn]
grapiprant [usan]
2-ethyl-4,6-dimethyl-1-(4-(2-(((((4-methylphenyl)sulfonyl)amino)carbonyl)amino)ethyl)phenyl)-1h-imidazo(4,5-c)pyridine
grapiprant [green book]
grapiprant [mi]
n-(((2-(4-(2-ethyl-4,6-dimethyl-1h-imidazo(4,5-c)pyridin-1-yl)phenyl)ethyl)amino)carbonyl)-4-methyl-benzenesulfonamide
n-(((2-(4-(2-ethyl-4,6-dimethyl-1h-imidazo(4,5-c)pyridin-1-yl)phenyl)ethyl)amino)carbonyl)-4-methylbenzenesulfonamide
HZVLFTCYCLXTGV-UHFFFAOYSA-N
n-[([2-[4-(2-ethyl-4,6-dimethyl-1h-imidazo[4,5-c]pyridin-1-yl)phenyl]ethyl]amino)carbonyl]-4-methylbenzenesulfonamide
SCHEMBL120428
D10638
grapiprant (usan/inn)
bdbm50107283
HY-16781
CS-5392
DTXSID60194419
AKOS030526811
n-((4-(2-ethyl-4,6-dimethyl-1h-imidazo[4,5-c]pyridin-1-yl)phenethyl)carbamoyl)-4-methylbenzenesulfonamide
cj-023423; rq-00000007; aat-007
DB12836
BCP20570
grapiprant; rq-00000007; aat-007; cj-023423
EX-A2544
Q27077852
SB18902
cj-023423;rq-00000007;aat-007
D83673
A900379
B0084-470919
grapiprant (cj-023423)
aat-007cj-023423
AS-77380
n-(((2-(4-(2-ethyl-4,6-dimethyl-1h-imidazo(4,5-c)pyridin-1-yl) phenyl)ethyl)amino)carbonyl)-4-methylbenzenesulfonamide
rq-07
galliprant
n-((2,4-(2-ethyl-4,6-dimethyl-1h-imidazo(4,5-c)pyridin-1-yl)phenylethylamino)carbonyl)-4-methyl-benzenesulfonamide
grapiprantum
cj023,423
AC-36123
n-(4-(2-ethyl-4,6-dimethyl-1h-imidazo[4,5-c]pyridin-1-yl)phenethylcarbamoyl)-4-methylbenzenesulfonamide

Research Excerpts

Toxicity

Excerpt	Reference	Relevance
" Grapiprant was well tolerated, and no adverse effects were detected at doses ≤ 15 mg/kg."	( Safety and toxicokinetic profiles associated with daily oral administration of grapiprant, a selective antagonist of the prostaglandin E2 EP4 receptor, to cats. Rausch-Derra, LC; Rhodes, L, 2016)	0.43

Pharmacokinetics

Excerpt	Reference	Relevance
" In the pyridine series, compound 7a was found to be a highly potent and selective EP4 antagonist, with suitable rat and dog pharmacokinetic profiles."	( Discovery of potent aryl-substituted 3-[(3-methylpyridine-2-carbonyl) amino]-2,4-dimethyl-benzoic acid EP4 antagonists with improved pharmacokinetic profile. Blanco, MJ; Chambers, M; Chandrasekhar, S; Fisher, MJ; Harvey, A; Lin, C; Mudra, D; Oskins, J; Vetman, T; Wang, XS; Warshawsky, AM; Yu, XP, 2016)	0.43
" 614 ng/mL) and delayed median time of peak concentration (1."	( Pharmacokinetics and estimated bioavailability of grapiprant, a novel selective prostaglandin E Barsotti, G; Gazzano, A; Giorgi, M; Lisowski, A; Owen, H; Łebkowska-Wieruszewska, B, 2017)	0.46
"A preliminary study, in which grapiprant (4 mg/kg [n = 2], 11 mg/kg [2], or 45 mg/kg [2]) was delivered into the crop of RTHAs from which food had been withheld for 24 hours, was performed to obtained pharmacokinetic data for use with modeling software to simulate results for grapiprant doses of 20, 25, 30, 35, and 40 mg/kg."	( Pharmacokinetics of grapiprant administered to red-tailed hawks ( Drazenovich, TL; Hawkins, MG; Knych, HK; Paul-Murphy, JR; Rodriguez, P, 2021)	0.62
"0 hours, and the harmonic mean terminal half-life was 17."	( Pharmacokinetics of grapiprant administered to red-tailed hawks ( Drazenovich, TL; Hawkins, MG; Knych, HK; Paul-Murphy, JR; Rodriguez, P, 2021)	0.62
" Further research that incorporates multidose assessments, safety monitoring, and pharmacodynamic data collection is warranted on the use of grapiprant in RTHAs from which food was withheld versus not withheld."	( Pharmacokinetics of grapiprant administered to red-tailed hawks ( Drazenovich, TL; Hawkins, MG; Knych, HK; Paul-Murphy, JR; Rodriguez, P, 2021)	0.62

Bioavailability

Excerpt	Reference	Relevance
" From this class, a potent and highly bioavailable compound (6) has been selected for potential clinical studies."	( Discovery and characterization of a potent and selective EP4 receptor antagonist. Chandrasekhar, S; Fisher, MJ; Harvey, A; Kuklish, SL; Schiffler, MA; Wang, XS; Warshawsky, AM; York, JS; Yu, XP, 2015)	0.42
"To assess the effect of food intake on the pharmacokinetics of grapiprant administered orally at 2 mg/kg, and to estimate its oral bioavailability in dogs."	( Pharmacokinetics and estimated bioavailability of grapiprant, a novel selective prostaglandin E Barsotti, G; Gazzano, A; Giorgi, M; Lisowski, A; Owen, H; Łebkowska-Wieruszewska, B, 2017)	0.46
" The estimated bioavailability in fasted and fed dogs was 111."	( Pharmacokinetics and estimated bioavailability of grapiprant, a novel selective prostaglandin E Barsotti, G; Gazzano, A; Giorgi, M; Lisowski, A; Owen, H; Łebkowska-Wieruszewska, B, 2017)	0.46

Dosage Studied

Excerpt	Relevance	Reference
" Structural modifications on lead compound 4a were explored with the aim of improving potency, physicochemical properties, and animal PK predictive of QD (once a day) dosing regimen in human."	( Discovery of AAT-008, a novel, potent, and selective prostaglandin EP4 receptor antagonist. Nakao, K; Nukui, S; Okumura, Y; Yamagishi, T, 2017)	0.46
" Simulations support a dosing frequency of 12-hour intervals with food reaching minimum effective concentrations established for canines, although it is unknown whether these plasma concentrations are therapeutic for birds."	( Absorption of grapiprant in red-tailed hawks (Buteo jamaicensis) is decreased when administered with food. Drazenovich, TL; Hawkins, MG; Knych, HK; Paul-Murphy, JR; Rodriguez, P, 2022)	0.72
" Pain and inflammation were assessed by masked investigators via mechanical nociceptive threshold testing and the short form of the Glasgow Composite Pain Scale before drug administration and at multiple time points for 72 hours following dosing and surgery."	( Preliminary evaluation of the effects of grapiprant compared with carprofen on acute pain and inflammation following ovariohysterectomy in dogs. Barnes, DN; Enomoto, H; Long, SM; Messenger, KM; Southern, BL, 2022)	0.72

[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Thromboxane A2 receptor	Homo sapiens (human)	Ki	5.0000	0.0006	1.2407	3.8040	AID1430132
Prostaglandin E2 receptor EP1 subtype	Homo sapiens (human)	Ki	5.0000	0.0091	0.6635	1.5849	AID1430141
Prostaglandin E2 receptor EP4 subtype	Homo sapiens (human)	IC50 (µMol)	0.1810	0.0004	0.9585	8.0390	AID1238243; AID1238244; AID1266062; AID1294271
Prostaglandin E2 receptor EP4 subtype	Homo sapiens (human)	Ki	0.3033	0.0001	0.4744	3.1623	AID1238243; AID1266061; AID1430136
Prostaglandin F2-alpha receptor	Homo sapiens (human)	Ki	5.0000	0.0310	3.3803	9.9910	AID1430146
Prostaglandin E2 receptor EP4 subtype	Rattus norvegicus (Norway rat)	Ki	0.0200	0.0200	0.0200	0.0200	AID1430130
Prostaglandin E2 receptor EP3 subtype	Homo sapiens (human)	Ki	5.0000	0.0003	1.7081	6.8000	AID1430143
Prostaglandin E2 receptor EP2 subtype	Homo sapiens (human)	Ki	5.0000	0.0010	0.5448	3.0000	AID1430142
Prostacyclin receptor	Homo sapiens (human)	Ki	5.0000	0.0032	0.4958	6.6280	AID1430131
Prostaglandin E2 receptor EP4 subtype	Canis lupus familiaris (dog)	Ki	0.0240	0.0240	0.0240	0.0240	AID1430128
[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 E2 receptor EP4 subtype	Mus musculus (house mouse)	Kd	0.0078	0.0078	0.0078	0.0078	AID1430127
Prostaglandin E2 receptor EP4 subtype	Homo sapiens (human)	Kd	0.0048	0.0018	0.0033	0.0048	AID1430133
Prostaglandin E2 receptor EP4 subtype	Rattus norvegicus (Norway rat)	Kd	0.0065	0.0065	0.0065	0.0065	AID1430129
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
smooth muscle contraction	Thromboxane A2 receptor	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Thromboxane A2 receptor	Homo sapiens (human)
response to nutrient	Thromboxane A2 receptor	Homo sapiens (human)
response to xenobiotic stimulus	Thromboxane A2 receptor	Homo sapiens (human)
positive regulation of blood coagulation	Thromboxane A2 receptor	Homo sapiens (human)
response to testosterone	Thromboxane A2 receptor	Homo sapiens (human)
thromboxane A2 signaling pathway	Thromboxane A2 receptor	Homo sapiens (human)
response to ethanol	Thromboxane A2 receptor	Homo sapiens (human)
positive regulation of angiogenesis	Thromboxane A2 receptor	Homo sapiens (human)
positive regulation of smooth muscle contraction	Thromboxane A2 receptor	Homo sapiens (human)
cellular response to lipopolysaccharide	Thromboxane A2 receptor	Homo sapiens (human)
negative regulation of cell migration involved in sprouting angiogenesis	Thromboxane A2 receptor	Homo sapiens (human)
inflammatory response	Thromboxane A2 receptor	Homo sapiens (human)
positive regulation of blood pressure	Thromboxane A2 receptor	Homo sapiens (human)
positive regulation of vasoconstriction	Thromboxane A2 receptor	Homo sapiens (human)
positive regulation of cytosolic calcium ion concentration	Thromboxane A2 receptor	Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathway	Thromboxane A2 receptor	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Prostaglandin E2 receptor EP1 subtype	Homo sapiens (human)
adenylate cyclase-activating dopamine receptor signaling pathway	Prostaglandin E2 receptor EP1 subtype	Homo sapiens (human)
response to lipopolysaccharide	Prostaglandin E2 receptor EP1 subtype	Homo sapiens (human)
positive regulation of cytosolic calcium ion concentration	Prostaglandin E2 receptor EP1 subtype	Homo sapiens (human)
inflammatory response	Prostaglandin E2 receptor EP1 subtype	Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathway	Prostaglandin E2 receptor EP1 subtype	Homo sapiens (human)
negative regulation of cytokine production	Prostaglandin E2 receptor EP4 subtype	Homo sapiens (human)
positive regulation of cytokine production	Prostaglandin E2 receptor EP4 subtype	Homo sapiens (human)
immune response	Prostaglandin E2 receptor EP4 subtype	Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathway	Prostaglandin E2 receptor EP4 subtype	Homo sapiens (human)
JNK cascade	Prostaglandin E2 receptor EP4 subtype	Homo sapiens (human)
response to mechanical stimulus	Prostaglandin E2 receptor EP4 subtype	Homo sapiens (human)
response to nematode	Prostaglandin E2 receptor EP4 subtype	Homo sapiens (human)
regulation of ossification	Prostaglandin E2 receptor EP4 subtype	Homo sapiens (human)
response to lipopolysaccharide	Prostaglandin E2 receptor EP4 subtype	Homo sapiens (human)
negative regulation of integrin activation	Prostaglandin E2 receptor EP4 subtype	Homo sapiens (human)
T-helper cell differentiation	Prostaglandin E2 receptor EP4 subtype	Homo sapiens (human)
negative regulation of inflammatory response	Prostaglandin E2 receptor EP4 subtype	Homo sapiens (human)
positive regulation of inflammatory response	Prostaglandin E2 receptor EP4 subtype	Homo sapiens (human)
regulation of stress fiber assembly	Prostaglandin E2 receptor EP4 subtype	Homo sapiens (human)
bone development	Prostaglandin E2 receptor EP4 subtype	Homo sapiens (human)
ERK1 and ERK2 cascade	Prostaglandin E2 receptor EP4 subtype	Homo sapiens (human)
cellular response to mechanical stimulus	Prostaglandin E2 receptor EP4 subtype	Homo sapiens (human)
negative regulation of eosinophil extravasation	Prostaglandin E2 receptor EP4 subtype	Homo sapiens (human)
cellular response to prostaglandin E stimulus	Prostaglandin E2 receptor EP4 subtype	Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathway	Prostaglandin E2 receptor EP4 subtype	Homo sapiens (human)
positive regulation of cytosolic calcium ion concentration	Prostaglandin E2 receptor EP4 subtype	Homo sapiens (human)
inflammatory response	Prostaglandin E2 receptor EP4 subtype	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Prostaglandin F2-alpha receptor	Homo sapiens (human)
parturition	Prostaglandin F2-alpha receptor	Homo sapiens (human)
positive regulation of cell population proliferation	Prostaglandin F2-alpha receptor	Homo sapiens (human)
positive regulation of gene expression	Prostaglandin F2-alpha receptor	Homo sapiens (human)
response to estradiol	Prostaglandin F2-alpha receptor	Homo sapiens (human)
response to lipopolysaccharide	Prostaglandin F2-alpha receptor	Homo sapiens (human)
negative regulation of apoptotic process	Prostaglandin F2-alpha receptor	Homo sapiens (human)
cellular response to prostaglandin D stimulus	Prostaglandin F2-alpha receptor	Homo sapiens (human)
inflammatory response	Prostaglandin F2-alpha receptor	Homo sapiens (human)
positive regulation of cytosolic calcium ion concentration	Prostaglandin F2-alpha receptor	Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathway	Prostaglandin F2-alpha receptor	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Prostaglandin E2 receptor EP3 subtype	Homo sapiens (human)
cell death	Prostaglandin E2 receptor EP3 subtype	Homo sapiens (human)
positive regulation of fever generation	Prostaglandin E2 receptor EP3 subtype	Homo sapiens (human)
intestine smooth muscle contraction	Prostaglandin E2 receptor EP3 subtype	Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway	Prostaglandin E2 receptor EP3 subtype	Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathway	Prostaglandin E2 receptor EP3 subtype	Homo sapiens (human)
inflammatory response	Prostaglandin E2 receptor EP3 subtype	Homo sapiens (human)
positive regulation of cytosolic calcium ion concentration	Prostaglandin E2 receptor EP3 subtype	Homo sapiens (human)
negative regulation of gastric acid secretion	Prostaglandin E2 receptor EP3 subtype	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Prostaglandin E2 receptor EP2 subtype	Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathway	Prostaglandin E2 receptor EP2 subtype	Homo sapiens (human)
response to nematode	Prostaglandin E2 receptor EP2 subtype	Homo sapiens (human)
response to lipopolysaccharide	Prostaglandin E2 receptor EP2 subtype	Homo sapiens (human)
response to progesterone	Prostaglandin E2 receptor EP2 subtype	Homo sapiens (human)
regulation of cell population proliferation	Prostaglandin E2 receptor EP2 subtype	Homo sapiens (human)
cellular response to prostaglandin E stimulus	Prostaglandin E2 receptor EP2 subtype	Homo sapiens (human)
positive regulation of cytosolic calcium ion concentration	Prostaglandin E2 receptor EP2 subtype	Homo sapiens (human)
inflammatory response	Prostaglandin E2 receptor EP2 subtype	Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	Prostacyclin receptor	Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathway	Prostacyclin receptor	Homo sapiens (human)
cell-cell signaling	Prostacyclin receptor	Homo sapiens (human)
negative regulation of platelet-derived growth factor receptor signaling pathway	Prostacyclin receptor	Homo sapiens (human)
response to lipopolysaccharide	Prostacyclin receptor	Homo sapiens (human)
negative regulation of smooth muscle cell proliferation	Prostacyclin receptor	Homo sapiens (human)
positive regulation of cytosolic calcium ion concentration	Prostacyclin receptor	Homo sapiens (human)
inflammatory response	Prostacyclin receptor	Homo sapiens (human)
negative regulation of cytokine production	Prostaglandin E2 receptor EP4 subtype	Canis lupus familiaris (dog)
positive regulation of cytokine production	Prostaglandin E2 receptor EP4 subtype	Canis lupus familiaris (dog)
adenylate cyclase-modulating G protein-coupled receptor signaling pathway	Prostaglandin E2 receptor EP4 subtype	Canis lupus familiaris (dog)
response to nematode	Prostaglandin E2 receptor EP4 subtype	Canis lupus familiaris (dog)
regulation of ossification	Prostaglandin E2 receptor EP4 subtype	Canis lupus familiaris (dog)
response to lipopolysaccharide	Prostaglandin E2 receptor EP4 subtype	Canis lupus familiaris (dog)
negative regulation of integrin activation	Prostaglandin E2 receptor EP4 subtype	Canis lupus familiaris (dog)
T-helper cell differentiation	Prostaglandin E2 receptor EP4 subtype	Canis lupus familiaris (dog)
negative regulation of inflammatory response	Prostaglandin E2 receptor EP4 subtype	Canis lupus familiaris (dog)
positive regulation of inflammatory response	Prostaglandin E2 receptor EP4 subtype	Canis lupus familiaris (dog)
regulation of stress fiber assembly	Prostaglandin E2 receptor EP4 subtype	Canis lupus familiaris (dog)
cellular response to mechanical stimulus	Prostaglandin E2 receptor EP4 subtype	Canis lupus familiaris (dog)
negative regulation of eosinophil extravasation	Prostaglandin E2 receptor EP4 subtype	Canis lupus familiaris (dog)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
thromboxane A2 receptor activity	Thromboxane A2 receptor	Homo sapiens (human)
guanyl-nucleotide exchange factor activity	Thromboxane A2 receptor	Homo sapiens (human)
protein binding	Thromboxane A2 receptor	Homo sapiens (human)
D1 dopamine receptor binding	Prostaglandin E2 receptor EP1 subtype	Homo sapiens (human)
prostaglandin E receptor activity	Prostaglandin E2 receptor EP1 subtype	Homo sapiens (human)
prostaglandin E receptor activity	Prostaglandin E2 receptor EP4 subtype	Homo sapiens (human)
protein binding	Prostaglandin E2 receptor EP4 subtype	Homo sapiens (human)
prostaglandin F receptor activity	Prostaglandin F2-alpha receptor	Homo sapiens (human)
prostaglandin E receptor activity	Prostaglandin E2 receptor EP3 subtype	Homo sapiens (human)
prostaglandin E receptor activity	Prostaglandin E2 receptor EP2 subtype	Homo sapiens (human)
guanyl-nucleotide exchange factor activity	Prostacyclin receptor	Homo sapiens (human)
prostacyclin receptor activity	Prostacyclin receptor	Homo sapiens (human)
prostaglandin E receptor activity	Prostaglandin E2 receptor EP4 subtype	Canis lupus familiaris (dog)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
acrosomal vesicle	Thromboxane A2 receptor	Homo sapiens (human)
plasma membrane	Thromboxane A2 receptor	Homo sapiens (human)
nuclear speck	Thromboxane A2 receptor	Homo sapiens (human)
plasma membrane	Thromboxane A2 receptor	Homo sapiens (human)
plasma membrane	Prostaglandin E2 receptor EP1 subtype	Homo sapiens (human)
plasma membrane	Prostaglandin E2 receptor EP1 subtype	Homo sapiens (human)
plasma membrane	Prostaglandin E2 receptor EP4 subtype	Homo sapiens (human)
membrane	Prostaglandin E2 receptor EP4 subtype	Homo sapiens (human)
plasma membrane	Prostaglandin E2 receptor EP4 subtype	Homo sapiens (human)
extracellular region	Prostaglandin F2-alpha receptor	Homo sapiens (human)
cytoplasm	Prostaglandin F2-alpha receptor	Homo sapiens (human)
plasma membrane	Prostaglandin F2-alpha receptor	Homo sapiens (human)
plasma membrane	Prostaglandin F2-alpha receptor	Homo sapiens (human)
nuclear envelope	Prostaglandin E2 receptor EP3 subtype	Homo sapiens (human)
plasma membrane	Prostaglandin E2 receptor EP3 subtype	Homo sapiens (human)
membrane	Prostaglandin E2 receptor EP3 subtype	Homo sapiens (human)
plasma membrane	Prostaglandin E2 receptor EP3 subtype	Homo sapiens (human)
plasma membrane	Prostaglandin E2 receptor EP2 subtype	Homo sapiens (human)
plasma membrane	Prostaglandin E2 receptor EP2 subtype	Homo sapiens (human)
cytosol	Prostacyclin receptor	Homo sapiens (human)
plasma membrane	Prostacyclin receptor	Homo sapiens (human)
plasma membrane	Prostacyclin receptor	Homo sapiens (human)
plasma membrane	Prostaglandin E2 receptor EP4 subtype	Canis lupus familiaris (dog)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (29)

Assay ID	Title	Year	Journal	Article
AID1430136	Displacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranes	2017	Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5	Discovery of AAT-008, a novel, potent, and selective prostaglandin EP4 receptor antagonist.
AID1238243	Displacement of [3H]-PGE2 from recombinant human EP4 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis	2015	Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16	Discovery and characterization of a potent and selective EP4 receptor antagonist.
AID1266061	Antagonist activity at human EP4 receptor	2016	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 26, Issue:1	Discovery of substituted-2,4-dimethyl-(naphthalene-4-carbonyl)amino-benzoic acid as potent and selective EP4 antagonists.
AID1266066	Drug metabolism in human hepatic microsomes	2016	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 26, Issue:1	Discovery of substituted-2,4-dimethyl-(naphthalene-4-carbonyl)amino-benzoic acid as potent and selective EP4 antagonists.
AID1430127	Antagonist activity at mouse recombinant EP4 receptor assessed as inhibition of PGE2-induced cAMP level by cell based assay	2017	Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5	Discovery of AAT-008, a novel, potent, and selective prostaglandin EP4 receptor antagonist.
AID1266067	Aqueous solubility of the compound at pH 6	2016	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 26, Issue:1	Discovery of substituted-2,4-dimethyl-(naphthalene-4-carbonyl)amino-benzoic acid as potent and selective EP4 antagonists.
AID1430130	Antagonist activity at rat recombinant EP4 receptor	2017	Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5	Discovery of AAT-008, a novel, potent, and selective prostaglandin EP4 receptor antagonist.
AID1430132	Antagonist activity at human platelet TP receptor	2017	Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5	Discovery of AAT-008, a novel, potent, and selective prostaglandin EP4 receptor antagonist.
AID1272653	Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassay	2016	Bioorganic & medicinal chemistry letters, Feb-01, Volume: 26, Issue:3	Discovery of potent aryl-substituted 3-[(3-methylpyridine-2-carbonyl) amino]-2,4-dimethyl-benzoic acid EP4 antagonists with improved pharmacokinetic profile.
AID1266063	Antagonist activity at EP4 receptor in human whole blood assessed as reversal of inhibition of PGE2 mediated LPS-induced TNF alpha production pretreated for 30 mins using 3,3',5,5' tetramethylbiphenyl-4,4'-diamine substrate measured after 20 to 24 hrs by	2016	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 26, Issue:1	Discovery of substituted-2,4-dimethyl-(naphthalene-4-carbonyl)amino-benzoic acid as potent and selective EP4 antagonists.
AID1238245	Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha reduction preincubated for 30 mins followed by PGE2 addition measured after 24 hrs by ELISA	2015	Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16	Discovery and characterization of a potent and selective EP4 receptor antagonist.
AID1430143	Antagonist activity at human EP3 receptor	2017	Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5	Discovery of AAT-008, a novel, potent, and selective prostaglandin EP4 receptor antagonist.
AID1430144	Analgesic activity in po dosed rat assessed as inhibition of carrageenan-induced mechanical hyperalgesia measured at 1 hr post dose	2017	Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5	Discovery of AAT-008, a novel, potent, and selective prostaglandin EP4 receptor antagonist.
AID1430182	Analgesic activity in po dosed rat model of chronic inflammatory pain assessed as inhibition of CFA-induced weight bearing deficit	2017	Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5	Discovery of AAT-008, a novel, potent, and selective prostaglandin EP4 receptor antagonist.
AID1294238	Aqueous solubility of compound at pH 6 at 2 mM after 20 hrs by HPLC	2016	Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9	Identification and biological activity of 6-alkyl-substituted 3-methyl-pyridine-2-carbonyl amino dimethyl-benzoic acid EP4 antagonists.
AID1430131	Antagonist activity at human IP receptor	2017	Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5	Discovery of AAT-008, a novel, potent, and selective prostaglandin EP4 receptor antagonist.
AID1430142	Antagonist activity at human EP2 receptor	2017	Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5	Discovery of AAT-008, a novel, potent, and selective prostaglandin EP4 receptor antagonist.
AID1430128	Antagonist activity at dog recombinant EP4 receptor	2017	Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5	Discovery of AAT-008, a novel, potent, and selective prostaglandin EP4 receptor antagonist.
AID1430146	Antagonist activity at human FP receptor	2017	Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5	Discovery of AAT-008, a novel, potent, and selective prostaglandin EP4 receptor antagonist.
AID1238244	Antagonist activity at recombinant human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP accumulation by scintillation proximity assay in presence of [125I]-cAMP	2015	Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16	Discovery and characterization of a potent and selective EP4 receptor antagonist.
AID1266062	Antagonist activity at human EP4 receptor in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation	2016	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 26, Issue:1	Discovery of substituted-2,4-dimethyl-(naphthalene-4-carbonyl)amino-benzoic acid as potent and selective EP4 antagonists.
AID1430133	Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay	2017	Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5	Discovery of AAT-008, a novel, potent, and selective prostaglandin EP4 receptor antagonist.
AID1430145	Antagonist activity at human DP receptor	2017	Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5	Discovery of AAT-008, a novel, potent, and selective prostaglandin EP4 receptor antagonist.
AID1430141	Antagonist activity at human EP1 receptor	2017	Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5	Discovery of AAT-008, a novel, potent, and selective prostaglandin EP4 receptor antagonist.
AID1294270	Antagonist activity against EP4 in human whole blood assessed as reversal of PGE2-mediated suppression of LPS-induced TNF-alpha production preincubated for 30 mins followed by LPS stimulation measured after 20 to 24 hrs by enzyme immunoassay	2016	Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9	Identification and biological activity of 6-alkyl-substituted 3-methyl-pyridine-2-carbonyl amino dimethyl-benzoic acid EP4 antagonists.
AID1430129	Antagonist activity at rat recombinant EP4 receptor assessed as inhibition of PGE2-induced cAMP level by cell based assay	2017	Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5	Discovery of AAT-008, a novel, potent, and selective prostaglandin EP4 receptor antagonist.
AID1266065	Drug metabolism in rat hepatic microsomes	2016	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 26, Issue:1	Discovery of substituted-2,4-dimethyl-(naphthalene-4-carbonyl)amino-benzoic acid as potent and selective EP4 antagonists.
AID1294271	Antagonist activity against human EP4 expressed in HEK293 cells assessed as inhibition of PGE2-stimulated production of cAMP incubated for 20 mins by HTRF assay	2016	Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9	Identification and biological activity of 6-alkyl-substituted 3-methyl-pyridine-2-carbonyl amino dimethyl-benzoic acid EP4 antagonists.
AID1346427	Human EP4 receptor (Prostanoid receptors)	2007	The Journal of pharmacology and experimental therapeutics, Aug, Volume: 322, Issue:2	CJ-023,423, a novel, potent and selective prostaglandin EP4 receptor antagonist with antihyperalgesic properties.
[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	3 (9.68)	29.6817
2010's	19 (61.29)	24.3611
2020's	9 (29.03)	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	9 (29.03%)	5.53%
Reviews	1 (3.23%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	21 (67.74%)	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
uric acid Uric Acid: An oxidation product, via XANTHINE OXIDASE, of oxypurines such as XANTHINE and HYPOXANTHINE. It is the final oxidation product of purine catabolism in humans and primates, whereas in most other mammals URATE OXIDASE further oxidizes it to ALLANTOIN.. uric acid : An oxopurine that is the final oxidation product of purine metabolism.. 6-hydroxy-1H-purine-2,8(7H,9H)-dione : A tautomer of uric acid having oxo groups at C-2 and C-8 and a hydroxy group at C-6.. 7,9-dihydro-1H-purine-2,6,8(3H)-trione : An oxopurine in which the purine ring is substituted by oxo groups at positions 2, 6, and 8.	4.56	2	2	uric acid	Escherichia coli metabolite; human metabolite; mouse metabolite
carprofen carprofen: RN given refers to cpd without isomeric designation. carprofen : Propanoic acid in which one of the methylene hydrogens is substituted by a 6-chloro-9H-carbazol-2-yl group. A non-steroidal anti-inflammatory drug, it is no longer used in human medicine but is still used for treatment of arthritis in elderly dogs.	5.55	4	3	carbazoles; organochlorine compound	EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; non-steroidal anti-inflammatory drug; photosensitizing agent
diclofenac Diclofenac: A non-steroidal anti-inflammatory agent (NSAID) with antipyretic and analgesic actions. It is primarily available as the sodium salt.. diclofenac : A monocarboxylic acid consisting of phenylacetic acid having a (2,6-dichlorophenyl)amino group at the 2-position.	2.53	2	0	amino acid; aromatic amine; dichlorobenzene; monocarboxylic acid; secondary amino compound	antipyretic; drug allergen; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; environmental contaminant; non-narcotic analgesic; non-steroidal anti-inflammatory drug; xenobiotic
rofecoxib [no description available]	2.04	1	0	butenolide; sulfone	analgesic; cyclooxygenase 2 inhibitor; non-steroidal anti-inflammatory drug
4-butyrolactone 4-Butyrolactone: One of the FURANS with a carbonyl thereby forming a cyclic lactone. It is an endogenous compound made from gamma-aminobutyrate and is the precursor of gamma-hydroxybutyrate. It is also used as a pharmacological agent and solvent.. tetrahydrofuranone : Any oxolane having an oxo- substituent at any position on the tetrahydrofuran ring.. gamma-butyrolactone : A butan-4-olide that is tetrahydrofuran substituted by an oxo group at position 2.	3.59	1	1	butan-4-olide	metabolite; neurotoxin
ivabradine Ivabradine: A benzazepine derivative and selective HYPERPOLARIZATION-ACTIVATED CYCLIC NUCLEOTIDE-GATED CHANNELS inhibitor that lowers the heart rate. It is used in the treatment of CHRONIC STABLE ANGINA in patients unable to take BETA-ADRENERGIC BLOCKERS, and in the treatment of HEART FAILURE.. ivabradine : A member of the class of benzazepines that is 7,8-dimethoxy-1,3,4,5-tetrahydro-3-benzazepin-2-one in which the amide hydrogen is replaced by a [{[(7S)-3,4-dimethoxybicyclo[4.2.0]octa-1,3,5-trien-7-yl]methyl}(methyl)amino]propyl} group. Used (as its hydrochloride salt) to treat patients with angina who have intolerance to beta blockers and/or heart failure.	2.21	1	0	aromatic ether; benzazepine; carbobicyclic compound; tertiary amino compound	cardiotonic drug
firocoxib firocoxib: a COX-2 inhibitor; structure in first source. firocoxib : An enol ether that is the cyclopropylmethyl ether of 3-hydroxy-5,5-dimethyl-4-[4-(methylsulfonyl)phenyl]furan-2-one. A selective cyclooxygenase 2 inhibitor, it is used in veterinary medicine for the control of pain and inflammation associated with osteoarthritis in horses and dogs.	3.59	1	1	butenolide; cyclopropanes; enol ether; sulfone	antineoplastic agent; cyclooxygenase 2 inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug
dinoprostone prostaglandin E2 : Prostaglandin F2alpha in which the hydroxy group at position 9 has been oxidised to the corresponding ketone. Prostaglandin E2 is the most common and most biologically potent of mammalian prostaglandins.	5.99	7	1	prostaglandins E	human metabolite; mouse metabolite; oxytocic
cj-042794 [no description available]	2.15	1	0	aromatic ether

Condition	Indicated	Relationship Strength	Studies	Trials
Allodynia [description not available]	0	2.47	2	0
Ache [description not available]	0	6.05	9	1
Pain An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS.	0	6.05	9	1
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	0	2.84	3	0
Acute Post-operative Pain [description not available]	0	5.05	3	2
Cat Diseases Diseases of the domestic cat (Felis catus or F. domesticus). This term does not include diseases of the so-called big cats such as CHEETAHS; LIONS; tigers, cougars, panthers, leopards, and other Felidae for which the heading CARNIVORA is used.	0	2.41	1	0
Pain, Postoperative Pain during the period after surgery.	0	5.05	3	2
Canine Diseases [description not available]	0	7.6	8	6
Innate Inflammatory Response [description not available]	0	4.42	4	1
Inflammation A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.	0	9.42	4	1
Acute Pain Intensely discomforting, distressful, or agonizing sensation associated with trauma or disease, with well-defined location, character, and timing.	0	3.8	1	1
Arthritis, Degenerative [description not available]	0	6.42	7	2
Swine Diseases Diseases of domestic swine and of the wild boar of the genus Sus.	0	2.6	1	0
Osteoarthritis A progressive, degenerative joint disease, the most common form of arthritis, especially in older persons. The disease is thought to result not from the aging process but from biochemical changes and biomechanical stresses affecting articular cartilage. In the foreign literature it is often called osteoarthrosis deformans.	1	8.42	7	2
Adjuvant Arthritis [description not available]	0	3.88	2	1
Gait Disorders, Animal [description not available]	0	4.56	2	2
Plica Syndrome [description not available]	0	3.59	1	1
Synovitis Inflammation of the SYNOVIAL MEMBRANE.	0	3.59	1	1
Autoimmune Diabetes [description not available]	0	2.17	1	0
Diabetes Mellitus, Type 1 A subtype of DIABETES MELLITUS that is characterized by INSULIN deficiency. It is manifested by the sudden onset of severe HYPERGLYCEMIA, rapid progression to DIABETIC KETOACIDOSIS, and DEATH unless treated with insulin. The disease may occur at any age, but is most common in childhood or adolescence.	0	2.17	1	0
Nerve Pain [description not available]	0	2.21	1	0
Neuralgia Intense or aching pain that occurs along the course or distribution of a peripheral or cranial nerve.	0	2.21	1	0
Emesis [description not available]	0	3.51	1	1
Vomiting The forcible expulsion of the contents of the STOMACH through the MOUTH.	0	3.51	1	1
Bone Loss, Osteoclastic [description not available]	0	2.04	1	0
Anasarca [description not available]	0	2.04	1	0
Edema Abnormal fluid accumulation in TISSUES or body cavities. Most cases of edema are present under the SKIN in SUBCUTANEOUS TISSUE.	0	2.04	1	0

cj-023,423

Description

Cross-References

Synonyms (61)

Research Excerpts

Toxicity

Pharmacokinetics

Bioavailability

Dosage Studied

Protein Targets (10)

Inhibition Measurements

Activation Measurements

Biological Processes (54)

Molecular Functions (7)

Ceullar Components (8)

Bioassays (29)

Research

Studies (31)

Market Indicators

Research Demand Index: 16.95

Study Types

cj-023,423

Description

Cross-References

Synonyms (61)

Research Excerpts

Toxicity

Pharmacokinetics

Bioavailability

Dosage Studied

Protein Targets (10)

Inhibition Measurements

Activation Measurements

Biological Processes (54)

Molecular Functions (7)

Ceullar Components (8)

Bioassays (29)

Research

Studies (31)

Market Indicators

Research Demand Index: 16.95

Study Types

Related Drugs (9)

Related Conditions (27)