Page last updated: 2024-11-07

ramatroban

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

Cross-References

ID SourceID
PubMed CID123879
CHEMBL ID361812
CHEBI ID32087
SCHEMBL ID29030
MeSH IDM0174394

Synonyms (81)

Synonym
AC-719
[3h]ramatroban
gtpl1911
gtpl1910
[3h]bay u 3405
[3h]bay u3405
[3h]baynas
baynas
bay-u-3405
ramatroban ,
116649-85-5
baynas (tn)
ramatroban (jan/inn)
D01128
9h-carbazole-9-propanoic acid, 3-(((4-fluorophenyl)sulfonyl)amino)-1,2,3,4-tetrahydro-, (r)-
bay u-3405
bay u 3405
3-(4-fluorophenylsulfonamido)-1,2,3,4-tetrahydro-9-carbazole propanoic acid
bay u3405
(+)-(3r)-3-(p-fluorobenzenesulfonamido)-1,2,3,4-tetrahydrocarbazole-9-propionic acid
bay u 3406
NCGC00167519-01
bdbm50161746
3-[(r)-3-(4-fluoro-benzenesulfonylamino)-1,2,3,4-tetrahydro-carbazol-9-yl]-propionic acid
(r)-3-(3-(4-fluorophenylsulfonamido)-1,2,3,4-tetrahydrocarbazol-9-yl)propanoic acid
3-[(3r)-3-[(4-fluorophenyl)sulfonylamino]-1,2,3,4-tetrahydrocarbazol-9-yl]propanoic acid
CHEMBL361812 ,
en 137774
en-137774
A803658
[(4-fluorophenyl)sulfonylamino] 3-(1,2,3,4-tetrahydrocarbazol-9-yl)propanoate
(r)-3-(3-(4-fluorophenylsulfonamido)-3,4-dihydro-1h-carbazol-9(2h)-yl)propanoic acid
tox21_112516
dtxcid9026685
dtxsid1046685 ,
cas-116649-85-5
AKOS015966619
ramatroban [inn:ban]
unii-p1ali72u6c
p1ali72u6c ,
(3r)-3-[[(4-fluorophenyl)sulfonyl]amino]-1,2,3,4-tetrahydro-9h-carbazole-9-propanoic acid
bay-u 3405
NCGC00167519-04
ramatroban [inn]
ramatroban [mart.]
ramatroban [mi]
(3r)-3-(((4-fluorophenyl)sulfonyl)amino)-1,2,3,4-tetrahydro-9h-carbazole-9-propanoic acid
9h-carbazole-9-propanoic acid, 3-(((4-fluorophenyl)sulfonyl)amino)-1,2,3,4-tetrahydro-, (3r)-
ramatroban [who-dd]
ramatroban [jan]
S5286
HY-B0745
MLS006010637
smr002530322
SCHEMBL29030
tox21_112516_1
NCGC00167519-02
KS-1310
3r-[[(4-fluorophenyl)sulfonyl]amino]-1,2,3,4-tetrahydro-9h-carbazole-9-propanoic acid
HMS3648E21
mfcd00887606
J-003466
sr-01000883932
SR-01000883932-1
CHEBI:32087
ramatroban, >=98% (hplc), solid
ramatroban (bay u3405)
3(r)-[[(4-fluoro-phenyl) sulfonyl]amino]-1,2,3,4-tetrahydro-9h-carbazole-9-propanoic acid
NCGC00167519-07
LDXDSHIEDAPSSA-OAHLLOKOSA-N
(r)-3-[3-(4-fluorophenylsulphonylamino)-1,2,3,4-tetrahydrocarbazol- 9-yl]propionic acid
DB13036
a8x ,
SR-01000946208-1
sr-01000946208
Q10357327
CCG-268842
9h-carbazole-9-propanoic acid, 3-[[(4-fluorophenyl)sulfonyl]amino]-1,2,3,4-tetrahydro-, (3r)-
EX-A4208
(r)-3-(3-(4-fluorophenylsulfonamido)-3,4-dihydro-1h-carbazol-9(2h)-yl)propanoicacid
R0144

Research Excerpts

Treatment

The treatment with ramatroban is safe and improves nasal symptoms. The treatment reversed the attenuation of the vascular response to acetylcholine in hypercholesterolemic groups.

ExcerptReferenceRelevance
"The treatment by ramatroban reversed the attenuation of the vascular response to acetylcholine in hypercholesterolemic groups."( Ramatroban, a TP receptor antagonist, improves vascular responses to acetylcholine in hypercholesterolemic rabbits in vivo.
Ishizuka, T; Kurita, A; Matsui, T, 2003
)
2.09
"The treatment with ramatroban is safe and improves nasal symptoms."( [Ramatroban (Baynas): a review of its pharmacological and clinical profile].
Imagawa, W; Motobayashi, Y; Saida, K, 2001
)
1.54

Pharmacokinetics

ExcerptReferenceRelevance
"kg-1, whereas in Cmax an over-proportional increase was observed."( Pharmacokinetics and metabolism of the new thromboxane A2 receptor antagonist ramatroban in animals. 1st communication: absorption, concentrations in plasma, metabolism, and excretion after single administration to rats and dogs.
Ahr, HJ; Beckermann, B; Boberg, M; Bühner, K; Hirayama, M; Siefert, HM; Steinke, W; Wünsche, C, 1997
)
0.53

Bioavailability

The oral bioavailability of ramatroban was complete in the dog but amounted to about 50% in the rat due to presystemic elimination.

ExcerptReferenceRelevance
" The oral bioavailability of ramatroban was complete in the dog but amounted to about 50% in the rat due to presystemic elimination."( Pharmacokinetics and metabolism of the new thromboxane A2 receptor antagonist ramatroban in animals. 1st communication: absorption, concentrations in plasma, metabolism, and excretion after single administration to rats and dogs.
Ahr, HJ; Beckermann, B; Boberg, M; Bühner, K; Hirayama, M; Siefert, HM; Steinke, W; Wünsche, C, 1997
)
0.82
" This is also the first report detailing an orally bioavailable small molecule CRTH2 antagonist."( An orally bioavailable small molecule antagonist of CRTH2, ramatroban (BAY u3405), inhibits prostaglandin D2-induced eosinophil migration in vitro.
Bacon, KB; Gantner, F; Iino, T; Manabe, Y; Shichijo, M; Shimazaki, M; Sugimoto, H; Watanabe, A, 2003
)
0.56
"The bioavailability (BA) of ramatroban was estimated at 21."( Pharmacokinetic analysis of ramatroban using a recirculatory model with enterohepatic circulation by measuring portal and systemic blood concentration difference in Sprague-Dawley and Eisai hyperbilirubinemic rats.
Moriwaki, T; Yamamoto, A; Yasui, H, 2004
)
0.91
" Moreover, compounds ( R)- 58 and ( R)- 71 were shown to possess pharmacokinetic properties suitable for development as an orally bioavailable drug."( Discovery of a new class of potent, selective, and orally bioavailable CRTH2 (DP2) receptor antagonists for the treatment of allergic inflammatory diseases.
Arrighi, JF; Atherall, J; Bernardinelli, G; Chollet, A; Cleva, C; Colovray, V; Crosignani, S; Filinchuk, Y; Gaudet, M; Giachetti, C; Golzio, L; Humbert, Y; Macritchie, J; Maio, M; Martin, T; Missotten, M; Page, P; Pittet, PA; Pupowicz, D; Rocha, C; Scheer, A; Schwarz, MK, 2008
)
0.35
"High throughput screening identified a 7-azaindole-3-acetic acid scaffold as a novel CRTh2 receptor antagonist chemotype, which could be optimised to furnish a highly selective compound with good functional potency for inhibition of human eosinophil shape change in whole blood and oral bioavailability in the rat."( 7-Azaindole-3-acetic acid derivatives: potent and selective CRTh2 receptor antagonists.
Adcock, C; Bala, K; Barker, L; Brown, Z; Budd, D; Cox, B; Dubois, G; Fairhurst, RA; Furegati, M; Leblanc, C; Manini, J; Profit, R; Reilly, J; Sandham, DA; Schmidt, A; Stringer, R; Turner, KL; Watson, SJ; Williams, G; Willis, J; Wilson, C, 2009
)
0.35
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

ExcerptRelevanceReference
" Increasing dosages of PGD2 were inhaled to establish dose-response curves that allowed determination of the provocative concentration necessary to decrease FEV1 by at least 20% (PC20) and to increase specific airway resistance (SR(aw)) by 100% (PC100)."( Effects of a thromboxane-receptor antagonist, BAY u 3405, on prostaglandin D2- and exercise-induced bronchoconstriction.
Baunack, AR; Boerger, S; Magnussen, H; Templin, K, 1992
)
0.28
" At four subsequent randomized visits, subjects received this concentration of PGD2 90 min after dosing with placebo or 20, 50 or 100 mg of BAY u 3405, a potent competitive TP receptor antagonist."( Prostaglandin D2-induced bronchoconstriction is mediated only in part by the thromboxane prostanoid receptor.
Freezer, NJ; Howarth, PH; Johnston, SL; O'Toole, S; Ritter, W, 1995
)
0.29
" BAY u 3405 is a potent selective competitive TP receptor antagonist, which inhibits the lower airway response to PG D2, and shifts the dose-response curve to the right by up to 16-fold."( The effect of BAY u 3405, a thromboxane receptor antagonist, on prostaglandin D2-induced nasal blockage.
Harrison, J; Howarth, PH; Johnston, SL; Ritter, W; Smith, S, 1993
)
0.29
" The local absorption ratio for the dosage after oral administration (Fa(dosage)) and the single-pass local absorption ratio for EHC (Fa') in the rats were similar and nearly 100%."( Pharmacokinetic analysis of ramatroban using a recirculatory model with enterohepatic circulation by measuring portal and systemic blood concentration difference in Sprague-Dawley and Eisai hyperbilirubinemic rats.
Moriwaki, T; Yamamoto, A; Yasui, H, 2004
)
0.62
" There was no difference in the severity of symptoms between the reduced dosage (n=14) and the maintained dosage (n=15) groups."( [Study of thromboxane A2 antagonist reduction in the treatment of patients with perennial allergic rhinitis].
Himi, T; Itoh, J; Kobayashi, K; Narita, S; Shirasaki, H, 2004
)
0.32
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

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

Protein Targets (26)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
SMAD family member 2Homo sapiens (human)Potency26.83250.173734.304761.8120AID1346859
SMAD family member 3Homo sapiens (human)Potency26.83250.173734.304761.8120AID1346859
progesterone receptorHomo sapiens (human)Potency13.33320.000417.946075.1148AID1346795
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency15.48710.01237.983543.2770AID1645841
estrogen nuclear receptor alphaHomo sapiens (human)Potency10.67170.000229.305416,493.5996AID743075
GVesicular stomatitis virusPotency17.37680.01238.964839.8107AID1645842
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency29.84700.023723.228263.5986AID743222
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency0.79430.035520.977089.1251AID504332
menin isoform 1Homo sapiens (human)Potency0.01030.010314.297036.5881AID651843
histone-lysine N-methyltransferase 2A isoform 2 precursorHomo sapiens (human)Potency0.01030.010323.856763.0957AID651843
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency33.48890.000627.21521,122.0200AID743202
muscleblind-like protein 1 isoform 1Homo sapiens (human)Potency0.01400.00419.962528.1838AID493199; AID493205
Interferon betaHomo sapiens (human)Potency17.37680.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency17.37680.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency17.37680.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency17.37680.01238.964839.8107AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Bile salt export pumpHomo sapiens (human)IC50 (µMol)62.40000.11007.190310.0000AID1449628
Cytochrome P450 3A4Homo sapiens (human)IC50 (µMol)30.00000.00011.753610.0000AID429620
Cytochrome P450 2D6Homo sapiens (human)IC50 (µMol)30.00000.00002.015110.0000AID429622
Cytochrome P450 2C9 Homo sapiens (human)IC50 (µMol)15.00000.00002.800510.0000AID429621
Thromboxane A2 receptor Homo sapiens (human)IC50 (µMol)0.01070.00110.71065.2000AID248580; AID248754; AID429618
Thromboxane A2 receptor Homo sapiens (human)Ki0.00770.00061.24073.8040AID238927; AID244585; AID551275
Prostacyclin receptorHomo sapiens (human)IC50 (µMol)100.00000.00840.07040.2880AID429619
Prostaglandin D2 receptorHomo sapiens (human)IC50 (µMol)21.70000.00011.15837.3000AID248439; AID429617
Prostaglandin D2 receptorHomo sapiens (human)Ki10.51000.00060.49131.4000AID238910; AID551274
Acyl-CoA:cholesterol acyltransferase Oryctolagus cuniculus (rabbit)IC50 (µMol)7.65550.00600.98467.6000AID429614; AID429621
Neuronal acetylcholine receptor subunit alpha-6Mus musculus (house mouse)IC50 (µMol)0.31100.00400.08170.3110AID429614
Prostaglandin D2 receptor 2Homo sapiens (human)IC50 (µMol)0.22890.00040.10090.9600AID248926; AID248959; AID330825; AID429614; AID429615; AID431338; AID431354; AID586985; AID586990
Prostaglandin D2 receptor 2Homo sapiens (human)Ki0.18900.00060.67358.0000AID239567; AID244593; AID244599; AID244604; AID431337; AID551273
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (129)

Processvia Protein(s)Taxonomy
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lipid hydroxylationCytochrome P450 3A4Homo sapiens (human)
lipid metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid catabolic processCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid metabolic processCytochrome P450 3A4Homo sapiens (human)
cholesterol metabolic processCytochrome P450 3A4Homo sapiens (human)
androgen metabolic processCytochrome P450 3A4Homo sapiens (human)
estrogen metabolic processCytochrome P450 3A4Homo sapiens (human)
alkaloid catabolic processCytochrome P450 3A4Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 3A4Homo sapiens (human)
calcitriol biosynthetic process from calciolCytochrome P450 3A4Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D metabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D catabolic processCytochrome P450 3A4Homo sapiens (human)
retinol metabolic processCytochrome P450 3A4Homo sapiens (human)
retinoic acid metabolic processCytochrome P450 3A4Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 3A4Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 3A4Homo sapiens (human)
oxidative demethylationCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2D6Homo sapiens (human)
steroid metabolic processCytochrome P450 2D6Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2D6Homo sapiens (human)
estrogen metabolic processCytochrome P450 2D6Homo sapiens (human)
coumarin metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid catabolic processCytochrome P450 2D6Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2D6Homo sapiens (human)
isoquinoline alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2D6Homo sapiens (human)
retinol metabolic processCytochrome P450 2D6Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2D6Homo sapiens (human)
negative regulation of bindingCytochrome P450 2D6Homo sapiens (human)
oxidative demethylationCytochrome P450 2D6Homo sapiens (human)
negative regulation of cellular organofluorine metabolic processCytochrome P450 2D6Homo sapiens (human)
arachidonic acid metabolic processCytochrome P450 2D6Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C9 Homo sapiens (human)
steroid metabolic processCytochrome P450 2C9 Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2C9 Homo sapiens (human)
estrogen metabolic processCytochrome P450 2C9 Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C9 Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
urea metabolic processCytochrome P450 2C9 Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 2C9 Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C9 Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
amide metabolic processCytochrome P450 2C9 Homo sapiens (human)
icosanoid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
oxidative demethylationCytochrome P450 2C9 Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
smooth muscle contractionThromboxane A2 receptor Homo sapiens (human)
G protein-coupled receptor signaling pathwayThromboxane A2 receptor Homo sapiens (human)
response to nutrientThromboxane A2 receptor Homo sapiens (human)
response to xenobiotic stimulusThromboxane A2 receptor Homo sapiens (human)
positive regulation of blood coagulationThromboxane A2 receptor Homo sapiens (human)
response to testosteroneThromboxane A2 receptor Homo sapiens (human)
thromboxane A2 signaling pathwayThromboxane A2 receptor Homo sapiens (human)
response to ethanolThromboxane A2 receptor Homo sapiens (human)
positive regulation of angiogenesisThromboxane A2 receptor Homo sapiens (human)
positive regulation of smooth muscle contractionThromboxane A2 receptor Homo sapiens (human)
cellular response to lipopolysaccharideThromboxane A2 receptor Homo sapiens (human)
negative regulation of cell migration involved in sprouting angiogenesisThromboxane A2 receptor Homo sapiens (human)
inflammatory responseThromboxane A2 receptor Homo sapiens (human)
positive regulation of blood pressureThromboxane A2 receptor Homo sapiens (human)
positive regulation of vasoconstrictionThromboxane A2 receptor Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationThromboxane A2 receptor Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayThromboxane A2 receptor Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerProstacyclin receptorHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayProstacyclin receptorHomo sapiens (human)
cell-cell signalingProstacyclin receptorHomo sapiens (human)
negative regulation of platelet-derived growth factor receptor signaling pathwayProstacyclin receptorHomo sapiens (human)
response to lipopolysaccharideProstacyclin receptorHomo sapiens (human)
negative regulation of smooth muscle cell proliferationProstacyclin receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationProstacyclin receptorHomo sapiens (human)
inflammatory responseProstacyclin receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayProstaglandin D2 receptorHomo sapiens (human)
male sex determinationProstaglandin D2 receptorHomo sapiens (human)
sleepProstaglandin D2 receptorHomo sapiens (human)
mast cell degranulationProstaglandin D2 receptorHomo sapiens (human)
adenosine metabolic processProstaglandin D2 receptorHomo sapiens (human)
cellular response to prostaglandin D stimulusProstaglandin D2 receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationProstaglandin D2 receptorHomo sapiens (human)
inflammatory responseProstaglandin D2 receptorHomo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
chemotaxisProstaglandin D2 receptor 2Homo sapiens (human)
immune responseProstaglandin D2 receptor 2Homo sapiens (human)
G protein-coupled receptor signaling pathwayProstaglandin D2 receptor 2Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayProstaglandin D2 receptor 2Homo sapiens (human)
calcium-mediated signalingProstaglandin D2 receptor 2Homo sapiens (human)
positive regulation of G protein-coupled receptor signaling pathwayProstaglandin D2 receptor 2Homo sapiens (human)
negative regulation of male germ cell proliferationProstaglandin D2 receptor 2Homo sapiens (human)
neuropeptide signaling pathwayProstaglandin D2 receptor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (61)

Processvia Protein(s)Taxonomy
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
steroid bindingCytochrome P450 3A4Homo sapiens (human)
iron ion bindingCytochrome P450 3A4Homo sapiens (human)
protein bindingCytochrome P450 3A4Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
retinoic acid 4-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
oxidoreductase activityCytochrome P450 3A4Homo sapiens (human)
oxygen bindingCytochrome P450 3A4Homo sapiens (human)
enzyme bindingCytochrome P450 3A4Homo sapiens (human)
heme bindingCytochrome P450 3A4Homo sapiens (human)
vitamin D3 25-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
caffeine oxidase activityCytochrome P450 3A4Homo sapiens (human)
quinine 3-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
testosterone 6-beta-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
aromatase activityCytochrome P450 3A4Homo sapiens (human)
vitamin D 24-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
monooxygenase activityCytochrome P450 2D6Homo sapiens (human)
iron ion bindingCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activityCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2D6Homo sapiens (human)
heme bindingCytochrome P450 2D6Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
iron ion bindingCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
caffeine oxidase activityCytochrome P450 2C9 Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
aromatase activityCytochrome P450 2C9 Homo sapiens (human)
heme bindingCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C9 Homo sapiens (human)
thromboxane A2 receptor activityThromboxane A2 receptor Homo sapiens (human)
guanyl-nucleotide exchange factor activityThromboxane A2 receptor Homo sapiens (human)
protein bindingThromboxane A2 receptor Homo sapiens (human)
guanyl-nucleotide exchange factor activityProstacyclin receptorHomo sapiens (human)
prostacyclin receptor activityProstacyclin receptorHomo sapiens (human)
prostaglandin J receptor activityProstaglandin D2 receptorHomo sapiens (human)
prostaglandin D receptor activityProstaglandin D2 receptorHomo sapiens (human)
protein bindingProstaglandin D2 receptorHomo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
prostaglandin J receptor activityProstaglandin D2 receptor 2Homo sapiens (human)
G protein-coupled receptor activityProstaglandin D2 receptor 2Homo sapiens (human)
prostaglandin D receptor activityProstaglandin D2 receptor 2Homo sapiens (human)
prostaglandin F receptor activityProstaglandin D2 receptor 2Homo sapiens (human)
neuropeptide bindingProstaglandin D2 receptor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (34)

Processvia Protein(s)Taxonomy
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cytoplasmCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 3A4Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 3A4Homo sapiens (human)
mitochondrionCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulumCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2D6Homo sapiens (human)
cytoplasmCytochrome P450 2D6Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C9 Homo sapiens (human)
plasma membraneCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
cytoplasmCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
acrosomal vesicleThromboxane A2 receptor Homo sapiens (human)
plasma membraneThromboxane A2 receptor Homo sapiens (human)
nuclear speckThromboxane A2 receptor Homo sapiens (human)
plasma membraneThromboxane A2 receptor Homo sapiens (human)
cytosolProstacyclin receptorHomo sapiens (human)
plasma membraneProstacyclin receptorHomo sapiens (human)
plasma membraneProstacyclin receptorHomo sapiens (human)
plasma membraneProstaglandin D2 receptorHomo sapiens (human)
membraneProstaglandin D2 receptorHomo sapiens (human)
plasma membraneProstaglandin D2 receptorHomo sapiens (human)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
plasma membraneProstaglandin D2 receptor 2Homo sapiens (human)
plasma membraneProstaglandin D2 receptor 2Homo sapiens (human)
neuron projectionProstaglandin D2 receptor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (91)

Assay IDTitleYearJournalArticle
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID76697Compound was tested for inhibition of U-46,619 induced increase in tracheal pressure of guinea pigs1998Bioorganic & medicinal chemistry letters, Jun-02, Volume: 8, Issue:11
Synthesis and biological evaluation of new tetrahydronaphthalene derivatives as thromboxane receptor antagonists.
AID248926Inhibition of PGD2-induced inositol phosphate formation at human chemoattractant receptor-homologous molecule expressed on TH2 cells2005Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
Minor structural modifications convert the dual TP/CRTH2 antagonist ramatroban into a highly selective and potent CRTH2 antagonist.
AID165613Anti-platelet activity was measured by studying their antagonist effects on rabbit platelets aggregated with U-46,619.; NT means not tested.2002Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18
Synthesis and antiaggregant properties of Stabilized analogues of polyunsaturated fatty acid metabolites.
AID431338Antagonist activity against CRTh2 receptor in human eosinophils assessed as cell shape change2009Bioorganic & medicinal chemistry letters, Aug-15, Volume: 19, Issue:16
7-Azaindole-3-acetic acid derivatives: potent and selective CRTh2 receptor antagonists.
AID238927Inhibition of [3H]SQ-29,548 binding to human Thromboxane A2 receptor2005Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
Minor structural modifications convert the dual TP/CRTH2 antagonist ramatroban into a highly selective and potent CRTH2 antagonist.
AID429619Displacement of [3H]iloprost from human prostacyclin receptor expressed in human 293 cell membrane2009Bioorganic & medicinal chemistry letters, Aug-15, Volume: 19, Issue:16
Novel tricyclic antagonists of the prostaglandin D2 receptor DP2 with efficacy in a murine model of allergic rhinitis.
AID586989Agonist activity at CRTh2 receptor in human whole blood assessed as eosinophil shape change by fluorescence assay relative to 13,14-dihydro-15-keto-PGD22011Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
Zwitterionic CRTh2 antagonists.
AID429616Inhibition of eosinophil degranulation in human whole blood assessed as change in morphology after 4 mins using flow cytometry by leukocyte shape change assay2009Bioorganic & medicinal chemistry letters, Aug-15, Volume: 19, Issue:16
Novel tricyclic antagonists of the prostaglandin D2 receptor DP2 with efficacy in a murine model of allergic rhinitis.
AID431356Antagonist activity against CRTh2 receptor in human whole blood assessed as eosinophil shape change2009Bioorganic & medicinal chemistry letters, Aug-15, Volume: 19, Issue:16
7-Azaindole-3-acetic acid derivatives: potent and selective CRTh2 receptor antagonists.
AID330825Antagonist activity at human CRTH2 receptor assessed as inhibition of DK-PGD2-induced eosinophil chemotaxis2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Discovery of a new class of potent, selective, and orally bioavailable CRTH2 (DP2) receptor antagonists for the treatment of allergic inflammatory diseases.
AID442515Inhibition of human H-PGDS expressed in Escherichia coli BL21 assessed as rate of glutathione-chloro-dinitro benzene conjugation at 50 uM2010European journal of medicinal chemistry, Feb, Volume: 45, Issue:2
Identification and characterisation of new inhibitors for the human hematopoietic prostaglandin D2 synthase.
AID431357Protein binding in human plasma by HSA column HPLC method2009Bioorganic & medicinal chemistry letters, Aug-15, Volume: 19, Issue:16
7-Azaindole-3-acetic acid derivatives: potent and selective CRTh2 receptor antagonists.
AID429622Inhibition of human CYP2D62009Bioorganic & medicinal chemistry letters, Aug-15, Volume: 19, Issue:16
Novel tricyclic antagonists of the prostaglandin D2 receptor DP2 with efficacy in a murine model of allergic rhinitis.
AID239567Inhibition of [3H]PGD-2 binding to human chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTH2)2005Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
Minor structural modifications convert the dual TP/CRTH2 antagonist ramatroban into a highly selective and potent CRTH2 antagonist.
AID429620Inhibition of human CYP3A42009Bioorganic & medicinal chemistry letters, Aug-15, Volume: 19, Issue:16
Novel tricyclic antagonists of the prostaglandin D2 receptor DP2 with efficacy in a murine model of allergic rhinitis.
AID442514Inhibition of human H-PGDS expressed in Escherichia coli BL21 assessed as rate of glutathione-chloro-dinitro benzene conjugation2010European journal of medicinal chemistry, Feb, Volume: 45, Issue:2
Identification and characterisation of new inhibitors for the human hematopoietic prostaglandin D2 synthase.
AID244604Inhibitory concentration for PGD2-mediated receptor activation in a fluorescence assay that measures changes in intracellular calcium2005Bioorganic & medicinal chemistry letters, Mar-15, Volume: 15, Issue:6
Isosteric ramatroban analogs: selective and potent CRTH-2 antagonists.
AID586986Lipophilicity, log D of the compound at pH 7.42011Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
Zwitterionic CRTh2 antagonists.
AID599064Plasma protein binding in human2011Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
Lipophilicity of acidic compounds: impact of ion pair partitioning on drug design.
AID251891Percentage inhibition for binding of PGD-2 in hTP binding assay using HEK293 cell membranes2005Bioorganic & medicinal chemistry letters, Mar-15, Volume: 15, Issue:6
Isosteric ramatroban analogs: selective and potent CRTH-2 antagonists.
AID166818Compound was tested for inhibition of U-46,619 induced contraction of isolated rabbit saphenous vein1998Bioorganic & medicinal chemistry letters, Jun-02, Volume: 8, Issue:11
Synthesis and biological evaluation of new tetrahydronaphthalene derivatives as thromboxane receptor antagonists.
AID429621Inhibition of human CYP2C92009Bioorganic & medicinal chemistry letters, Aug-15, Volume: 19, Issue:16
Novel tricyclic antagonists of the prostaglandin D2 receptor DP2 with efficacy in a murine model of allergic rhinitis.
AID5985271-Octanol-sodium citrate buffer distribution coefficient, log D of the compound at pH 5.5 by shake-flask method2011Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
Lipophilicity of acidic compounds: impact of ion pair partitioning on drug design.
AID586990Antagonist activity against human CRTh2 receptor expressed in CHO cells assessed as inhibition of PGD2-mediated Ca2+ flux2011Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
Zwitterionic CRTh2 antagonists.
AID248439Inhibition of PGD2-induced inositol phosphate formation at human Prostaglandin D2 receptor2005Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
Minor structural modifications convert the dual TP/CRTH2 antagonist ramatroban into a highly selective and potent CRTH2 antagonist.
AID244599Inhibitory activity for PGD2-mediated receptor activation in a fluorescence assay that measures changes in intracellular calcium2005Bioorganic & medicinal chemistry letters, Mar-15, Volume: 15, Issue:6
Isosteric ramatroban analogs: selective and potent CRTH-2 antagonists.
AID429615Displacement of [3H]PGD2 from human prostaglandin D2 receptor in presence of human serum albumin2009Bioorganic & medicinal chemistry letters, Aug-15, Volume: 19, Issue:16
Novel tricyclic antagonists of the prostaglandin D2 receptor DP2 with efficacy in a murine model of allergic rhinitis.
AID248580Inhibition of beta-arrestin translocation at human Thromboxane A2 receptor in BRET assay2005Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
Minor structural modifications convert the dual TP/CRTH2 antagonist ramatroban into a highly selective and potent CRTH2 antagonist.
AID551275Binding affinity to thromboxane receptor2011Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases.
AID238910Inhibition of [3H]-PGD-2 binding to human Prostaglandin D2 receptor2005Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
Minor structural modifications convert the dual TP/CRTH2 antagonist ramatroban into a highly selective and potent CRTH2 antagonist.
AID429624Toxicity in human liver microsomes assessed as GSH adduct formation in presence of NADPH and glutathione2009Bioorganic & medicinal chemistry letters, Aug-15, Volume: 19, Issue:16
Novel tricyclic antagonists of the prostaglandin D2 receptor DP2 with efficacy in a murine model of allergic rhinitis.
AID248754Inhibition of U-46,619-induced inositol phosphate accumulation at human Thromboxane A2 receptor2005Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
Minor structural modifications convert the dual TP/CRTH2 antagonist ramatroban into a highly selective and potent CRTH2 antagonist.
AID431355Potency shift, ratio of IC50 for human CRTh2 receptor in presence of 0.1% HSA to IC50 for human CRTh2 receptor in absence of 0.1% HSA by cAMP accumulation assay2009Bioorganic & medicinal chemistry letters, Aug-15, Volume: 19, Issue:16
7-Azaindole-3-acetic acid derivatives: potent and selective CRTh2 receptor antagonists.
AID431354Antagonist activity against human CRTh2 receptor expressed in CHO cells assessed as effect on cAMP accumulation2009Bioorganic & medicinal chemistry letters, Aug-15, Volume: 19, Issue:16
7-Azaindole-3-acetic acid derivatives: potent and selective CRTh2 receptor antagonists.
AID551273Binding affinity to human recombinant CRTH2 receptor by cell based radioligand equilibrium competition assay2011Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases.
AID5985261-Octanol-water distribution coefficient, log D of the compound at pH 7.4 by shake-flask method2011Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
Lipophilicity of acidic compounds: impact of ion pair partitioning on drug design.
AID429614Displacement of [3H]PGD2 from human prostaglandin D2 receptor2009Bioorganic & medicinal chemistry letters, Aug-15, Volume: 19, Issue:16
Novel tricyclic antagonists of the prostaglandin D2 receptor DP2 with efficacy in a murine model of allergic rhinitis.
AID586985Displacement of [3H]PGD2 from human CRTh2 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay2011Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
Zwitterionic CRTh2 antagonists.
AID244585Inhibitory activity for binding of PGD-2 in hTP binding assay using HEK293 cell membranes2005Bioorganic & medicinal chemistry letters, Mar-15, Volume: 15, Issue:6
Isosteric ramatroban analogs: selective and potent CRTH-2 antagonists.
AID429617Displacement of [3H]PGD2 from prostaglandin D1 receptor in human platelet membrane2009Bioorganic & medicinal chemistry letters, Aug-15, Volume: 19, Issue:16
Novel tricyclic antagonists of the prostaglandin D2 receptor DP2 with efficacy in a murine model of allergic rhinitis.
AID429618Displacement of [3H]SQ-29548 from thromboxane receptor in human platelet membrane2009Bioorganic & medicinal chemistry letters, Aug-15, Volume: 19, Issue:16
Novel tricyclic antagonists of the prostaglandin D2 receptor DP2 with efficacy in a murine model of allergic rhinitis.
AID598525Lipophilicity, log P of the compound2011Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
Lipophilicity of acidic compounds: impact of ion pair partitioning on drug design.
AID92808Anti-platelet activity was measured by studying their antagonist effects on human platelets aggregated with collagen2002Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18
Synthesis and antiaggregant properties of Stabilized analogues of polyunsaturated fatty acid metabolites.
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID244593Inhibitory activity for binding of PGD-2 to CRTH-2 in hCRTH-2 binding assay using HEK293 cell membranes2005Bioorganic & medicinal chemistry letters, Mar-15, Volume: 15, Issue:6
Isosteric ramatroban analogs: selective and potent CRTH-2 antagonists.
AID248959Inhibition of beta-arrestin translocation at human chemoattractant receptor-homologous molecule expressed on TH2 cells in BRET assay2005Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
Minor structural modifications convert the dual TP/CRTH2 antagonist ramatroban into a highly selective and potent CRTH2 antagonist.
AID92098Compound was tested for inhibition of U-46,619 induced aggregation of human platelets1998Bioorganic & medicinal chemistry letters, Jun-02, Volume: 8, Issue:11
Synthesis and biological evaluation of new tetrahydronaphthalene derivatives as thromboxane receptor antagonists.
AID431337Displacement of [3H]PGD2 from human CRTh2 receptor expressed in CHO cells2009Bioorganic & medicinal chemistry letters, Aug-15, Volume: 19, Issue:16
7-Azaindole-3-acetic acid derivatives: potent and selective CRTh2 receptor antagonists.
AID429623Induction of CYP3A4 activity in cryopreserved human hepatocytes at 10 uM using midazolam as substrate after 2 days relative to rifampicin2009Bioorganic & medicinal chemistry letters, Aug-15, Volume: 19, Issue:16
Novel tricyclic antagonists of the prostaglandin D2 receptor DP2 with efficacy in a murine model of allergic rhinitis.
AID551274Binding affinity to prostanoid DP1 receptor2011Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1346326Human DP2 receptor (Prostanoid receptors)2005European journal of pharmacology, Nov-07, Volume: 524, Issue:1-3
CRTH2-specific binding characteristics of [3H]ramatroban and its effects on PGD2-, 15-deoxy-Delta12, 14-PGJ2- and indomethacin-induced agonist responses.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1346300Rat DP2 receptor (Prostanoid receptors)2003The Journal of pharmacology and experimental therapeutics, Nov, Volume: 307, Issue:2
Chemoattractant receptor-homologous molecule expressed on Th2 cells activation in vivo increases blood leukocyte counts and its blockade abrogates 13,14-dihydro-15-keto-prostaglandin D2-induced eosinophilia in rats.
AID1346401Mouse DP2 receptor (Prostanoid receptors)2005The Journal of biological chemistry, Sep-16, Volume: 280, Issue:37
Identification of determinants of ligand binding affinity and selectivity in the prostaglandin D2 receptor CRTH2.
AID1346422Human TP receptor (Prostanoid receptors)1992Biochemical pharmacology, Aug-04, Volume: 44, Issue:3
Binding characteristics of the new thromboxane A2/prostaglandin H2 receptor antagonist [3H]BAY U 3405 to washed human platelets and platelet membranes.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (138)

TimeframeStudies, This Drug (%)All Drugs %
pre-19903 (2.17)18.7374
1990's58 (42.03)18.2507
2000's45 (32.61)29.6817
2010's22 (15.94)24.3611
2020's10 (7.25)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 29.26

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index29.26 (24.57)
Research Supply Index5.03 (2.92)
Research Growth Index5.94 (4.65)
Search Engine Demand Index36.71 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (29.26)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials10 (7.04%)5.53%
Reviews9 (6.34%)6.00%
Case Studies2 (1.41%)4.05%
Observational0 (0.00%)0.25%
Other121 (85.21%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (2)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Randomized, Double-Blind, Placebo-Controlled, Parallel-Design, Multi- Centre, Adaptive Phase 2/Phase 3 Study To Evaluate The Efficacy And Safety Of Ramatroban Along With The Standard Of Care In Subjects Hospitalized For SARS-CoV-2 Infection [NCT05706454]Phase 2/Phase 3324 participants (Anticipated)Interventional2022-11-10Recruiting
A Randomized Double-blind and Placebo-controlled Study to the Influence of Ramatroban/Montelukast Versus Montelukast/Placebo on the Early Allergic Reaction in Patients With Mild to Moderate Atopic Asthma (House Dust Mite) [NCT00311051]Phase 2/Phase 30 participants (Actual)Interventional2005-04-30Withdrawn
[information is prepared from clinicaltrials.gov, extracted Sep-2024]