| Assay ID | Title | Year | Journal | Article |
|---|
| AID551287 | Oxidative metabolism in human microsomes assessed as protein covalent binding | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
| Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases. |
| AID551298 | Volume of distribution at steady state in cynomolgus monkey at 1 mg/kg, po and 0.5 mg/kg, iv | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
| Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases. |
| AID551280 | Inhibition of CYP2C9 | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
| Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases. |
| AID705368 | Inhibition of CRTH2 in human whole blood | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
| Update on the development of antagonists of chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTH2). From lead optimization to clinical proof-of-concept in asthma and allergic rhinitis. |
| AID628374 | Inverse agonist activity at human CRTH2 expressed in chinese hamster CHO cells by [35S]GTPgamma binding assay relative to control | 2011 | Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
| Discovery of potent, selective, and orally bioavailable alkynylphenoxyacetic acid CRTH2 (DP2) receptor antagonists for the treatment of allergic inflammatory diseases. |
| AID429617 | Displacement of [3H]PGD2 from prostaglandin D1 receptor in human platelet membrane | 2009 | Bioorganic & 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. |
| AID429619 | Displacement of [3H]iloprost from human prostacyclin receptor expressed in human 293 cell membrane | 2009 | Bioorganic & 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. |
| AID551289 | Clearance in Sprague-Dawley rat at 10 mg/kg, po and 5 mg/kg, iv | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
| Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases. |
| AID551296 | Oral bioavailability in cynomolgus monkey at 1 mg/kg | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
| Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases. |
| AID598046 | Oral bioavailability in Sprague-Dawley rat at 5 mg/kg | 2011 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 21, Issue:11
| New indole amide derivatives as potent CRTH2 receptor antagonists. |
| AID598051 | Inhibition of CYP2C9 | 2011 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 21, Issue:11
| New indole amide derivatives as potent CRTH2 receptor antagonists. |
| AID550701 | Inhibition of CYP2C9 | 2011 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
| Azaindoles as potent CRTH2 receptor antagonists. |
| AID550697 | Antagonist activity at human CRTH2 expressed in HEK293 cells assessed as inhibition of forskolin-induced increase intracellular [125I]cAMP level by scintillation proximity assay | 2011 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
| Azaindoles as potent CRTH2 receptor antagonists. |
| AID598050 | Inhibition of CYP3A4 | 2011 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 21, Issue:11
| New indole amide derivatives as potent CRTH2 receptor antagonists. |
| AID550705 | Clearance in Sprague-Dawley rat at 5 mg/kg, po and 1 mg/kg, iv | 2011 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
| Azaindoles as potent CRTH2 receptor antagonists. |
| AID551274 | Binding affinity to prostanoid DP1 receptor | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
| Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases. |
| AID551308 | Metabolic stability in human hepatocytes | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
| Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases. |
| AID429623 | Induction of CYP3A4 activity in cryopreserved human hepatocytes at 10 uM using midazolam as substrate after 2 days relative to rifampicin | 2009 | Bioorganic & 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. |
| AID551282 | Inhibition of human CYP3A4-mediated degradation of testosterone to 6-beta-hydroxytestosterone at 10 uM | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
| Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases. |
| AID550698 | Antagonist activity at CRTH2 in human eosinophil assessed as effect of cellular shape change by EOS assay | 2011 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
| Azaindoles as potent CRTH2 receptor antagonists. |
| AID551293 | Clearance in Beagle dog at 1 mg/kg, po and 0.5 mg/kg, iv | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
| Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases. |
| AID429614 | Displacement of [3H]PGD2 from human prostaglandin D2 receptor | 2009 | Bioorganic & 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. |
| AID551294 | Volume of distribution at steady state in Beagle dog at 1 mg/kg, po and 0.5 mg/kg, iv | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
| Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases. |
| AID551273 | Binding affinity to human recombinant CRTH2 receptor by cell based radioligand equilibrium competition assay | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
| Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases. |
| AID551283 | Induction of pregnane X receptor | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
| Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases. |
| AID550706 | Volume of distribution in Sprague-Dawley rat at 5 mg/kg, po and 1 mg/kg, iv | 2011 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
| Azaindoles as potent CRTH2 receptor antagonists. |
| AID551305 | Metabolic stability in Beagle dog hepatocytes | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
| Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases. |
| AID550702 | Inhibition of CYP3A4 | 2011 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
| Azaindoles as potent CRTH2 receptor antagonists. |
| AID597989 | Antagonist activity at human CRTH2 receptor expressed in HEK293-EBNA cells assessed as inhibition of forskolin-stimulated intracellular cAMP production by [125I]-cAMP scintillation proximity assay | 2011 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 21, Issue:11
| New indole amide derivatives as potent CRTH2 receptor antagonists. |
| AID551301 | Clearance in rhesus monkey at 1 mg/kg, po and 0.5 mg/kg, iv | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
| Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases. |
| AID598039 | Inhibition of PGD2-induced eosinophil shape change in human whole blood | 2011 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 21, Issue:11
| New indole amide derivatives as potent CRTH2 receptor antagonists. |
| AID551281 | Inhibition of CYP3A4 | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
| Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases. |
| AID429620 | Inhibition of human CYP3A4 | 2009 | Bioorganic & 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. |
| AID598047 | Clearance in Sprague-Dawley rat at 5 mg/kg, po and 1 mg/kg, iv | 2011 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 21, Issue:11
| New indole amide derivatives as potent CRTH2 receptor antagonists. |
| AID551277 | Antagonist activity at human recombinant CRTH2 receptor expressed in HEK293 cells assessed as inhibition of DK-PGD2-induced intracellular cAMP formation | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
| Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases. |
| AID551288 | Oral bioavailability in Sprague-Dawley rat at 10 mg/kg | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
| Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases. |
| AID551278 | Antagonist activity at CRTH2 receptor in human whole blood assessed as inhibition of DK-PGD2-induced eosinophils shape change | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
| Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases. |
| AID550707 | Half life in Sprague-Dawley rat at 5 mg/kg, po and 1 mg/kg, iv | 2011 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
| Azaindoles as potent CRTH2 receptor antagonists. |
| AID550700 | Displacement of radioligand from prostanoid TP receptor expressed in HEK293 cells by competitive binding assay | 2011 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
| Azaindoles as potent CRTH2 receptor antagonists. |
| AID550699 | Displacement of radioligand from prostanoid DP receptor expressed in HEK293 cells by competitive binding assay | 2011 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
| Azaindoles as potent CRTH2 receptor antagonists. |
| AID551285 | Inhibition of human ERG | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
| Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases. |
| AID597988 | Binding affinity to human CRTH2 receptor expressed in HEK293-EBNA cells by radioligand competition binding assay | 2011 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 21, Issue:11
| New indole amide derivatives as potent CRTH2 receptor antagonists. |
| AID598049 | Half life in Sprague-Dawley rat at 5 mg/kg, po and 1 mg/kg, iv | 2011 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 21, Issue:11
| New indole amide derivatives as potent CRTH2 receptor antagonists. |
| AID551292 | Oral bioavailability in Beagle dog at 1 mg/kg | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
| Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases. |
| AID705369 | Displacement of [3H]PGD2 from human CRTH2 expressed in HEK293 cells after 60 mins by liquid scintillation counting | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
| Update on the development of antagonists of chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTH2). From lead optimization to clinical proof-of-concept in asthma and allergic rhinitis. |
| AID550696 | Displacement of radioligand from human CRTH2 expressed in HEK293 cells by competitive binding assay | 2011 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
| Azaindoles as potent CRTH2 receptor antagonists. |
| AID551303 | Terminal half life in rhesus monkey at 1 mg/kg, po and 0.5 mg/kg, iv | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
| Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases. |
| AID429622 | Inhibition of human CYP2D6 | 2009 | Bioorganic & 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. |
| AID551304 | Metabolic stability in Sprague-Dawley rat hepatocytes | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
| Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases. |
| AID551290 | Volume of distribution at steady state in Sprague-Dawley rat at 10 mg/kg, po and 5 mg/kg, iv | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
| Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases. |
| AID551306 | Metabolic stability in cynomolgus monkey hepatocytes | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
| Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases. |
| AID551291 | Terminal half life in Sprague-Dawley rat at 10 mg/kg, po and 5 mg/kg, iv | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
| Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases. |
| AID551275 | Binding affinity to thromboxane receptor | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
| Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases. |
| AID551276 | Binding affinity to prostanoid receptor | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
| Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases. |
| AID551286 | Oxidative metabolism in rat microsomes assessed as protein covalent binding | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
| Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases. |
| AID429618 | Displacement of [3H]SQ-29548 from thromboxane receptor in human platelet membrane | 2009 | Bioorganic & 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. |
| AID551299 | Terminal half life in cynomolgus monkey at 1 mg/kg, po and 0.5 mg/kg, iv | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
| Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases. |
| AID551310 | Drug excretion in permanently bile-cannulated rat bile assessed as parent compound level at 1 mg/kg, iv after 48 hrs | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
| Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases. |
| AID551284 | Photosensitivity of the compound in MeOH solution assessed as degradation at 2 mM after 15 mins presence of UV light | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
| Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases. |
| AID429616 | Inhibition of eosinophil degranulation in human whole blood assessed as change in morphology after 4 mins using flow cytometry by leukocyte shape change assay | 2009 | Bioorganic & 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. |
| AID551302 | Volume of distribution at steady state in rhesus monkey at 1 mg/kg, po and 0.5 mg/kg, iv | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
| Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases. |
| AID429615 | Displacement of [3H]PGD2 from human prostaglandin D2 receptor in presence of human serum albumin | 2009 | Bioorganic & 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. |
| AID550704 | Bioavailability in Sprague-Dawley rat at 1 mg/kg, iv | 2011 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
| Azaindoles as potent CRTH2 receptor antagonists. |
| AID551279 | Inhibition of CYP2D6 | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
| Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases. |
| AID429621 | Inhibition of human CYP2C9 | 2009 | Bioorganic & 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. |
| AID551295 | Terminal half life in Beagle dog at 1 mg/kg, po and 0.5 mg/kg, iv | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
| Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases. |
| AID551300 | Oral bioavailability in rhesus monkey at 1 mg/kg | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
| Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases. |
| AID551307 | Metabolic stability in rhesus monkey hepatocytes | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
| Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases. |
| AID598048 | Volume of distribution in Sprague-Dawley rat at 5 mg/kg, po and 1 mg/kg, iv | 2011 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 21, Issue:11
| New indole amide derivatives as potent CRTH2 receptor antagonists. |
| AID551297 | Clearance in cynomolgus monkey at 1 mg/kg, po and 0.5 mg/kg, iv | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
| Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |