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Half life in human
Assay data:1 Tested
SummaryPubMed Citation
Antiglaucoma activity in ocular hypersensitive monkey assessed as reduction in intraocular pressure
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed Citation
Binding affinity to EP2 (unknown origin) assessed as inhibition constant
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Potency index, ratio of CP-533,536 EC50 to compound EC50 for recombinant human EP2 receptor expressed in HEK293 cells by cAMP accumulation assay
SummaryPubMed CitationRelated BioAssays by Target
Reduction of intraocular pressure in ocular normotensive cynomolgus monkey at 0.3 to 1% administered topically to the eyes once daily at around 5 pm from day 1 to day 14 and measured at 10 pm at day 8 and 15 post dose
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed Citation
Induction of CYP1A2 in human Fa2N-4 cells up to 100 uM using phenacetin as substrate incubated for 24 hrs followed by compound replacement for every 24 hrs during 72 hrs incubation period followed by substrate addition for 4 hrs by LC-MS analysis
Induction of CYP3A4 in human Fa2N-4 cells up to 100 uM using testosterone as substrate incubated for 24 hrs followed by compound replacement for every 24 hrs during 72 hrs incubation period followed by substrate addition for 4 hrs by LC-MS analysis
Inhibition of recombinant human CYP1A2 using 3-cyano-7-ethoxycoumarin fluorescent substrate in presence of NADPH-generating system after 15 mins
Inhibition of recombinant human CYP2C19 using 3-cyano-7-ethoxycoumarin fluorescent substrate in presence of NADPH-generating system after 15 mins
Inhibition of recombinant human CYP2C9 using 7-methoxy-4-(trifluoromethyl)coumarin fluorescent substrate in presence of NADPH-generating system after 15 mins
Inhibition of recombinant human CYP2D6 using 3-(2-(N,N-diethyl-N-methylammonium)ethyl)-7-methoxy-4-methylcoumariniodide fluorescent substrate in presence of NADPH-generating system after 15 mins
Inhibition of recombinant human CYP3A4 using 7-benzyloxyquinoline fluorescent substrate in presence of NADPH-generating system after 15 mins
Drug metabolism in human liver microsomes assessed as metabolic rate at 10 uM after 30 mins by HPLC-MS analysis
Apparent permeability of the compound at 100 uM after 5 hrs by PAMPA
Assay data:2 Tested
Apparent permeability from apical side at pH 6.5 to basolateral side at pH 7.4 in human Caco2 cells a 10 uM after 30 to 120 mins by HPLC-MS analysis
Apparent permeability from apical side at pH 7.4 to basolateral side at pH 7.4 in human Caco2 cells a 10 uM after 30 to 120 mins by HPLC-MS analysis
Displacement of [3H]prostaglandin E2 from recombinant human full length EP4 receptor expressed in Chem-1 cell membranes after 60 mins by liquid scintillation counting
Assay data:2 Active, 1 Activity ≤ 1 µM, 3 Tested
Displacement of [3H]prostaglandin E2 from recombinant human full length EP3 receptor expressed in Chem-1 cell membranes after 60 mins by liquid scintillation counting
Assay data:1 Active, 1 Activity ≤ 1 µM, 3 Tested
Displacement of [3H]prostaglandin E2 from recombinant human full length EP1 receptor expressed in Chem-1 cell membranes after 60 mins by liquid scintillation counting
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
Assay data:32 Active, 36 Activity ≤ 1 µM, 36 Tested
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