| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
| Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings 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. |
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings 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. |
| AID1274617 | Time-dependent inhibition of microsomal CYP3A4 (unknown origin) using midazolam as substrate assessed as alpha-hydroxymidazolam-d4 at 10 uM pre-incubated for 12 mins before NADPH addition formation after 30 mins by LC-MS/MS analysis | 2016 | Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1
| Discovery and Characterization of 2-Acylaminoimidazole Microsomal Prostaglandin E Synthase-1 Inhibitors. |
| AID405537 | Inhibition of PGE2 synthesis in human A549 cells | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
| Microsomal prostaglandin E2 synthase-1 (mPGES-1): a novel anti-inflammatory therapeutic target. |
| AID405545 | Inhibition of PGF2 production in humanixed knock-in mouse stomach at 100 mg/kg | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
| Microsomal prostaglandin E2 synthase-1 (mPGES-1): a novel anti-inflammatory therapeutic target. |
| AID446424 | Analgesic activity against LPS-induced thermal hyperalgesia in po dosed Hartley guinea pig assessed as decrease in paw withdrawal latency administered 1 hr before LPS challenge measured after 4.5 hrs | 2009 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
| Discovery of disubstituted phenanthrene imidazoles as potent, selective and orally active mPGES-1 inhibitors. |
| AID580217 | Inhibition of mPGES1 | 2011 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 21, Issue:5
| Trisubstituted ureas as potent and selective mPGES-1 inhibitors. |
| AID446421 | Inhibition of TX synthase | 2009 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
| Discovery of disubstituted phenanthrene imidazoles as potent, selective and orally active mPGES-1 inhibitors. |
| AID580219 | Inhibition of PGF synthase in IL1-beta treated human A549 cell microsome assessed as inhibition of PGF2alpha production after 1 min in presence of 50% FBS | 2011 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 21, Issue:5
| Trisubstituted ureas as potent and selective mPGES-1 inhibitors. |
| AID1333646 | Inhibition of human recombinant mPGES-1 expressed in CHO cells assessed as reduction in conversion of PGH2 to PGE2 incubated for 10 mins followed by substrate addition measured after 1 min in presence of GSH | | | |
| AID405526 | Inhibition of rat mPGES1 | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
| Microsomal prostaglandin E2 synthase-1 (mPGES-1): a novel anti-inflammatory therapeutic target. |
| AID446419 | Inhibition of PGES1 in guinea pig whole blood | 2009 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
| Discovery of disubstituted phenanthrene imidazoles as potent, selective and orally active mPGES-1 inhibitors. |
| AID580220 | Inhibition of mPGES1 in LPS-stimulated human whole blood assessed as inhibition of PGE2 production | 2011 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 21, Issue:5
| Trisubstituted ureas as potent and selective mPGES-1 inhibitors. |
| AID1274613 | Inhibition of mPGES1 in LPS-induced human whole blood assessed as suppression of PGE2 response after 20 to 24 hrs by LC-MS/MS analysis | 2016 | Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1
| Discovery and Characterization of 2-Acylaminoimidazole Microsomal Prostaglandin E Synthase-1 Inhibitors. |
| AID317366 | Cmax in rat at 20 mg/kg, po | 2007 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
| Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors. |
| AID446417 | Metabolic stability in rat liver hepatocytes assessed as compound remaining after 2 hrs | 2009 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
| Discovery of disubstituted phenanthrene imidazoles as potent, selective and orally active mPGES-1 inhibitors. |
| AID405542 | Inhibition of guinea pig mPGES1 | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
| Microsomal prostaglandin E2 synthase-1 (mPGES-1): a novel anti-inflammatory therapeutic target. |
| AID446428 | Half life in monkey | 2009 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
| Discovery of disubstituted phenanthrene imidazoles as potent, selective and orally active mPGES-1 inhibitors. |
| AID446414 | Inhibition of PGE2 production in LPS-stimulated human whole blood | 2009 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
| Discovery of disubstituted phenanthrene imidazoles as potent, selective and orally active mPGES-1 inhibitors. |
| AID405539 | Selectivity for human mPGES1 over PGE2 | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
| Microsomal prostaglandin E2 synthase-1 (mPGES-1): a novel anti-inflammatory therapeutic target. |
| AID1226828 | Inhibition of purified mPGES-1 (1 to 152) (unknown origin) extracted from detergent-solubilized baculovirus-infected insect Sf9 cell membranes using PGH2 as substrate assessed as PGE2 production after 2.5 mins by LC/MS analysis | 2015 | Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11
| Crystal Structures of mPGES-1 Inhibitor Complexes Form a Basis for the Rational Design of Potent Analgesic and Anti-Inflammatory Therapeutics. |
| AID317359 | Inhibition of human mPGES2 | 2007 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
| Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors. |
| AID1166435 | Inhibition of guinea pig recombinant mPGES-1 | 2014 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 24, Issue:20
| Development of 2-aryl substituted quinazolin-4(3H)-one, pyrido[4,3-d]pyrimidin-4(3H)-one and pyrido[2,3-d]pyrimidin-4(3H)-one derivatives as microsomal prostaglandin E(2) synthase-1 inhibitors. |
| AID405541 | Inhibition of LPS-stimulated PGE2 production in human whole blood | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
| Microsomal prostaglandin E2 synthase-1 (mPGES-1): a novel anti-inflammatory therapeutic target. |
| AID698649 | Inhibition of mPGES1 expressed in Escherichia coli Rosetta-DE3 assessed as reduction in PGE2 production by enzyme immunoassay based cell-free system assay | 2012 | Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6
| Dynamic modeling of human 5-lipoxygenase-inhibitor interactions helps to discover novel inhibitors. |
| AID446420 | Inhibition of human PGES2 | 2009 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
| Discovery of disubstituted phenanthrene imidazoles as potent, selective and orally active mPGES-1 inhibitors. |
| AID1152198 | Inhibition of microsomal PGES-1 (unknown origin) assessed as PGH2 conversion to PGE2 after 1 min by enzyme immunoassay | 2014 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12
| Benzo[d]isothiazole 1,1-dioxide derivatives as dual functional inhibitors of 5-lipoxygenase and microsomal prostaglandin E(2) synthase-1. |
| AID446412 | Displacement of [3H]PGH2 from human recombinant PGES1 expressed in CHOK1 cells | 2009 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
| Discovery of disubstituted phenanthrene imidazoles as potent, selective and orally active mPGES-1 inhibitors. |
| AID317365 | Oral bioavailability in rat at 20 mg/kg | 2007 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
| Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors. |
| AID1333647 | Inhibition of mPGES-1 in human A549 cells assessed as reduction in interleukin-1 beta-induced PGE2 production incubated for 30 mins followed by IL-1beta stimulation for 16 to 20 hrs in presence of 2% fetal bovine serum by HTRF assay | | | |
| AID317358 | Inhibition of guinea pig mPGES1 | 2007 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
| Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors. |
| AID446413 | Inhibition of mPGES1 in IL-1-beta-stimulated human A549 cells assessed as blockade of PGH2 to PGE2 conversion in presence of 50% fetal bovine serum | 2009 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
| Discovery of disubstituted phenanthrene imidazoles as potent, selective and orally active mPGES-1 inhibitors. |
| AID405544 | Inhibition of LPS-induced hyperalgesia in guinea pig | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
| Microsomal prostaglandin E2 synthase-1 (mPGES-1): a novel anti-inflammatory therapeutic target. |
| AID317362 | Inhibition of LPS-stimulated TXB2 production in human whole blood | 2007 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
| Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors. |
| AID733350 | Inhibition of PGES-1 in human whole blood assessed as LPS-induced PGE2 formation incubated for 15 mins prior to LPS addition measured after 24 hrs by EIA | 2013 | Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8
| Discovery of highly potent microsomal prostaglandin e2 synthase 1 inhibitors using the active conformation structural model and virtual screen. |
| AID446422 | Inhibition of PGF2alpha production in human A549 cells in presence of 50% fetal bovine serum | 2009 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
| Discovery of disubstituted phenanthrene imidazoles as potent, selective and orally active mPGES-1 inhibitors. |
| AID405538 | Inhibition of PGE2alpha synthesis in human A549 cells | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
| Microsomal prostaglandin E2 synthase-1 (mPGES-1): a novel anti-inflammatory therapeutic target. |
| AID405546 | Inhibition of LPS-stimulated TBX2 production in human whole blood | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
| Microsomal prostaglandin E2 synthase-1 (mPGES-1): a novel anti-inflammatory therapeutic target. |
| AID721277 | Inhibition of human recombinant mPGES-1 using PGH2 as substrate incubated 20 mins prior to substrate addition measured after 30 secs by EIA | 2013 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 23, Issue:3
| Novel benzoxazole inhibitors of mPGES-1. |
| AID1474675 | Inhibition of recombinant human mPGES-1 expressed in CHO cells assessed as reduction in PGE2 formation using PGH2 a substrate preincubated for 10 mins followed by substrate addition measured after 1 min | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
| Tricyclic 4,4-dimethyl-3,4-dihydrochromeno[3,4-d]imidazole derivatives as microsomal prostaglandin E |
| AID1274612 | Inhibition of mPGES1 in rhIL-1beta-stimulated human A549 cells assessed as PGE2 level treated for 18 hrs after 30 mins pre-incubation with rhIL-1beta by EIA method | 2016 | Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1
| Discovery and Characterization of 2-Acylaminoimidazole Microsomal Prostaglandin E Synthase-1 Inhibitors. |
| AID317363 | Inhibition of human JAK2 | 2007 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
| Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors. |
| AID317360 | Inhibition of TX synthase | 2007 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
| Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors. |
| AID317357 | Inhibition of rat mPGES1 | 2007 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
| Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors. |
| AID317361 | Inhibition of LPS-stimulated PGE2 production in human whole blood | 2007 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
| Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors. |
| AID317351 | Inhibition of IL-1-beta-stimulated PGE2 production in human A549 cells in presence of 50% fetal bovine serum | 2007 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
| Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors. |
| AID1274611 | Inhibition of human microsomal PGES1 expressed in 293E cells by LC/MS/MS analysis | 2016 | Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1
| Discovery and Characterization of 2-Acylaminoimidazole Microsomal Prostaglandin E Synthase-1 Inhibitors. |
| AID405540 | Selectivity for human mPGES1 over PGE2alpha | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
| Microsomal prostaglandin E2 synthase-1 (mPGES-1): a novel anti-inflammatory therapeutic target. |
| AID317367 | Inhibition of LPS-induced hyperalgesia in guinea pig at 30 mg/kg, po relative to control | 2007 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
| Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors. |
| AID639314 | Inhibition of microsomal PGES1 transfected in human HEK293 cells assessed as PGE2 production after 60 mins by HTRF assay | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
| Synthesis and SAR study of imidazoquinolines as a novel structural class of microsomal prostaglandin E₂ synthase-1 inhibitors. |
| AID580218 | Inhibition of mPGES1 in IL1-beta treated human A549 cell microsome assessed as inhibition of PGE2 production after 1 min in presence of 50% FBS | 2011 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 21, Issue:5
| Trisubstituted ureas as potent and selective mPGES-1 inhibitors. |
| AID698648 | Inhibition of mPGES1 in LPS-stimulated human whole blood assessed as reduction in PGE2 production incubated for 24 hrs at 37 degC by enzyme immunoassay | 2012 | Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6
| Dynamic modeling of human 5-lipoxygenase-inhibitor interactions helps to discover novel inhibitors. |
| AID1367396 | Inhibition of mPGES1 in human whole blood assessed as inhibition of LPS-induced PGE2 production measured after 20 to 24 hrs | 2017 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23
| Discovery of furan and dihydrofuran-fused tricyclic benzo[d]imidazole derivatives as potent and orally efficacious microsomal prostaglandin E synthase-1 (mPGES-1) inhibitors: Part-1. |
| AID317354 | Inhibition of IL-1-beta-stimulated PGF2alpha production in human A549 cells in presence of 50% fetal bovine serum | 2007 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
| Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors. |
| AID1226827 | Inhibition of recombinant human mPGES-1 expressed in human 293E cell microsomes using PGH2 as substrate assessed as PGE2 production after 2.5 mins by LC/MS analysis | 2015 | Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11
| Crystal Structures of mPGES-1 Inhibitor Complexes Form a Basis for the Rational Design of Potent Analgesic and Anti-Inflammatory Therapeutics. |
| AID733351 | Inhibition of full-length microsomal PGES-1 (unknown origin) expressed in Escherichia coli Rosetta(DE3) using PGH2 as substrate assessed as inhibition of PGH2 conversion to PGE2 incubated 15 mins prior to substrate addition measured after 1 min by EIA | 2013 | Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8
| Discovery of highly potent microsomal prostaglandin e2 synthase 1 inhibitors using the active conformation structural model and virtual screen. |
| AID446418 | Metabolic stability in human liver hepatocytes assessed as compound remaining after 2 hrs | 2009 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
| Discovery of disubstituted phenanthrene imidazoles as potent, selective and orally active mPGES-1 inhibitors. |
| AID580215 | Inhibition of TX synthase in LPS-stimulated human whole blood assessed as inhibition of TXB2 production | 2011 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 21, Issue:5
| Trisubstituted ureas as potent and selective mPGES-1 inhibitors. |
| AID465968 | Inhibition of human mPGES1 assessed as PGE2 level after 41 sec by ELISA | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
| Selective inducible microsomal prostaglandin E(2) synthase-1 (mPGES-1) inhibitors derived from an oxicam template. |
| AID446415 | Half life in rat at 5 mg/kg, iv administered as single dose | 2009 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
| Discovery of disubstituted phenanthrene imidazoles as potent, selective and orally active mPGES-1 inhibitors. |
| AID1474676 | Inhibition of mPGES-1 in human A549 cells assessed as decrease in IL1beta induced PGE2 release preincubated for 30 mins followed by IL-1beta addition after 16 to 20 hrs by HTRF method | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
| Tricyclic 4,4-dimethyl-3,4-dihydrochromeno[3,4-d]imidazole derivatives as microsomal prostaglandin E |
| AID1226829 | Binding affinity to mPGES-1 (unknown origin) assessed as increase in protein aggregation temperature at 0.1 mM by differential static light scattering method | 2015 | Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11
| Crystal Structures of mPGES-1 Inhibitor Complexes Form a Basis for the Rational Design of Potent Analgesic and Anti-Inflammatory Therapeutics. |
| AID405527 | Inhibition of human recombinant mPGES1 expressed in CHO cells | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
| Microsomal prostaglandin E2 synthase-1 (mPGES-1): a novel anti-inflammatory therapeutic target. |
| AID317364 | Inhibition of human JAK3 | 2007 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
| Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors. |
| AID317350 | Inhibition of human recombinant mPGES1 | 2007 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
| Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors. |
| AID446423 | Inhibition of TXB2 production in LPS-stimulated human whole blood | 2009 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
| Discovery of disubstituted phenanthrene imidazoles as potent, selective and orally active mPGES-1 inhibitors. |
| AID1333648 | Inhibition of mPGES-1 in human whole blood assessed as reduction in LPS-induced PGE2 production preincubated followed by LPS stimulation for 20 to 24 hrs | | | |
| AID1274616 | Inhibition of microsomal CYP3A4 (unknown origin) using bufuralol/midazolam/diclofinac as substrate assessed as 1-hydroxybufuralol maleate-d9/alpha-hydroxymidazolam-d4/[13C6]-4-hydroxydiclofinac formation at 10 uM pre-incubated for 10 mins before NADPH add | 2016 | Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1
| Discovery and Characterization of 2-Acylaminoimidazole Microsomal Prostaglandin E Synthase-1 Inhibitors. |
| AID317368 | Inhibition of LPS-induced hyperalgesia in guinea pig at 100 mg/kg, po relative to control | 2007 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
| Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |