Assay ID | Title | Year | Journal | Article |
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. |
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. |
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. |
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. |
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. |
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. |
AID705355 | Inhibition of rat aldose reductase | 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. |
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. |
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. |
AID705364 | Antagonistic activity at CRTH2 in human eosinophils assessed as inhibition of PGD2-induced calcium mobilization after 60 mins by Fluo-3 based fluorescence assay | 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. |
AID749181 | Antagonist activity at CRTh2 receptor (unknown origin) overexpressed in CHOK1 cell membranes assessed as inhibition of [35S]-GTPgammaS binding preincubated for 1 hr followed by 50 nM PGD2 and 0.1 nM [35S]-GTPgammaS addition measured after 2 hrs by liquid | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
| 2-(1H-Pyrazol-4-yl)acetic acids as CRTh2 antagonists. |
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. |
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. |
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. |
AID705357 | Antagonist activity at CRTH2 expressed in Th2 cells assessed as inhibition of PGD2-induced antiapoptotic activity | 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. |
AID705363 | Oral bioavailability in rat | 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. |
AID705359 | Antagonist activity at CRTH2 expressed in Th2 cells assessed as inhibition of PGD2-induced chemotaxis | 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. |
AID705362 | Half life in rat | 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. |
AID705358 | Antagonist activity at CRTH2 expressed in Th2 cells assessed as inhibition of PGD2-induced IL13 production | 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. |
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. |
AID705361 | Inhibition of CRTH2 in human whole blood relative to control | 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. |
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. |
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. |
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. |
AID705360 | Antagonist activity at CRTH2 in human eosinophils assessed as inhibition of PGD2-induced shape change | 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. |
AID1346326 | Human DP2 receptor (Prostanoid receptors) | 2012 | The Journal of pharmacology and experimental therapeutics, Feb, Volume: 340, Issue:2
| Pharmacologic profile of OC000459, a potent, selective, and orally active D prostanoid receptor 2 antagonist that inhibits mast cell-dependent activation of T helper 2 lymphocytes and eosinophils. |
AID1346300 | Rat DP2 receptor (Prostanoid receptors) | 2012 | The Journal of pharmacology and experimental therapeutics, Feb, Volume: 340, Issue:2
| Pharmacologic profile of OC000459, a potent, selective, and orally active D prostanoid receptor 2 antagonist that inhibits mast cell-dependent activation of T helper 2 lymphocytes and eosinophils. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |