Assay ID | Title | Year | Journal | Article |
AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347081 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Confirmatory Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
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. |
AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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. |
AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347084 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Confirmatory Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347154 | Primary screen GU AMC 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. |
AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347088 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): Viability assay - Alamar blue signal for LCMV Confirmatory Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | | | |
AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4
| A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347087 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Confirmatory Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1190578 | Binding affinity to PDE10A (unknown origin) | 2015 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 25, Issue:4
| Synthesis and in vitro characterization of cinnoline and benzimidazole analogues as phosphodiesterase 10A inhibitors. |
AID715546 | Selectivity ratio of Ki for human PDE11A to Ki for human PDE10A | 2012 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18
| Discovery of tetrahydropyridopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia. |
AID1724759 | Binding affinity to recombinant human galectin 3 assessed as dissociation constant by fluorescent anisotropy assay | 2020 | ACS medicinal chemistry letters, Sep-10, Volume: 11, Issue:9
| Quinoline-Pyrazole Scaffold as a Novel Ligand of Galectin-3 and Suppressor of TREM2 Signaling. |
AID442318 | Binding affinity to PDE1C | 2009 | Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
| Identification of a brain penetrant PDE9A inhibitor utilizing prospective design and chemical enablement as a rapid lead optimization strategy. |
AID428644 | Volume of distribution at steady state in Beagle dog at 0.3 mg/kg, iv | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
| Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia. |
AID767808 | Intrinsic clearance in human liver microsomes | 2013 | Bioorganic & medicinal chemistry, Oct-01, Volume: 21, Issue:19
| N-Methylanilide and N-methylbenzamide derivatives as phosphodiesterase 10A (PDE10A) inhibitors. |
AID677554 | Displacement of [3H]5-(6,7-dimethoxycinnolin-4-yl)-N-isopropyl-3-methylpyridin-2-amine from PDE10A in Sprague-Dawley rat striatum | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
| Rapid identification of a novel small molecule phosphodiesterase 10A (PDE10A) tracer. |
AID705195 | Selectivity ratio of IC50 for PDE4 to IC50 for PDE10A | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Current landscape of phosphodiesterase 10A (PDE10A) inhibition. |
AID1724766 | Antiinflammatory activity in mouse BV-2 cells assessed as reduction in Abeta-induced IL-12 release at 10 uM incubated for 12 hrs by ELISA relative to control | 2020 | ACS medicinal chemistry letters, Sep-10, Volume: 11, Issue:9
| Quinoline-Pyrazole Scaffold as a Novel Ligand of Galectin-3 and Suppressor of TREM2 Signaling. |
AID1724762 | Antiinflammatory activity in mouse BV-2 cells assessed as reduction in Abeta-induced TNFalpha release incubated for 12 hrs by ELISA | 2020 | ACS medicinal chemistry letters, Sep-10, Volume: 11, Issue:9
| Quinoline-Pyrazole Scaffold as a Novel Ligand of Galectin-3 and Suppressor of TREM2 Signaling. |
AID715549 | Selectivity ratio of Ki for human PDE7A to Ki for human PDE10A | 2012 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18
| Discovery of tetrahydropyridopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia. |
AID615724 | Inhibition of rat PDE10A | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| Synthesis and in vitro evaluation of new analogues as inhibitors for phosphodiesterase 10A. |
AID428642 | Hepatic clearance in cynomolgus monkey at 0.03 mg/kg, iv | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
| Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia. |
AID1235025 | Inhibition of PDE10A (unknown origin) | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
| BN/CC isosterism in borazaronaphthalenes towards phosphodiesterase 10A (PDE10A) inhibitors. |
AID428650 | Half life in cynomolgus monkey at 0.03 mg/kg, iv | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
| Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia. |
AID428654 | Behavioral effect in mouse assessed as conditioned avoidance response at 115 nM plasma exposure | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
| Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia. |
AID1724764 | Antiinflammatory activity in mouse BV-2 cells assessed as reduction in Abeta-induced IL-8 release incubated for 12 hrs by ELISA | 2020 | ACS medicinal chemistry letters, Sep-10, Volume: 11, Issue:9
| Quinoline-Pyrazole Scaffold as a Novel Ligand of Galectin-3 and Suppressor of TREM2 Signaling. |
AID705190 | Selectivity ratio of IC50 for PDE9 to IC50 for PDE10A | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Current landscape of phosphodiesterase 10A (PDE10A) inhibition. |
AID442317 | Binding affinity to PDE9A | 2009 | Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
| Identification of a brain penetrant PDE9A inhibitor utilizing prospective design and chemical enablement as a rapid lead optimization strategy. |
AID428628 | Increase in cGMP level in sc dosed mouse striatum | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
| Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia. |
AID1724765 | Antiinflammatory activity in mouse BV-2 cells assessed as reduction in Abeta-induced TNFalpha release at 10 uM incubated for 12 hrs by ELISA relative to control | 2020 | ACS medicinal chemistry letters, Sep-10, Volume: 11, Issue:9
| Quinoline-Pyrazole Scaffold as a Novel Ligand of Galectin-3 and Suppressor of TREM2 Signaling. |
AID705199 | Inhibition of PDE10A | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Current landscape of phosphodiesterase 10A (PDE10A) inhibition. |
AID715547 | Selectivity ratio of Ki for human PDE9A to Ki for human PDE10A | 2012 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18
| Discovery of tetrahydropyridopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia. |
AID428648 | Half life in Beagle dog at 0.3 mg/kg, iv | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
| Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia. |
AID1141266 | Ex vivo PDE10A receptor occupancy in po dosed Wistar rat striatum assessed as inhibition of [3H]-MP10 binding after 1 hr by autoradiography | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of a potent, selective, and orally active phosphodiesterase 10A inhibitor for the potential treatment of schizophrenia. |
AID767804 | Antipsychotic activity in rat assessed as inhibition of amphetamine-stimulated locomotor activity | 2013 | Bioorganic & medicinal chemistry, Oct-01, Volume: 21, Issue:19
| N-Methylanilide and N-methylbenzamide derivatives as phosphodiesterase 10A (PDE10A) inhibitors. |
AID628043 | Inhibition of rat recombinant PDE10A expressed in baculovirus infected insect Sf9 cells using [3H]cAMP as substrate after 60 mins by scintillation counting | 2011 | Journal of medicinal chemistry, Aug-25, Volume: 54, Issue:16
| Synthesis, in vivo occupancy, and radiolabeling of potent phosphodiesterase subtype-10 inhibitors as candidates for positron emission tomography imaging. |
AID767807 | Intrinsic clearance in rat liver microsomes | 2013 | Bioorganic & medicinal chemistry, Oct-01, Volume: 21, Issue:19
| N-Methylanilide and N-methylbenzamide derivatives as phosphodiesterase 10A (PDE10A) inhibitors. |
AID1557548 | Inhibition of PDE10 in PDGF-BB-induced human pulmonary artery smooth muscle cells assessed as reduction in proliferating cell nuclear antigen at 0.1 to 1 uM after 22 hrs by Western blot analysis | 2019 | Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
| Validation of Phosphodiesterase-10 as a Novel Target for Pulmonary Arterial Hypertension via Highly Selective and Subnanomolar Inhibitors. |
AID428637 | Metabolic stability in human liver microsome assessed as intrinsic clearance | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
| Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia. |
AID615725 | Selectivity ratio of IC50 for rat PDE10A to IC50 for rat PDE3B | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| Synthesis and in vitro evaluation of new analogues as inhibitors for phosphodiesterase 10A. |
AID428645 | Volume of distribution at steady state in cynomolgus monkey at 0.03 mg/kg, iv | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
| Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia. |
AID428630 | Inhibition of rat recombinant PDE10A transfected in Sf9 cells | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
| Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia. |
AID715550 | Selectivity ratio of Ki for human PDE6A to Ki for human PDE10A | 2012 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18
| Discovery of tetrahydropyridopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia. |
AID1724761 | Binding affinity to recombinant human galectin 3 assessed as dissociation constant by SPR assay | 2020 | ACS medicinal chemistry letters, Sep-10, Volume: 11, Issue:9
| Quinoline-Pyrazole Scaffold as a Novel Ligand of Galectin-3 and Suppressor of TREM2 Signaling. |
AID1140351 | Inhibition of N-terminal GST-tagged human recombinant PDE10A assessed as substrate hydrolysis using [3H]cAMP as substrate after 30 mins by two-step radiometric assay | 2014 | Bioorganic & medicinal chemistry letters, May-01, Volume: 24, Issue:9
| Design, synthesis and pharmacological evaluation of novel polycyclic heteroarene ethers as PDE10A inhibitors: Part I. |
AID428636 | Efflux ratio of permeability from basolateral to apical side over apical to basolateral side in MDR1 overexpressing MDCK cells | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
| Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia. |
AID715555 | Selectivity ratio of Ki for human PDE1A to Ki for human PDE10A | 2012 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18
| Discovery of tetrahydropyridopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia. |
AID428634 | Behavioral effect in sc dosed mouse assessed as conditioned avoidance response after 30 mins | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
| Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia. |
AID428656 | Behavioral effect in sc dosed PDE10A knockout mouse assessed as conditioned avoidance response after 30 mins | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
| Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia. |
AID705189 | Selectivity ratio of IC50 for PDE11 to IC50 for PDE10A | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Current landscape of phosphodiesterase 10A (PDE10A) inhibition. |
AID428638 | Increase in cGMP level in mouse striatum at 1 mg/kg, sc relative to control | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
| Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia. |
AID428653 | Oral bioavailability in cynomolgus monkey rat at 3 mg/kg, po | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
| Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia. |
AID428629 | Half life in Beagle dog at 3 mg/kg, po | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
| Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia. |
AID767814 | Inhibition of PDE10A (unknown origin) | 2013 | Bioorganic & medicinal chemistry, Oct-01, Volume: 21, Issue:19
| N-Methylanilide and N-methylbenzamide derivatives as phosphodiesterase 10A (PDE10A) inhibitors. |
AID428643 | Volume of distribution at steady state in Sprague-Dawley rat at 0.1 mg/kg, iv | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
| Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia. |
AID1557506 | Inhibition of human PDE10A2 catalytic domain (446 to 789 residues) expressed in Escherichia coli BL21 cells using [3H]-cGMP as substrate after 15 mins by liquid scintillation analysis | 2019 | Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
| Validation of Phosphodiesterase-10 as a Novel Target for Pulmonary Arterial Hypertension via Highly Selective and Subnanomolar Inhibitors. |
AID1872562 | Inhibition of PDE10 (unknown origin) | 2022 | European journal of medicinal chemistry, Mar-15, Volume: 232 | Therapeutic potential of phosphodiesterase inhibitors for cognitive amelioration in Alzheimer's disease. |
AID1724767 | Inhibition of galectin 3 in mouse BWZ cells transfected with TREM2 and DAP12 assessed as reduction in lacZ activity incubated for 24 hrs by lacZ reporter gene based beta-galactosidase assay | 2020 | ACS medicinal chemistry letters, Sep-10, Volume: 11, Issue:9
| Quinoline-Pyrazole Scaffold as a Novel Ligand of Galectin-3 and Suppressor of TREM2 Signaling. |
AID705193 | Selectivity ratio of IC50 for PDE5 to IC50 for PDE10A | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Current landscape of phosphodiesterase 10A (PDE10A) inhibition. |
AID1141264 | Antipsychotic activity in sc dosed Wiga rat assessed as reversal of apomorphine-induced stereotypy treated 30 mins prior to apomorphine challenge measured every 5 mins over first hour after apomorphine injection | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of a potent, selective, and orally active phosphodiesterase 10A inhibitor for the potential treatment of schizophrenia. |
AID715552 | Selectivity ratio of Ki for human PDE4A to Ki for human PDE10A | 2012 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18
| Discovery of tetrahydropyridopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia. |
AID715551 | Selectivity ratio of Ki for human PDE5A to Ki for human PDE10A | 2012 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18
| Discovery of tetrahydropyridopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia. |
AID428649 | Half life in Beagle dog at 0.1 mg/kg, po | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
| Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia. |
AID428655 | Unbound fraction in mouse plasma | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
| Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia. |
AID1557569 | Inhibition of PDE10 in PDGF-BB-induced human pulmonary artery smooth muscle cells assessed as increase in alpha-SMA expression at 0.1 to 1 uM after 22 hrs by Western blot analysis | 2019 | Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
| Validation of Phosphodiesterase-10 as a Novel Target for Pulmonary Arterial Hypertension via Highly Selective and Subnanomolar Inhibitors. |
AID428652 | Oral bioavailability in Beagle dog at 0.1 mg/kg, po | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
| Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia. |
AID715548 | Selectivity ratio of Ki for human PDE8A to Ki for human PDE10A | 2012 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18
| Discovery of tetrahydropyridopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia. |
AID428640 | Hepatic clearance in Sprague-Dawley rat at 0.1 mg/kg, iv | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
| Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia. |
AID705196 | Selectivity ratio of IC50 for PDE2 to IC50 for PDE10A | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Current landscape of phosphodiesterase 10A (PDE10A) inhibition. |
AID1724760 | Binding affinity to recombinant human galectin 1 assessed as dissociation constant by fluorescent anisotropy assay | 2020 | ACS medicinal chemistry letters, Sep-10, Volume: 11, Issue:9
| Quinoline-Pyrazole Scaffold as a Novel Ligand of Galectin-3 and Suppressor of TREM2 Signaling. |
AID1141267 | Plasma protein binding in Sprague-Dawley rat at 5 uM after 4.5 hrs | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of a potent, selective, and orally active phosphodiesterase 10A inhibitor for the potential treatment of schizophrenia. |
AID1724758 | Inhibition of recombinant human galectin-3/recombinant human TREM2 interaction assessed as reduction in TR-FRET signal incubated for 3 hrs by TR-FRET assay | 2020 | ACS medicinal chemistry letters, Sep-10, Volume: 11, Issue:9
| Quinoline-Pyrazole Scaffold as a Novel Ligand of Galectin-3 and Suppressor of TREM2 Signaling. |
AID1181667 | Antipsychotic activity in Sprague-Dawley rat conditioned avoidance response model assessed as reversal of MK-801-induced stereotypy at 3 mg/kg, ip administered 2 hrs prior to MK-801 challenge measured every 5 mins for 1 hr starting 15 mins post MK-801 inj | 2014 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15
| Design, synthesis and pharmacological evaluation of novel polycyclic heteroarene ethers as PDE10A inhibitors: part II. |
AID705197 | Selectivity ratio of IC50 for PDE3 to IC50 for PDE10A | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Current landscape of phosphodiesterase 10A (PDE10A) inhibition. |
AID1140226 | Inhibition of full-length human recombinant PDE10A using cyclic AMP as substrate by scintillation proximity assay | 2014 | Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9
| Radiosyntheses and in vivo evaluation of carbon-11 PET tracers for PDE10A in the brain of rodent and nonhuman primate. |
AID715554 | Selectivity ratio of Ki for human PDE2A to Ki for human PDE10A | 2012 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18
| Discovery of tetrahydropyridopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia. |
AID1141268 | Protein binding in Sprague-Dawley rat brain at 5 uM after 5 hrs | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of a potent, selective, and orally active phosphodiesterase 10A inhibitor for the potential treatment of schizophrenia. |
AID1181668 | Antipsychotic activity in Sprague-Dawley rat conditioned avoidance response model assessed as reversal of MK-801-induced ataxia at 3 mg/kg, ip administered 2 hrs prior to MK-801 challenge measured every 5 mins for 1 hr starting 15 mins post MK-801 injecti | 2014 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15
| Design, synthesis and pharmacological evaluation of novel polycyclic heteroarene ethers as PDE10A inhibitors: part II. |
AID428647 | Half life in Sprague-Dawley rat at 1 mg/kg, po | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
| Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia. |
AID428639 | Increase in cGMP level in mouse striatum at 3.2 mg/kg, sc relative to control | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
| Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia. |
AID1181666 | Antipsychotic activity in Sprague-Dawley rat conditioned avoidance response model assessed as reversal of MK-801-induced locomotion at 3 mg/kg, ip administered 2 hrs prior to MK-801 challenge measured every 5 mins for 1 hr starting 15 mins post MK-801 inj | 2014 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15
| Design, synthesis and pharmacological evaluation of novel polycyclic heteroarene ethers as PDE10A inhibitors: part II. |
AID1181683 | Antipsychotic activity in Sprague-Dawley rat conditioned avoidance response model assessed as avoidance of shock at 3 mg/kg, ip measured after 30 mins relative to vehicle-treated control | 2014 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15
| Design, synthesis and pharmacological evaluation of novel polycyclic heteroarene ethers as PDE10A inhibitors: part II. |
AID428646 | Half life in Sprague-Dawley rat at 0.1 mg/kg, iv | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
| Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia. |
AID428641 | Hepatic clearance in Beagle dog at 0.3 mg/kg, iv | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
| Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia. |
AID1557570 | Inhibition of PDE10 in PDGF-BB-induced human pulmonary artery smooth muscle cells assessed as increase in SM22alpha expression at 0.1 to 1 uM after 22 hrs by Western blot analysis | 2019 | Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
| Validation of Phosphodiesterase-10 as a Novel Target for Pulmonary Arterial Hypertension via Highly Selective and Subnanomolar Inhibitors. |
AID598564 | Inhibition of PDE10A | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
| Triazoloquinazolines as a novel class of phosphodiesterase 10A (PDE10A) inhibitors. |
AID705191 | Selectivity ratio of IC50 for PDE8 to IC50 for PDE10A | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Current landscape of phosphodiesterase 10A (PDE10A) inhibition. |
AID715553 | Selectivity ratio of Ki for human PDE3A to Ki for human PDE10A | 2012 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18
| Discovery of tetrahydropyridopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia. |
AID1141258 | Antipsychotic activity in sc dosed Wiga rat assessed as reversal of phencyclidine-induced hyperlocomotion administered 60 mins prior to PCP challenge measured for 30 mins | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of a potent, selective, and orally active phosphodiesterase 10A inhibitor for the potential treatment of schizophrenia. |
AID1235026 | Intrinsic clearance in rat liver microsomes | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
| BN/CC isosterism in borazaronaphthalenes towards phosphodiesterase 10A (PDE10A) inhibitors. |
AID615722 | Selectivity ratio of IC50 for rat PDE10A to IC50 for rat PDE3A | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| Synthesis and in vitro evaluation of new analogues as inhibitors for phosphodiesterase 10A. |
AID1267480 | Aqueous solubility of the compound at pH 7 | 2016 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 26, Issue:1
| Discovery of pyrazolopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia. |
AID705194 | Selectivity ratio of IC50 for PDE6 to IC50 for PDE10A | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Current landscape of phosphodiesterase 10A (PDE10A) inhibition. |
AID1724763 | Antiinflammatory activity in mouse BV-2 cells assessed as reduction in Abeta-induced IL-12 release incubated for 12 hrs by ELISA | 2020 | ACS medicinal chemistry letters, Sep-10, Volume: 11, Issue:9
| Quinoline-Pyrazole Scaffold as a Novel Ligand of Galectin-3 and Suppressor of TREM2 Signaling. |
AID484805 | Inhibition of human recombinant PDE10A expressed in baculovirus-SF21 cell system assessed as hydrolysis of [3H]cAMP after 1 hr by liquid scintillation counting | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
| Discovery of imidazo[1,5-a]pyrido[3,2-e]pyrazines as a new class of phosphodiesterase 10A inhibitiors. |
AID1141259 | Inhibition of rat recombinant PDE10A expressed in baculovirus infected Sf9 cells using [3H]cAMP as substrate after 60 mins by TopCount scintillation counting analysis | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of a potent, selective, and orally active phosphodiesterase 10A inhibitor for the potential treatment of schizophrenia. |
AID705192 | Selectivity ratio of IC50 for PDE7 to IC50 for PDE10A | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Current landscape of phosphodiesterase 10A (PDE10A) inhibition. |
AID1724757 | Inhibition of recombinant human galectin-3/recombinant human TREM2 interaction assessed as reduction in TR-FRET signal at 10 uM incubated for 3 hrs by TR-FRET assay relative to control | 2020 | ACS medicinal chemistry letters, Sep-10, Volume: 11, Issue:9
| Quinoline-Pyrazole Scaffold as a Novel Ligand of Galectin-3 and Suppressor of TREM2 Signaling. |
AID1557547 | Inhibition of PDE10 in PDGF-BB-induced human pulmonary artery smooth muscle cells assessed as reduction in osteopontin expression at 0.1 to 1 uM after 22 hrs by Western blot analysis | 2019 | Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
| Validation of Phosphodiesterase-10 as a Novel Target for Pulmonary Arterial Hypertension via Highly Selective and Subnanomolar Inhibitors. |
AID428651 | Oral bioavailability in Sprague-Dawley rat at 1 mg/kg, po | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
| Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia. |
AID615723 | Lipophilicity, log D of the compound | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| Synthesis and in vitro evaluation of new analogues as inhibitors for phosphodiesterase 10A. |
AID705198 | Selectivity ratio of IC50 for PDE1 to IC50 for PDE10A | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Current landscape of phosphodiesterase 10A (PDE10A) inhibition. |
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. |
AID1347411 | qHTS 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) Libary | 2020 | ACS 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. |
AID1345255 | Human phosphodiesterase 10A (Phosphodiesterases, 3',5'-cyclic nucleotide (PDEs)) | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
| Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia. |
AID1799159 | PDE Enzyme Inhibition Assay from Article 10.1021/jm900521k: \\Discovery of a Novel Class of Phosphodiesterase 10A Inhibitors and Identification of Clinical Candidate 2-[4-(1-Methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for t | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
| Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia. |
AID977608 | Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
| Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |