Showing 41 - 60 results of 30,321 for search '(((( 50 ng decrease ) OR ( 5 ((nn decrease) OR (we decrease)) ))) OR ( 5 nm decrease ))', query time: 0.71s Refine Results
  1. 41
  2. 42
  3. 43
  4. 44

    Discovery of the Triazolo[1,5‑<i>a</i>]Pyrimidine-Based Derivative WS-898 as a Highly Efficacious and Orally Bioavailable ABCB1 Inhibitor Capable of Overcoming Multidrug Resistance... by Shuai Wang (109515)

    Published 2021
    “…Targeting P-glycoprotein (ABCB1 or P-gp) has been recognized as a promising strategy to overcome multidrug resistance. Here, we reported our medicinal chemistry efforts that led to the discovery of the triazolo­[1,5-<i>a</i>]­pyrimidine derivative <b>WS-898</b> as a highly effective ABCB1 inhibitor capable of reversing paclitaxel (PTX) resistance in drug-resistant SW620/Ad300, KB-C2, and HEK293/ABCB1 cells (IC<sub>50</sub> = 5.0, 3.67, and 3.68 nM, respectively), more potent than verapamil and zosuquidar. …”
  5. 45

    Discovery of the Triazolo[1,5‑<i>a</i>]Pyrimidine-Based Derivative WS-898 as a Highly Efficacious and Orally Bioavailable ABCB1 Inhibitor Capable of Overcoming Multidrug Resistance... by Shuai Wang (109515)

    Published 2021
    “…Targeting P-glycoprotein (ABCB1 or P-gp) has been recognized as a promising strategy to overcome multidrug resistance. Here, we reported our medicinal chemistry efforts that led to the discovery of the triazolo­[1,5-<i>a</i>]­pyrimidine derivative <b>WS-898</b> as a highly effective ABCB1 inhibitor capable of reversing paclitaxel (PTX) resistance in drug-resistant SW620/Ad300, KB-C2, and HEK293/ABCB1 cells (IC<sub>50</sub> = 5.0, 3.67, and 3.68 nM, respectively), more potent than verapamil and zosuquidar. …”
  6. 46

    Structure-Based Design of a Chemical Probe Set for the 5‑HT<sub>5A</sub> Serotonin Receptor by Anat Levit Kaplan (12126567)

    Published 2022
    “…Docking over 6 million molecules against a 5-HT<sub>5A</sub>R homology model identified 5 mid-μM ligands, one of which was optimized to <b>UCSF678</b>, a 42 nM arrestin-biased partial agonist at the 5-HT<sub>5A</sub>R with a more restricted off-target profile and decreased assay liabilities versus SB-699551. …”
  7. 47

    Structure-Based Design of a Chemical Probe Set for the 5‑HT<sub>5A</sub> Serotonin Receptor by Anat Levit Kaplan (12126567)

    Published 2022
    “…Docking over 6 million molecules against a 5-HT<sub>5A</sub>R homology model identified 5 mid-μM ligands, one of which was optimized to <b>UCSF678</b>, a 42 nM arrestin-biased partial agonist at the 5-HT<sub>5A</sub>R with a more restricted off-target profile and decreased assay liabilities versus SB-699551. …”
  8. 48
  9. 49
  10. 50

    Structure–Activity Relationship of 3‑Methylcytidine-5′-α,β-methylenediphosphates as CD73 Inhibitors by Mirko Scortichini (4007366)

    Published 2022
    “…We now expand the structure–activity relationship of pyrimidine nucleotides as human CD73 inhibitors. 4-Chloro (MRS4598 <b>16</b>; <i>K</i><sub>i</sub> = 0.673 nM) and 4-iodo (MRS4620 <b>18</b>; <i>K</i><sub>i</sub> = 0.436 nM) substitution of the <i>N</i><sup>4</sup>-benzyloxy group decreased <i>K</i><sub>i</sub> by ∼20-fold. …”
  11. 51

    Structure–Activity Relationship of 3‑Methylcytidine-5′-α,β-methylenediphosphates as CD73 Inhibitors by Mirko Scortichini (4007366)

    Published 2022
    “…We now expand the structure–activity relationship of pyrimidine nucleotides as human CD73 inhibitors. 4-Chloro (MRS4598 <b>16</b>; <i>K</i><sub>i</sub> = 0.673 nM) and 4-iodo (MRS4620 <b>18</b>; <i>K</i><sub>i</sub> = 0.436 nM) substitution of the <i>N</i><sup>4</sup>-benzyloxy group decreased <i>K</i><sub>i</sub> by ∼20-fold. …”
  12. 52

    Structure–Activity Relationship of 3‑Methylcytidine-5′-α,β-methylenediphosphates as CD73 Inhibitors by Mirko Scortichini (4007366)

    Published 2022
    “…We now expand the structure–activity relationship of pyrimidine nucleotides as human CD73 inhibitors. 4-Chloro (MRS4598 <b>16</b>; <i>K</i><sub>i</sub> = 0.673 nM) and 4-iodo (MRS4620 <b>18</b>; <i>K</i><sub>i</sub> = 0.436 nM) substitution of the <i>N</i><sup>4</sup>-benzyloxy group decreased <i>K</i><sub>i</sub> by ∼20-fold. …”
  13. 53
  14. 54
  15. 55
  16. 56
  17. 57

    High resolution structures visible with the 25 nm zone plate objective. by Kamal L. Nahas (13014698)

    Published 2022
    “…(<b>F</b>) The width of nuclear capsids was remeasured after imaging with the 25 nm zone plate: 124.5 nm ± 0.96 nm SEM (n = 80 from 4 tomograms; 8.55 nm SD). …”
  18. 58
  19. 59
  20. 60