5 Matching Annotations
  1. Sep 2021
  2. www.ncbi.nlm.nih.gov www.ncbi.nlm.nih.gov
    PAINS in the Assay: Chemical Mechanisms of Assay Interference and Promiscuous Enzymatic Inhibition Observed during a Sulfhydryl-Scavenging HTS
    1
    1. zhentg 19 Sep 2021

      this paper described some hit compounds that interfere with the assay components. some compounds react with thiol, and their SAR is reported.

      PAINS covalent warhead
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    ncbi.nlm.nih.gov/pmc/articles/PMC4360378/
  3. Nov 2020
  4. www.scripps.edu www.scripps.edu
    The Cravatt Lab
    1
    1. zhentg 13 Nov 2020
      Journal of the American Chemical Society. 2018, 140, 8069-8073.

      covalent warhead

      covalent warhead
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    scripps.edu/cravatt/refs.html
  5. Aug 2020
  6. Local file Local file
    Fragment screening for a protein-protein interaction inhibitor to WDR5
    1
    1. zhentg 21 Aug 2020
      however, there was noevidence of covalent bonding to the protein.

      this result is similar to CNIBR result, thus it is important to assess the cysteine reactivity before any MedChem efforts.

      covalent cysteine

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  7. Jun 2020
  8. Local file Local file
    10.1172@JCI66398.pdf
    1
    1. zhentg 17 Jun 2020
      SDS-PAGE disrupts noncovalent interactions and is used to determine covalent binding.

      SDS-PAGE is used to identify covalent binder with the help of click chemistry

      covalent

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  9. Mar 2020
  10. pubs.acs.org pubs.acs.org
    ja9b02822 1..18
    1
    1. zhentg 27 Mar 2020

      covalent fragment screening

      covalent fragment screening
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    pubs.acs.org/doi/pdf/10.1021/jacs.9b02822