Forster, Michael; Liang, Xiaojun Julia; Schroeder, Martin; Gerstenecker, Stefan; Chaikuad, Apirat; Knapp, Stefan; Laufer, Stefan; Gehringer, Matthias published the artcile< Discovery of a novel class of covalent dual inhibitors targeting the protein kinases BMX and BTK>, Formula: C7H5N3O2, the main research area is phenyl pyrrolopyridine prepare kinase inhibitor mol docking SAR; Bruton’s tyrosine kinase; Janus kinase 3; bone marrow tyrosine kinase on chromosome X; chemical probes; covalent inhibitors; tyrosine kinases.
Here a novel class of dual BMX/BTK inhibitors, which were designed from irreversible inhibitors of Janus kinase (JAK) 3 targeting a cysteine located within the solvent-exposed front region of the ATP binding pocket was presented. Structure-guided design exploiting the differences in the gatekeeper residues enabled the achievement of high selectivity over JAK3 and certain other kinases harboring a sterically demanding residue at this position. The most active compounds inhibited BMX and BTK with apparent IC50 values in the single digit nanomolar range or below showing moderate selectivity within the TEC family and potent cellular target engagement. These compounds represent an important first step towards selective chem. probes for the protein kinase BMX.
International Journal of Molecular Sciencespublished new progress about Acid chlorides Role: RCT (Reactant), RACT (Reactant or Reagent). 101083-92-5 belongs to class indole-building-block, and the molecular formula is C7H5N3O2, Formula: C7H5N3O2.
Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles