852714-76-2

Upstream product

• 641638-41-7 (2S,3S)-3-(4-{bis[(tert-butyl)oxycarbonyl]methyl}-phenyl)-2-{[(tert-butyl)oxycarbonyl]methyl}-pent-4-enoic acid 
• 666259-67-2 N-{(2R)-2-[(5-methylindol-1-yl)methyl]pent-4-enyl}(2S)-2-[(aminocyclohexyl)carbonylamino]-3-carbamoylpropanamide 

Downstream Products

• 852714-80-8 2-{4-[(E)-(9S,10S,14R,18S)-18-Carbamoylmethyl-9-carboxymethyl-14-(5-methyl-indol-1-ylmethyl)-8,17,20-trioxo-7,16,19-triaza-spiro[5.14]icos-11-en-10-yl]-phenyl}-malonic acid 
• 852714-78-4 di-tert-butyl 2-[4-((9S,10S,18S,14R)-7,16,19-triaza-9-{[(tert-butyl)oxycarbonyl]methyl}-18-(carbamoylmethyl)-14-[(5-methylindolyl)methyl]-8,17,20-trioxospiro[5.14]icos-11-en-10-yl)phenyl]propane-1,3-dioate 

Relevant academic research and scientific papers

Examination of phosphoryl-mimicking functionalities within a macrocyclic Grb2 SH2 domain-binding platform

Reported herein are the design, synthesis, and Grb2 SH2 domain-binding affinities of several phosphoryl-mimicking groups displayed within the context of a conformationally constrained macrocyclic platform. With use of surface plasmon resonance techniques, single-digit nanomolar affinities were exhibited by phosphonic acid and malonyl-containing diacidic phosphoryl mimetics (for 4h and 4g, KD = 1.47 and 3.62 nM, respectively). Analogues containing monoacidic phosphoryl mimetics provided affinities of KD = 16-67 nM. Neutral phosphoryl-mimicking groups did not show appreciable binding.