Displacement of [125I]-pyr-1-apelin-13 from rat C-terminal EGFP-tagged APJ receptor expressed in CHO cell membranes after 3 hrs by Wallac gamma counting
Substrate activity at KLKB1 in human plasma assessed as (S)-2-((S)-2-((S)-2,6-diaminohexanamido)-3-phenylpropanamido)-5-guanidinopentanoic acid formation at 400 uM measured after 10 to 30 mins by LC-MS analysis
Substrate activity at KLKB1 in human plasma assessed as (S)-2-(2-((S)-2-((S)-1-((6S,9S,12S,15S,18S)-15-((1H-imidazol-4-yl)methyl)-1-amino-18-(4-aminobutyl)-6-((S)-1-((S)-2-((S)-2,5-diamino-5-oxopentanamido)-5-guanidinopentanoyl)pyrrolidine-2-carboxamido)-12-(hydroxymethyl)-1-imino-9-isobutyl-7,10,13,16,19-pentaoxo-2,8,11,14,17,20-hexaazadocosane)pyrrolidine-2-carboxamido)hexanamido)-2-methylpropanamido)-3-(4-bromophenyl)propanoic acid formation at 400 uM measured after 10 to 30 mins by LC-MS analysis
Substrate activity at recombinant human NEP (Tyr52 to Trp750 residues) expressed in HEK293 cells assessed as enzyme-mediated degradation onset time at 1 mM by MALDI-TOF MS analysis
Substrate activity at recombinant human C-terminal His6-tagged KLKB1 (Pro19 to Ser262 residues) expressed in mammalian expression system assessed as enzyme-mediated degradation onset time at 1 mM by MALDI-TOF MS analysis
Substrate activity at recombinant human C-terminal His6-tagged KLKB1 (Pro19 to Ser262 residues) expressed in mammalian expression system assessed as Km measured after 30 to 60 mins by LC-MS analysis
Substrate activity at recombinant human C-terminal His6-tagged KLKB1 (Pro19 to Ser262 residues) expressed in mammalian expression system assessed as Kcat measured after 30 to 60 mins by LC-MS analysis
Substrate activity at recombinant human C-terminal His6-tagged KLKB1 (Pro19 to Ser262 residues) expressed in mammalian expression system assessed as ratio of Kcat to Km measured after 30 to 60 mins by LC-MS analysis
Substrate activity at recombinant human C-terminal His6-tagged KLKB1 (Pro19 to Ser262 residues) expressed in mammalian expression system assessed as Vmax measured after 30 to 60 mins by LC-MS analysis
Substrate activity at recombinant human C-terminal His6-tagged KLKB1 (Pro19 to Ser262 residues) expressed in mammalian expression system assessed as compound half life by LC-MS analysis