Assay Method Information | |
| ChEMBL_2066557 (CHEMBL4721810) |
Description: | Covalent binding affinity to KRAS G12C mutant at Cys12 residue in human NCI-H358 cells assessed as reduction of log2 H/L ratio for tryptic peptide LVVVGACGVGK incubated for 4 hrs followed by cell lysis and subsequently labelled with light thiol probe N-((S)-18-iodo-11-isopropyl-10,13,17-trioxo-3,6-dioxa-9,12,16-triazaoctadecyl)-6-((4R,5S)-5-methyl-2-oxoimidazolidin-4-yl)hexanamide and heavy thiol probe 4 for 1 hr under dark conditions followed by tryptic digestion for overnight and measured by ABPP target occupancy based UHPLC Q-SIM MS analysis |
Affinity data for this assay | |
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