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. Author manuscript; available in PMC: 2010 Jan 12.

Published in final edited form as: Chembiochem. 2009 Aug 17;10(12):1955–1958. doi: 10.1002/cbic.200900079

A) Saturation-binding curve of HRP-labeled SCF (SCF*) binding to ELISA plates coated with the whole extracellular ligand-binding domain of KIT (K_D(app) = 16 nm). B) Competition-binding curves for the lead inhibitors (In.) P2 () and P3 (●); K_I(app) = 31 and 33 nm, respectively. C) Cell-based assays testing the efficiency of the lead compounds (IC₅₀ < 10 µm) to inhibit SCF-induced KIT phosphorylation. Four compounds (P1–3, C10) strongly inhibited cell stimulation; P2 completely abolished KIT phosphorylation (p-KIT).

Inline graphic — A) Saturation-binding curve of HRP-labeled SCF (SCF*) binding to ELISA plates coated with the whole extracellular ligand-binding domain of KIT (K_D(app) = 16 nm). B) Competition-binding curves for the lead inhibitors (In.) P2 () and P3 (●); K_I(app) = 31 and 33 nm, respectively. C) Cell-based assays testing the efficiency of the lead compounds (IC₅₀ < 10 µm) to inhibit SCF-induced KIT phosphorylation. Four compounds (P1–3, C10) strongly inhibited cell stimulation; P2 completely abolished KIT phosphorylation (p-KIT).