Fluorescent probes for use in protein kinase inhibitor...

Details Fluorescent probes for use in protein kinase inhibitor... Fluorescent probes for use in protein kinase inhibitor...

C - Chemistry, Metallurgy

07

D

C07D 405/12 (2006.01) G01N 33/542 (2006.01) G01N 33/58 (2006.01)

Patent

CA 2541059

The invention provides methods relating to a novel screening assay format that can be applied to broad members of the protein kinase gene family. The assay uses a series of labeled, active site probes described herein that can be displaced by an inhibitor agent. The Kd for the inhibitor compound is derived based on the Kd of the probe for the kinase and the dose response of the inhibitor agent. The invention also provides novel active site probes suitable for use with the screening method.

L'invention concerne des procédés relatifs à un format de test d'analyse pouvant être appliqué à une large gamme de membres de la famille des gènes de protéine kinase. On utilise une série de sondes de site actif marquées, décrites dans l'invention, pouvant être déplacées par un agent inhibiteur. Le K¿d? pour le composé inhibiteur est dérivé sur la base du K¿d? de la sonde pour la kinase et de la dose-réponse de l'agent inhibiteur. L'invention concerne également des sondes de site actif se prêtant à une utilisation dans le cadre du procédé considéré.

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