| Assay Method Information | |
| | Concentration Response fluorescence polarization-based assay to confirm small molecule inhibitors identified in the Polo box domain (PBD) of Plk1 Primary HTS. |
| Description: | List of compounds to be tested: Compounds that met the active criterion of Z-score is </= -3 in the in vitro PLK1-PBD binding primary screen AID 693, will be confirmed in 10-point concentration response assays. Extracted from the MH078944 proposal submitted by Dr. Michael Yaffe of MIT. The Polo-like kinases (Plks) play important roles in many cell cycle-related events including the initiation of mitosis, chromosome segregation, centrosome maturation, bipolar spindle formation, regulation of anaphase-promoting complex and execution of cytokinesis. The prototypic Polo kinase was originally identified in flies, in which mutants resulted in abnormal spindle poles. A single Polo family member is found in flies, budding yeast, and fission yeast (Polo, CDC5 and Plo1, respectively), while 3 Plk family members are found in humans, mice and frogs (Plk1/Plx1, Plk2/Snk/Plx2 and Plk3/Fnk/Prk/Plx3 respectively). One human family member, Plk1, as well as its homologues in Xenopus (Plx1) and buddi |
| Affinity data for this assay | |
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