| Assay Method Information | |
| | MKP-3 in vitro secondary assay for identification of irreversible and slow-binding inhibitors |
| Description: | Data Source: Sanford-Burnham Center for Chemical Genomics (SBCCG) Source Affiliation: Sanford-Burnham Medical Research Institute(SBMRI, San Diego, CA) Network: NIH Molecular Libraries Screening Centers Network (MLSCN) Grant Number: XO1 MH076390-01 Assay Provider: Dr. John Lazo, University of Pittsburg This assay is designed as a counter-screen for the MKP-3 in vitro HTS assay (AID 425) aimed at identification of compounds with time-dependent behavior. MKP-3 (mitogen-activated protein kinase phosphatase-3; EC 3.1.3.48, EC 3.1.3.16), a dual specificity phosphatase negatively regulates ERK1/2 by catalyzing the removal of a phosphoryl group from Thr(P) and Tyr(P) in the activation loop consensus motif -pTXpY. MKP-3 has a labile cysteine in its active site that is crucial for the catalysis. As a result compounds capable of cysteine oxidation or modification are likely to appear as screening hits. The current biochemical assay is designed as a rapid diagnostic tool for identification of |
| Affinity data for this assay | |
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