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Literature summary for 2.7.11.24 extracted from

  • Zaman, G.J.; van der Lee, M.M.; Kok, J.J.; Nelissen, R.L.; Loomans, E.E.
    Enzyme fragment complementation binding assay for p38alpha mitogen-activated protein kinase to study the binding kinetics of enzyme inhibitors (2006), Assay Drug Dev. Technol., 4, 411-420.
    View publication on PubMed
Search for more literature for 2.7.11.24

Application

Application Comment Organism
analysis HitHunter EFC binding assay can be used to select compounds that specifically target inactive kinase Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
BIRB 796 no preference for either active or inactive p38alpha, slow association kinetics of BIRB 796 as compared to SB 203580, corresponding with the requirement of a relatively long preincubation time to obtain maximal effect in a cellular assay Homo sapiens
SB 203580 no preference for either active or inactive p38alpha, no preincubation required to achieve maximum inhibition Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
THP-1 cell
-
 Homo sapiens
-

Synonyms

Synonyms Comment Organism
p38alpha mitogen-activated protein kinase
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000011
-
 EFC binding assay with active P38alpha Homo sapiens BIRB 796
0.000011
-
 EFC binding assay with inactive P38alpha Homo sapiens BIRB 796
0.000057
-
 in cell-based assay measuring LPS-induced TNFalpha secretion Homo sapiens BIRB 796
0.000079
-
 IMAP enzyme activity assay Homo sapiens BIRB 796
0.00008
-
 EFC binding assay with active P38alpha Homo sapiens SB 203580
0.000083
-
 IMAP enzyme activity assay Homo sapiens SB 203580
0.0001
-
 EFC binding assay with inactive P38alpha Homo sapiens SB 203580
0.00015
-
 in cell-based assay measuring LPS-induced TNFalpha secretion Homo sapiens SB 203580