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Assay Detail

CHEMBL5680491

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of recombinant PRAK (unknown origin) expressed in Escherichia coli using KKKALSRQLSVAA as substrate incubated for 1 hr followed by substrate addition in presence of ATP
1
Total Activities
1
Compounds Tested
1
Activity Types
2
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

MAP kinase-activated protein kinase 5 (CHEMBL3094)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A benzothiophene inhibitor of mitogen-activated protein kinase-activated protein kinase 2 inhibits tumor necrosis factor alpha production and has oral anti-inflammatory efficacy in acute and chronic models of inflammation.
Mourey RJ, Burnette BL, Brustkern SJ, Daniels JS, Hirsch JL, Hood WF, Meyers MJ, Mnich SJ, Pierce BS, Saabye MJ, Schindler JF, South SA, Webb EG, Zhang J, Anderson DR.
J Pharmacol Exp Ther (2010) 333 : 797 -807
PubMed 20237073 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.30 8.30

Assay Parameters

Parameter Type Value Units Text
EFO_ID EFO_ID - HP:0001370
EFO_TERM EFO_TERM - rheumatoid arthritis

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1231206 1 8.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1231206 IC50 = 5.0 nM 8.30