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Assay Detail

CHEMBL1027395

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

Binding
Inhibition of human recombinant MK2 expressed in Escherichia coli BL21(DE3) after 60 mins
4
Total Activities
4
Compounds Tested
1
Activity Types
0
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 2 (CHEMBL2208)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Multiple and single binding modes of fragment-like kinase inhibitors revealed by molecular modeling, residue type-selective protonation, and nuclear overhauser effects.
Constantine KL, Mueller L, Metzler WJ, McDonnell PA, Todderud G, Goldfarb V, Fan Y, Newitt JA, Kiefer SE, Gao M, Tortolani D, Vaccaro W, Tokarski J.
J Med Chem (2008) 51 : 6225 -6229
PubMed 18771253 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.48 8.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL226403 1 8.07
CHEMBL510545 1 7.31
CHEMBL57481 1 4.07
CHEMBL122617 1-NAPHTHOL 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL226403 IC50 = 8.5 nM 8.07
CHEMBL510545 IC50 = 49.0 nM 7.31
CHEMBL57481 IC50 = 85000.0 nM 4.07
CHEMBL122617 1-NAPHTHOL IC50 > 100000.0 nM -