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Assay Detail

CHEMBL1114528

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

Binding
Inhibition of human recombinant p38alpha by liquid scintillation counting
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

Mitogen-activated protein kinase 14 (CHEMBL260)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Selective p38alpha inhibitors clinically evaluated for the treatment of chronic inflammatory disorders.
Goldstein DM, Kuglstatter A, Lou Y, Soth MJ.
J Med Chem (2010) 53 : 2345 -2353
PubMed 19950901 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 8.06 8.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1088750 ARRY-797 3.0 1 8.35
CHEMBL514201 TALMAPIMOD 2.0 1 8.05
CHEMBL119385 NEFLAMAPIMOD 2.0 1 8.00
CHEMBL1090089 PAMAPIMOD 2.0 1 7.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1088750 ARRY-797 IC50 = 4.5 nM 8.35
CHEMBL514201 TALMAPIMOD IC50 = 9.0 nM 8.05
CHEMBL119385 NEFLAMAPIMOD IC50 = 10.0 nM 8.00
CHEMBL1090089 PAMAPIMOD IC50 = 14.0 nM 7.85