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Assay Detail

CHEMBL1067804

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Binding
Inhibition of p38alpha
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Design and synthesis of piperazine-indole p38 alpha MAP kinase inhibitors with improved pharmacokinetic profiles.
Tan X, Tester RW, Luedtke GR, Chakravarty S, Mavunkel BJ, Perumattam JJ, Lu Q, Nashashibi I, Jung J, Hu J, Liclican A, Almirez R, Tabora J, Tran V, Laney M, Levy DE, Dugar S.
Bioorg Med Chem Lett (2010) 20 : 828 -831
PubMed 20071169 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.61 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL605134 1 8.22
CHEMBL514201 TALMAPIMOD 2.0 1 8.05
CHEMBL591217 1 8.05
CHEMBL600470 1 7.62
CHEMBL600583 1 7.54
CHEMBL601666 1 7.33
CHEMBL605790 1 7.32
CHEMBL601452 1 6.74

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL605134 IC50 = 6.0 nM 8.22
CHEMBL514201 TALMAPIMOD IC50 = 9.0 nM 8.05
CHEMBL591217 IC50 = 9.0 nM 8.05
CHEMBL600470 IC50 = 24.0 nM 7.62
CHEMBL600583 IC50 = 29.0 nM 7.54
CHEMBL601666 IC50 = 47.0 nM 7.33
CHEMBL605790 IC50 = 48.0 nM 7.32
CHEMBL601452 IC50 = 183.0 nM 6.74