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Assay Detail

CHEMBL987301

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

Binding
Inhibition of p38alpha phosphorylation in IL-1-alpha-stimulated HLF cells
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Biphenyl amide p38 kinase inhibitors 4: DFG-in and DFG-out binding modes.
Angell RM, Angell TD, Bamborough P, Bamford MJ, Chung CW, Cockerill SG, Flack SS, Jones KL, Laine DI, Longstaff T, Ludbrook S, Pearson R, Smith KJ, Smee PA, Somers DO, Walker AL.
Bioorg Med Chem Lett (2008) 18 : 4433 -4437
PubMed 18602262 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.78 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL476141 1 8.70
CHEMBL476351 GW775608X 1 8.22
CHEMBL477583 GW743024X 1 7.80
CHEMBL478649 1 7.75
CHEMBL103667 DORAMAPIMOD 2.0 1 7.33
CHEMBL95692 SB-242235 1 6.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL476141 IC50 = 2.0 nM 8.70
CHEMBL476351 GW775608X IC50 = 6.0 nM 8.22
CHEMBL477583 GW743024X IC50 = 16.0 nM 7.80
CHEMBL478649 IC50 = 18.0 nM 7.75
CHEMBL103667 DORAMAPIMOD IC50 = 47.0 nM 7.33
CHEMBL95692 SB-242235 IC50 = 130.0 nM 6.89