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Assay Detail

CHEMBL820595

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

Functional
Tested for inhibition of Tumor necrosis factor, alpha in THP cells
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type THP
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Tumor necrosis factor (CHEMBL1825)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-activity relationships of the p38alpha MAP kinase inhibitor 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)naph- thalen-1-yl]urea (BIRB 796).
Regan J, Capolino A, Cirillo PF, Gilmore T, Graham AG, Hickey E, Kroe RR, Madwed J, Moriak M, Nelson R, Pargellis CA, Swinamer A, Torcellini C, Tsang M, Moss N.
J Med Chem (2003) 46 : 4676 -4686
PubMed 14561087 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 10 7.72 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL344625 1 8.05
CHEMBL318810 1 8.05
CHEMBL344800 1 7.96
CHEMBL143886 1 7.80
CHEMBL103667 DORAMAPIMOD 2.0 1 7.75
CHEMBL104991 1 7.72
CHEMBL143134 1 7.70
CHEMBL336001 1 7.44
CHEMBL143373 1 7.38
CHEMBL142115 1 7.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL344625 EC50 = 9.0 nM 8.05
CHEMBL318810 EC50 = 9.0 nM 8.05
CHEMBL344800 EC50 = 11.0 nM 7.96
CHEMBL143886 EC50 = 16.0 nM 7.80
CHEMBL103667 DORAMAPIMOD EC50 = 18.0 nM 7.75
CHEMBL104991 EC50 = 19.0 nM 7.72
CHEMBL143134 EC50 = 20.0 nM 7.70
CHEMBL336001 EC50 = 36.0 nM 7.44
CHEMBL143373 EC50 = 42.0 nM 7.38
CHEMBL142115 EC50 = 50.0 nM 7.30