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Assay Detail

CHEMBL756829

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Functional
Inhibition of LPS-stimulated TNF-alpha release from human peripheral blood mononuclear cells
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type PBMC
Confidence 1 — Organism
Curated By Expert

Target

PBMC (CHEMBL613107)
Type CELL-LINE
Organism Homo sapiens

Publication

SAR of 2,6-diamino-3,5-difluoropyridinyl substituted heterocycles as novel p38MAP kinase inhibitors.
Revesz L, Di Padova FE, Buhl T, Feifel R, Gram H, Hiestand P, Manning U, Wolf R, Zimmerlin AG.
Bioorg Med Chem Lett (2002) 12 : 2109 -2112
PubMed 12127515 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.06 7.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL304523 1 7.75
CHEMBL66600 1 7.57
CHEMBL65541 1 7.51
CHEMBL63983 1 7.36
CHEMBL306667 1 7.36
CHEMBL304416 1 7.27
CHEMBL63442 1 7.13
CHEMBL66601 1 6.53
CHEMBL307336 1 6.43
CHEMBL291834 1 5.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL304523 IC50 = 18.0 nM 7.75
CHEMBL66600 IC50 = 27.0 nM 7.57
CHEMBL65541 IC50 = 31.0 nM 7.51
CHEMBL63983 IC50 = 44.0 nM 7.36
CHEMBL306667 IC50 = 44.0 nM 7.36
CHEMBL304416 IC50 = 54.0 nM 7.27
CHEMBL63442 IC50 = 74.0 nM 7.13
CHEMBL66601 IC50 = 294.0 nM 6.53
CHEMBL307336 IC50 = 373.0 nM 6.43
CHEMBL291834 IC50 = 1930.0 nM 5.71