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Assay Detail

CHEMBL2405975

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

Binding
Inhibition of p38 MAPK-mediated TNFalpha production in LPS-induced human whole blood preincubated for 5 mins prior to LPS-treatment measured after 6 hrs by ELISA
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Tissue Blood
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

MAP kinase p38 (CHEMBL2094115)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

The identification of novel p38α isoform selective kinase inhibitors having an unprecedented p38α binding mode.
Wrobleski ST, Lin S, Dhar TG, Dyckman AJ, Li T, Pitt S, Zhang R, Fan Y, Doweyko AM, Tokarski JS, Kish KF, Kiefer SE, Sack JS, Newitt JA, Witmer MR, McKinnon M, Barrish JC, Dodd JH, Schieven GL, Leftheris K.
Bioorg Med Chem Lett (2013) 23 : 4120 -4126
PubMed 23746475 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 8.54 9.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2402001 1 9.14
CHEMBL2401997 1 8.77
CHEMBL2401999 1 8.22
CHEMBL2401998 1 8.02
CHEMBL2402000 1 -
CHEMBL2401996 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2402001 IC50 = 0.72 nM 9.14
CHEMBL2401997 IC50 = 1.7 nM 8.77
CHEMBL2401999 IC50 = 6.0 nM 8.22
CHEMBL2401998 IC50 = 9.6 nM 8.02
CHEMBL2402000 IC50 - -
CHEMBL2401996 IC50 - -