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Assay Detail

CHEMBL732631

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

Functional
Inhibition of p38 kinase related TNF-alpha release
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

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

Publication

p38 Inhibitors: piperidine- and 4-aminopiperidine-substituted naphthyridinones, quinolinones, and dihydroquinazolinones.
Hunt JA, Kallashi F, Ruzek RD, Sinclair PJ, Ita I, McCormick SX, Pivnichny JV, Hop CE, Kumar S, Wang Z, O'Keefe SJ, O'Neill EA, Porter G, Thompson JE, Woods A, Zaller DM, Doherty JB.
Bioorg Med Chem Lett (2003) 13 : 467 -470
PubMed 12565952 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 7.72 8.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL356754 1 8.31
CHEMBL356125 1 8.26
CHEMBL328242 1 8.25
CHEMBL343682 1 8.00
CHEMBL358108 1 7.89
CHEMBL357598 1 7.75
CHEMBL142187 1 7.70
CHEMBL142697 1 7.62
CHEMBL142289 1 7.62
CHEMBL142050 1 7.51
CHEMBL327987 1 7.44
CHEMBL142463 1 7.29
CHEMBL356994 1 6.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL356754 IC50 = 4.9 nM 8.31
CHEMBL356125 IC50 = 5.5 nM 8.26
CHEMBL328242 IC50 = 5.6 nM 8.25
CHEMBL343682 IC50 = 10.0 nM 8.00
CHEMBL358108 IC50 = 13.0 nM 7.89
CHEMBL357598 IC50 = 18.0 nM 7.75
CHEMBL142187 IC50 = 20.0 nM 7.70
CHEMBL142697 IC50 = 24.0 nM 7.62
CHEMBL142289 IC50 = 24.0 nM 7.62
CHEMBL142050 IC50 = 31.0 nM 7.51
CHEMBL327987 IC50 = 36.0 nM 7.44
CHEMBL142463 IC50 = 51.0 nM 7.29
CHEMBL356994 IC50 = 200.0 nM 6.70