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Assay Detail

CHEMBL863945

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

Functional
Inhibition of TNF alpha release in THP1 cells
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type THP-1
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

p38 MAP kinase inhibitors: metabolically stabilized piperidine-substituted quinolinones and naphthyridinones.
Bao J, Hunt JA, Miao S, Rupprecht KM, Stelmach JE, Liu L, Ruzek RD, Sinclair PJ, Pivnichny JV, Hop CE, Kumar S, Zaller DM, Shoop WL, O'neill EA, O'keefe SJ, Thompson CM, Cubbon RM, Wang R, Zhang WX, Thompson JE, Doherty JB.
Bioorg Med Chem Lett (2006) 16 : 64 -68
PubMed 16242322 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 8.87 9.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL381632 1 9.57
CHEMBL199484 1 9.38
CHEMBL199625 1 9.16
CHEMBL199593 1 9.13
CHEMBL199435 1 9.11
CHEMBL200093 1 9.09
CHEMBL199701 1 9.05
CHEMBL199680 1 9.00
CHEMBL380806 1 9.00
CHEMBL199316 1 8.89
CHEMBL199291 1 8.80
CHEMBL199679 1 8.77
CHEMBL199707 1 8.74
CHEMBL200534 1 8.66
CHEMBL381201 1 8.62
CHEMBL199632 1 8.59
CHEMBL199565 1 8.49
CHEMBL369989 1 8.48
CHEMBL200047 1 8.43
CHEMBL200018 1 8.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL381632 IC50 = 0.27 nM 9.57
CHEMBL199484 IC50 = 0.42 nM 9.38
CHEMBL199625 IC50 = 0.69 nM 9.16
CHEMBL199593 IC50 = 0.74 nM 9.13
CHEMBL199435 IC50 = 0.77 nM 9.11
CHEMBL200093 IC50 = 0.82 nM 9.09
CHEMBL199701 IC50 = 0.89 nM 9.05
CHEMBL199680 IC50 = 1.0 nM 9.00
CHEMBL380806 IC50 = 0.99 nM 9.00
CHEMBL199316 IC50 = 1.3 nM 8.89
CHEMBL199291 IC50 = 1.6 nM 8.80
CHEMBL199679 IC50 = 1.7 nM 8.77
CHEMBL199707 IC50 = 1.8 nM 8.74
CHEMBL200534 IC50 = 2.2 nM 8.66
CHEMBL381201 IC50 = 2.4 nM 8.62
CHEMBL199632 IC50 = 2.59 nM 8.59
CHEMBL199565 IC50 = 3.2 nM 8.49
CHEMBL369989 IC50 = 3.32 nM 8.48
CHEMBL200047 IC50 = 3.75 nM 8.43
CHEMBL200018 IC50 = 3.8 nM 8.42