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Assay Detail

CHEMBL701923

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

Functional
Inhibition of LPS-induced release of Tumor necrosis factor-alpha (TNF-alpha) from human whole blood
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Design and synthesis of potent, selective, and orally bioavailable tetrasubstituted imidazole inhibitors of p38 mitogen-activated protein kinase.
Liverton NJ, Butcher JW, Claiborne CF, Claremon DA, Libby BE, Nguyen KT, Pitzenberger SM, Selnick HG, Smith GR, Tebben A, Vacca JP, Varga SL, Agarwal L, Dancheck K, Forsyth AJ, Fletcher DS, Frantz B, Hanlon WA, Harper CF, Hofsess SJ, Kostura M, Lin J, Luell S, O'Neill EA, O'Keefe SJ.
J Med Chem (1999) 42 : 2180 -2190
PubMed 10377223 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 7.18 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL446404 1 9.40
CHEMBL303144 1 8.55
CHEMBL305178 1 8.37
CHEMBL308939 1 8.22
CHEMBL69331 1 7.47
CHEMBL307435 1 7.30
CHEMBL69764 1 6.76
CHEMBL424418 1 6.72
CHEMBL307980 1 6.54
CHEMBL67874 1 6.23
CHEMBL10 SB-203580 1 6.00
CHEMBL305749 1 4.62
CHEMBL302805 1 -
CHEMBL67633 1 -
CHEMBL302728 1 -
CHEMBL67658 1 -
CHEMBL63135 1 -
CHEMBL68572 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL446404 IC50 = 0.4 nM 9.40
CHEMBL303144 IC50 = 2.8 nM 8.55
CHEMBL305178 IC50 = 4.3 nM 8.37
CHEMBL308939 IC50 = 6.0 nM 8.22
CHEMBL69331 IC50 = 34.0 nM 7.47
CHEMBL307435 IC50 = 50.0 nM 7.30
CHEMBL69764 IC50 = 175.0 nM 6.76
CHEMBL424418 IC50 = 190.0 nM 6.72
CHEMBL307980 IC50 = 290.0 nM 6.54
CHEMBL67874 IC50 = 585.0 nM 6.23
CHEMBL10 SB-203580 IC50 = 1000.0 nM 6.00
CHEMBL305749 IC50 = 24000.0 nM 4.62
CHEMBL302805 IC50 > 100000.0 nM -
CHEMBL67633 IC50 > 100000.0 nM -
CHEMBL302728 IC50 > 100000.0 nM -
CHEMBL67658 IC50 > 100000.0 nM -
CHEMBL63135 IC50 > 10000.0 nM -
CHEMBL68572 IC50 > 100000.0 nM -