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Assay Detail

CHEMBL860432

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

Functional
Inhibition of LPS-induced TNFalpha production in primary human monocytes
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Inhibition of Tpl2 kinase and TNF-alpha production with 1,7-naphthyridine-3-carbonitriles: synthesis and structure-activity relationships.
Gavrin LK, Green N, Hu Y, Janz K, Kaila N, Li HQ, Tam SY, Thomason JR, Gopalsamy A, Ciszewski G, Cuozzo JW, Hall JP, Hsu S, Telliez JB, Lin LL.
Bioorg Med Chem Lett (2005) 15 : 5288 -5292
PubMed 16165349 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.81 6.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL200381 1 6.16
CHEMBL371658 1 6.10
CHEMBL371095 1 5.85
CHEMBL199210 1 5.57
CHEMBL197538 1 5.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL200381 IC50 = 700.0 nM 6.16
CHEMBL371658 IC50 = 800.0 nM 6.10
CHEMBL371095 IC50 = 1400.0 nM 5.85
CHEMBL199210 IC50 = 2700.0 nM 5.57
CHEMBL197538 IC50 = 4500.0 nM 5.35