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Assay Detail

CHEMBL810024

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

Functional
Inhibition of LPS-stimulated TNF-alpha production in THP-1 cells
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type THP-1
Confidence 1 — Organism
Curated By Expert

Target

THP-1 (CHEMBL614245)
Type CELL-LINE
Organism Homo sapiens

Publication

Design and synthesis of potent, orally bioavailable dihydroquinazolinone inhibitors of p38 MAP kinase.
Stelmach JE, Liu L, Patel SB, Pivnichny JV, Scapin G, Singh S, Hop CE, Wang Z, Strauss JR, Cameron PM, Nichols EA, O'Keefe SJ, O'Neill EA, Schmatz DM, Schwartz CD, Thompson CM, Zaller DM, Doherty JB.
Bioorg Med Chem Lett (2003) 13 : 277 -280
PubMed 12482439 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 9.20 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL328242 1 9.70
CHEMBL419134 1 9.52
CHEMBL419140 1 9.30
CHEMBL316604 1 9.22
CHEMBL96345 1 9.15
CHEMBL327959 1 9.15
CHEMBL327987 1 8.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL328242 IC50 = 0.2 nM 9.70
CHEMBL419134 IC50 = 0.3 nM 9.52
CHEMBL419140 IC50 = 0.5 nM 9.30
CHEMBL316604 IC50 = 0.6 nM 9.22
CHEMBL96345 IC50 = 0.7 nM 9.15
CHEMBL327959 IC50 = 0.7 nM 9.15
CHEMBL327987 IC50 = 4.4 nM 8.36