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Assay Detail

CHEMBL1112960

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

Functional
Inhibition of LPS-induced TNFalpha production in human THP1 cells after 4 hrs by ELISA
12
Total Activities
12
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 Autocuration

Target

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

Publication

Synthesis and biological activity of 2H-quinolizin-2-one based p38alpha MAP kinase inhibitors.
Tynebor RM, Chen MH, Natarajan SR, O'Neill EA, Thompson JE, Fitzgerald CE, O'Keefe SJ, Doherty JB.
Bioorg Med Chem Lett (2010) 20 : 2765 -2769
PubMed 20378346 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 6.96 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL219804 1 9.00
CHEMBL94417 1 8.40
CHEMBL1098524 1 8.25
CHEMBL1098554 1 7.62
CHEMBL1096192 1 7.59
CHEMBL1098797 1 6.75
CHEMBL1098822 1 6.58
CHEMBL1098551 1 6.57
CHEMBL1098552 1 6.37
CHEMBL1098546 1 6.02
CHEMBL1098525 1 5.19
CHEMBL1096830 1 5.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL219804 IC50 = 1.0 nM 9.00
CHEMBL94417 IC50 = 4.0 nM 8.40
CHEMBL1098524 IC50 = 5.6 nM 8.25
CHEMBL1098554 IC50 = 23.8 nM 7.62
CHEMBL1096192 IC50 = 25.4 nM 7.59
CHEMBL1098797 IC50 = 180.0 nM 6.75
CHEMBL1098822 IC50 = 265.0 nM 6.58
CHEMBL1098551 IC50 = 270.0 nM 6.57
CHEMBL1098552 IC50 = 430.0 nM 6.37
CHEMBL1098546 IC50 = 950.0 nM 6.02
CHEMBL1098525 IC50 = 6490.0 nM 5.19
CHEMBL1096830 IC50 = 6490.0 nM 5.19