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Assay Detail

CHEMBL2090339

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 pre-incubated for before LPS challenge and measured 4 hrs post LPS challenge by ELISA
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 1 — Organism
Curated By Autocuration

Target

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

Publication

Synthesis and biological activity of pyridopyridazin-6-one p38α MAP kinase inhibitors. Part 2.
Tynebor RM, Chen MH, Natarajan SR, O'Neill EA, Thompson JE, Fitzgerald CE, O'Keefe SJ, Doherty JB.
Bioorg Med Chem Lett (2012) 22 : 5979 -5983
PubMed 22901390 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 7.42 8.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2088588 1 8.36
CHEMBL2088591 1 8.34
CHEMBL2088578 1 8.28
CHEMBL1098524 1 8.25
CHEMBL2088582 1 8.06
CHEMBL2088575 1 7.75
CHEMBL2088583 1 7.72
CHEMBL1096192 1 7.60
CHEMBL2088586 1 7.54
CHEMBL2088576 1 7.39
CHEMBL2088580 1 7.37
CHEMBL2088585 1 7.35
CHEMBL2088590 1 7.34
CHEMBL2088577 1 7.33
CHEMBL2088579 1 7.10
CHEMBL2088589 1 7.06
CHEMBL2088587 1 6.92
CHEMBL2088584 1 6.92
CHEMBL1098546 1 6.02
CHEMBL2088581 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2088588 IC50 = 4.4 nM 8.36
CHEMBL2088591 IC50 = 4.6 nM 8.34
CHEMBL2088578 IC50 = 5.2 nM 8.28
CHEMBL1098524 IC50 = 5.6 nM 8.25
CHEMBL2088582 IC50 = 8.7 nM 8.06
CHEMBL2088575 IC50 = 18.0 nM 7.75
CHEMBL2088583 IC50 = 19.0 nM 7.72
CHEMBL1096192 IC50 = 25.0 nM 7.60
CHEMBL2088586 IC50 = 29.0 nM 7.54
CHEMBL2088576 IC50 = 41.0 nM 7.39
CHEMBL2088580 IC50 = 43.0 nM 7.37
CHEMBL2088585 IC50 = 45.0 nM 7.35
CHEMBL2088590 IC50 = 46.0 nM 7.34
CHEMBL2088577 IC50 = 47.0 nM 7.33
CHEMBL2088579 IC50 = 80.0 nM 7.10
CHEMBL2088589 IC50 = 88.0 nM 7.06
CHEMBL2088587 IC50 = 120.0 nM 6.92
CHEMBL2088584 IC50 = 120.0 nM 6.92
CHEMBL1098546 IC50 = 950.0 nM 6.02
CHEMBL2088581 IC50 = 2000.0 nM 5.70