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Assay Detail

CHEMBL1048178

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

Functional
Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha production
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type PBMC
Confidence 1 — Organism
Curated By Autocuration

Target

PBMC (CHEMBL613107)
Type CELL-LINE
Organism Homo sapiens

Publication

Quinolines as a novel structural class of potent and selective PDE4 inhibitors. Optimisation for inhaled administration.
Woodrow MD, Ballantine SP, Barker MD, Clarke BJ, Dawson J, Dean TW, Delves CJ, Evans B, Gough SL, Guntrip SB, Holman S, Holmes DS, Kranz M, Lindvaal MK, Lucas FS, Neu M, Ranshaw LE, Solanke YE, Somers DO, Ward P, Wiseman JO.
Bioorg Med Chem Lett (2009) 19 : 5261 -5265
PubMed 19656678 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 9.19 11.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL570015 GSK-256066 2.0 1 11.00
CHEMBL571381 1 10.50
CHEMBL569791 1 10.00
CHEMBL584327 1 9.30
CHEMBL569556 1 8.90
CHEMBL515240 1 8.20
CHEMBL571171 1 7.80
CHEMBL570029 1 7.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL570015 GSK-256066 IC50 = 0.01 nM 11.00
CHEMBL571381 IC50 = 0.03162 nM 10.50
CHEMBL569791 IC50 = 0.1 nM 10.00
CHEMBL584327 IC50 = 0.5012 nM 9.30
CHEMBL569556 IC50 = 1.259 nM 8.90
CHEMBL515240 IC50 = 6.31 nM 8.20
CHEMBL571171 IC50 = 15.85 nM 7.80
CHEMBL570029 IC50 = 15.85 nM 7.80